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Trial record 20 of 243 for:    "Viral Infectious Disease" | "Lopinavir"

Safety and Tolerability Study to Evaluate Lower Dose of GSK2248761 in Antiretroviral Treatment-Naive HIV-1 Infected Adults.

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ClinicalTrials.gov Identifier: NCT00945282
Recruitment Status : Completed
First Posted : July 24, 2009
Results First Posted : November 29, 2018
Last Update Posted : November 29, 2018
Sponsor:
Collaborator:
GlaxoSmithKline
Information provided by (Responsible Party):
ViiV Healthcare

Study Type Interventional
Study Design Allocation: Randomized;   Intervention Model: Parallel Assignment;   Masking: Double (Participant, Investigator);   Primary Purpose: Treatment
Condition Infection, Human Immunodeficiency Virus
Interventions Drug: GSK2248761
Drug: Lopinavir/ritonavir
Drug: HAART
Drug: Placebo
Enrollment 8
Recruitment Details A total of 8 participants with Treatment-Naive, Human Immuno deficiency virus (HIV-1) infection were randomized to the study. The study was conducted from 20 October 2009 to 28 November 2009 at one center in Argentina.
Pre-assignment Details One participant was initially enrolled in the study, however withdrew consent prior to randomization. The study was planned to be conducted in 2 cohorts, however based on safety and antiviral activity of Cohort 1, a second cohort of participants was not needed and the study was stopped.
Arm/Group Title GSK2248761 30 mg Placebo
Hide Arm/Group Description Eligible participants received 3 capsules of GSK2248761 10 milligrams (mg) orally once daily dosed with 360 milliliter (mL) water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or Highly active antiretroviral therapy (HAART) for 28 days. Eligible participants received matching placebo capsules to GSK2248761 10 mg capsules, orally once daily dosed with 360 mL water after a standard breakfast upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days.
Period Title: Overall Study
Started 6 2
Completed 6 2
Not Completed 0 0
Arm/Group Title GSK2248761 30 mg Placebo Total
Hide Arm/Group Description Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days Eligible participants matching placebo capsules to GSK2248761 10 mg capsules orally once daily dosed with 360 mL water after a standard breakfast upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days Total of all reporting groups
Overall Number of Baseline Participants 6 2 8
Hide Baseline Analysis Population Description
[Not Specified]
Age, Continuous  
Mean (Standard Deviation)
Unit of measure:  Years
Number Analyzed 6 participants 2 participants 8 participants
35.0  (7.10) 28.0  (5.66) 33.3  (7.15)
Sex: Female, Male  
Measure Type: Count of Participants
Unit of measure:  Participants
Number Analyzed 6 participants 2 participants 8 participants
Female
0
   0.0%
0
   0.0%
0
   0.0%
Male
6
 100.0%
2
 100.0%
8
 100.0%
Race (NIH/OMB)  
Measure Type: Count of Participants
Unit of measure:  Participants
Number Analyzed 6 participants 2 participants 8 participants
American Indian or Alaska Native
0
   0.0%
0
   0.0%
0
   0.0%
Asian
0
   0.0%
0
   0.0%
0
   0.0%
Native Hawaiian or Other Pacific Islander
0
   0.0%
0
   0.0%
0
   0.0%
Black or African American
1
  16.7%
0
   0.0%
1
  12.5%
White
5
  83.3%
2
 100.0%
7
  87.5%
More than one race
0
   0.0%
0
   0.0%
0
   0.0%
Unknown or Not Reported
0
   0.0%
0
   0.0%
0
   0.0%
1.Primary Outcome
Title Number of Participants With Serious Adverse Events (SAEs) and Adverse Events (AEs)
Hide Description An AE is defined as any untoward medical occurrence in a clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of a medicinal product. An SAE is defined as any untoward medical occurrence that, at any dose, results in death, is life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, or is a congenital anomaly/birth defect, or is an important medical events that jeopardize the participants or may require medical or surgical intervention to prevent one of the other outcomes listed in the above definition, or a drug-induced liver injury.
Time Frame Up to 38 days
Hide Outcome Measure Data
Hide Analysis Population Description
Safety population was defined as all participants who were randomized into the study with documented evidence of receipt of at least one dose of randomized treatment.
Arm/Group Title GSK2248761 30 mg Placebo
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days.
Eligible participants matching placebo capsules to GSK2248761 10 mg capsules orally once daily dosed with 360 mL water after a standard breakfast upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days.
Overall Number of Participants Analyzed 6 2
Measure Type: Count of Participants
Unit of Measure: Participants
Any AE
4
  66.7%
1
  50.0%
Any SAE
0
   0.0%
0
   0.0%
2.Primary Outcome
Title Change From Baseline in Hematology Paramaters- Basophils, Eosinophils, Lymphocytes, Monocytes, White Blood Cell Count
Hide Description The data for hematology parameters for Basophils, eosinophils, lymphocytes, monocytes, and white blood cell count from the change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise.
Time Frame Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)
Hide Outcome Measure Data
Hide Analysis Population Description
Safety population.
Arm/Group Title GSK2248761 30 mg Placebo
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days. Eligible participants matching placebo capsules to GSK2248761 10 mg capsules orally once daily dosed with 360 mL water after a standard breakfast upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days.
Eligible participants matching placebo capsules to GSK2248761 10 mg capsules orally once daily dosed with 360 mL water after a standard breakfast upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days.
Overall Number of Participants Analyzed 6 2
Mean (Standard Deviation)
Unit of Measure: thousand cells per microliter
Basophils, Day 2 -1.7  (4.08) -5.0  (7.07)
Basophils, Day 4 8.3  (9.83) 5.0  (7.07)
Basophils, Day 7 1.7  (7.53) -10.0  (14.14)
Basophils, Day 8 3.3  (8.16) -10.0  (14.14)
Basophils, Follow-Up -3.3  (10.33) -15.0  (7.07)
Eosinophils, Day 2 -1.7  (35.45) -120.0  (141.42)
Eosinophils, Day 4 -60.0  (150.33) -20.0  (0.00)
Eosinophils, Day 7 -38.3  (106.85) -50.0  (28.28)
Eosinophils, Day 8 -96.7  (229.49) -80.0  (70.71)
Eosinophils, Follow-Up -63.3  (153.84) -135.0  (162.63)
Lymphocytes, Day 2 -120.0  (272.18) 315.0  (1067.73)
Lymphocytes, Day 4 268.3  (298.83) 260.0  (296.98)
Lymphocytes, Day 7 126.7  (415.44) 180.0  (410.12)
Lymphocytes, Day 8 273.3  (357.64) 480.0  (1060.66)
Lymphocytes, Follow-Up -110.0  (375.34) 50.0  (551.54)
Monocytes, Day 2 28.3  (71.11) 125.0  (176.78)
Monocytes, Day 4 33.3  (76.59) 120.0  (155.56)
Monocytes, Day 7 -15.0  (135.17) 25.0  (77.78)
Monocytes, Day 8 23.3  (103.67) 75.0  (134.35)
Monocytes, Follow-Up 10.0  (143.67) -115.0  (35.36)
White blood cell, Day 2 148.3  (649.78) 1295.0  (2849.64)
White blood cell, Day 4 758.3  (896.78) -10.0  (155.56)
White blood cell, Day 7 45.0  (1017.70) -600.0  (367.70)
White blood cell, Day 8 500.0  (776.79) -240.0  (1513.21)
White blood cell, Follow-Up -90.0  (699.29) -110.0  (2573.87)
3.Primary Outcome
Title Change From Baseline in Hematology Paramaters- Hemoglobin
Hide Description The data for hematology parameter hemoglobin from the change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise.
Time Frame Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)
Hide Outcome Measure Data
Hide Analysis Population Description
Safety population.
Arm/Group Title GSK2248761 30 mg Placebo
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Eligible participants matching placebo capsules to GSK2248761 10 mg capsules orally once daily dosed with 360 mL water after a standard breakfast upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Overall Number of Participants Analyzed 6 2
Mean (Standard Deviation)
Unit of Measure: gram per decilitre
Day 2 -0.40  (0.316) -0.50  (0.283)
Day 4 -0.28  (0.794) 0.60  (1.273)
Day 7 -0.25  (0.864) -0.45  (0.071)
Day 8 -0.48  (0.585) -0.45  (0.354)
Follow-up -0.93  (0.550) -1.00  (0.424)
4.Primary Outcome
Title Change From Baseline in Hematology Paramaters- Platelet Count
Hide Description The data for hematology parameter platelet count, for the change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise.
Time Frame Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)
Hide Outcome Measure Data
Hide Analysis Population Description
Safety population.
Arm/Group Title GSK2248761 30 mg Placebo
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Eligible participants matching placebo capsules to GSK2248761 10 mg capsules orally once daily dosed with 360 mL water after a standard breakfast upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Overall Number of Participants Analyzed 6 2
Mean (Standard Deviation)
Unit of Measure: per cubic millimeter
Day 2 -5.7  (24.86) 3.0  (9.90)
Day 4 5.0  (18.34) -23.5  (37.48)
Day 7 18.5  (19.77) 2.5  (10.61)
Day 8 29.3  (21.04) 2.0  (2.83)
Follow-up 23.3  (6.50) -1.0  (33.94)
5.Primary Outcome
Title Change From Baseline in Hematology Paramaters- Red Blood Cell Count
Hide Description The data for hematology parameter red blood cell count, for the change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise.
Time Frame Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)
Hide Outcome Measure Data
Hide Analysis Population Description
Safety population.
Arm/Group Title GSK2248761 30 mg Placebo
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Eligible participants matching placebo capsules to GSK2248761 10 mg capsules orally once daily dosed with 360 mL water after a standard breakfast upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Overall Number of Participants Analyzed 6 2
Mean (Standard Deviation)
Unit of Measure: million cells per microliter
Day 2 -0.153  (0.1129) -0.240  (0.0283)
Day 4 -0.112  (0.2601) 0.200  (0.4525)
Day 7 -0.083  (0.2947) -0.190  (0.0707)
Day 8 -0.170  (0.1764) -0.170  (0.1556)
Follow-up -0.343  (0.2300) -0.375  (0.1344)
6.Primary Outcome
Title Change From Baseline in Hematology Parameters- Total Neutrophil
Hide Description The data for hematology parameter total neutrophil count, for the change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise.
Time Frame Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)
Hide Outcome Measure Data
Hide Analysis Population Description
Safety population.
Arm/Group Title GSK2248761 30 mg Placebo
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Eligible participants matching placebo capsules to GSK2248761 10 mg capsules orally once daily dosed with 360 mL water after a standard breakfast upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Overall Number of Participants Analyzed 6 2
Mean (Standard Deviation)
Unit of Measure: giga cells per liter
Day 2 243.3  (499.83) 980.0  (1753.62)
Day 4 508.3  (692.05) -375.0  (21.21)
Day 7 -30.0  (750.55) -745.0  (49.50)
Day 8 296.7  (535.82) -705.0  (374.77)
Follow-up 76.7  (433.34) 105.0  (2142.53)
7.Primary Outcome
Title Change From Baseline in Hematology Paramaters- Mean Corpuscle Hemoglobin (MCH)
Hide Description The data for hematology parameter MCH, the change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise.
Time Frame Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)
Hide Outcome Measure Data
Hide Analysis Population Description
Safety population.
Arm/Group Title GSK2248761 30 mg Placebo
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Eligible participants matching placebo capsules to GSK2248761 10 mg capsules orally once daily dosed with 360 mL water after a standard breakfast upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Overall Number of Participants Analyzed 6 2
Mean (Standard Deviation)
Unit of Measure: picogram
Day 2 0.07  (0.197) 0.45  (0.495)
Day 4 0.08  (0.147) 0.05  (0.071)
Day 7 0.03  (0.320) 0.20  (0.283)
Day 8 0.07  (0.151) 0.10  (0.141)
Follow-up 0.13  (0.367) 0.25  (0.071)
8.Primary Outcome
Title Change From Baseline in Hematology Paramaters- Mean Corpuscle Volume (MCV)
Hide Description The change from baseline data for hematology parameter MCV, was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise.
Time Frame Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)
Hide Outcome Measure Data
Hide Analysis Population Description
Safety population.
Arm/Group Title GSK2248761 30 mg Placebo
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Eligible participants matching placebo capsules to GSK2248761 10 mg capsules orally once daily dosed with 360 mL water after a standard breakfast upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Overall Number of Participants Analyzed 6 2
Mean (Standard Deviation)
Unit of Measure: femtoliters
Day 2 0.27  (1.109) -0.10  (0.990)
Day 4 0.15  (0.698) -0.20  (0.990)
Day 7 -0.10  (0.341) -0.40  (0.283)
Day 8 0.13  (0.333) -0.15  (0.354)
Follow-up 0.47  (0.753) -0.50  (0.566)
9.Primary Outcome
Title Change From Baseline in Hematology Paramaters- Hematocrit
Hide Description The data for hematology parameter Hematocrit, the change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise.
Time Frame Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)
Hide Outcome Measure Data
Hide Analysis Population Description
Safety population.
Arm/Group Title GSK2248761 30 mg Placebo
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Eligible participants matching placebo capsules to GSK2248761 10 mg capsules orally once daily dosed with 360 mL water after a standard breakfast upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Overall Number of Participants Analyzed 6 2
Mean (Standard Deviation)
Unit of Measure: percentage of red blood cells
Day 2 -1.22  (1.286) -2.15  (0.212)
Day 4 -0.92  (2.110) 1.70  (3.536)
Day 7 -0.80  (2.563) -1.85  (0.495)
Day 8 -1.45  (1.508) -1.55  (1.202)
Follow-up -2.78  (1.907) -3.55  (0.919)
10.Primary Outcome
Title Change From Baseline in Hematology Paramaters-Mean Corpuscle Hemoglobin Concentration
Hide Description The data for hematology parameter Mean Corpuscle Hemoglobin concentration, the change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise.
Time Frame Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)
Hide Outcome Measure Data
Hide Analysis Population Description
Safety population
Arm/Group Title GSK2248761 30 mg Placebo
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Eligible participants matching placebo capsules to GSK2248761 10 mg capsules orally once daily dosed with 360 mL water after a standard breakfast upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Overall Number of Participants Analyzed 6 2
Mean (Standard Deviation)
Unit of Measure: percentage of red blood cells
Day 2 0.02  (0.445) 0.55  (0.778)
Day 4 0.05  (0.373) 0.15  (0.212)
Day 7 0.07  (0.361) 0.40  (0.283)
Day 8 0.02  (0.214) 0.15  (0.212)
Follow-up -0.03  (0.301) 0.45  (0.212)
11.Primary Outcome
Title Change From Baseline in Clinical Chemistry Paramaters- Albumin and Total Protein
Hide Description The data for clinical chemistry parameters Albumin and total protein, the change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise.
Time Frame Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)
Hide Outcome Measure Data
Hide Analysis Population Description
Safety population.
Arm/Group Title GSK2248761 30 mg Placebo
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days.
Eligible participants matching placebo capsules to GSK2248761 10 mg capsules orally once daily dosed with 360 mL water after a standard breakfast upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days.
Overall Number of Participants Analyzed 6 2
Mean (Standard Deviation)
Unit of Measure: gram per deciliter
Albumin, Day 2 -0.17  (0.207) -0.20  (0.000)
Albumin, Day 4 -0.08  (0.248) 0.00  (0.000)
Albumin, Day 7 -0.10  (0.283) -0.05  (0.212)
Albumin, Day 8 -0.05  (0.383) -0.10  (0.000)
Albumin, Follow-up -0.07  (0.137) 0.05  (0.071)
Total protein, Day 2 -0.45  (0.302) -0.55  (0.212)
Total protein, Day 4 -0.10  (0.385) -0.10  (0.283)
Total protein, Day 7 0.10  (0.494) 0.05  (0.071)
Total protein, Day 8 0.00  (0.636) -0.25  (0.071)
Total protein, Follow-up -0.30  (0.268) -0.20  (0.283)
12.Primary Outcome
Title Change From Baseline in Clinical Chemistry Parameters- Blood Urea Nitrogen, Triglycerides, Glucose, Creatinine, Calcium, Cholesterol, Total Bilirubin, and Direct Bilirubin.
Hide Description The data for clinical chemistry parameters- Blood urea nitrogen, triglycerides, glucose, creatinine, calcium, cholesterol, total bilirubin, and direct bilirubin. The change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise.
Time Frame Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)
Hide Outcome Measure Data
Hide Analysis Population Description
Safety population.
Arm/Group Title GSK2248761 30 mg Placebo
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Eligible participants matching placebo capsules to GSK2248761 10 mg capsules orally once daily dosed with 360 mL water after a standard breakfast upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days.
Overall Number of Participants Analyzed 6 2
Mean (Standard Deviation)
Unit of Measure: milligram per deciliter
Blood urea nitrogen, Day 2 1.5  (7.20) -1.0  (2.83)
Blood urea nitrogen, Day 4 4.3  (5.32) 4.0  (5.66)
Blood urea nitrogen, Day 7 1.0  (7.67) 3.5  (2.12)
Blood urea nitrogen, Day 8 2.7  (6.38) 5.5  (9.19)
Blood urea nitrogen, Follow-up -2.2  (7.41) 1.0  (15.56)
Triglycerides, Day 2 -17.8  (19.05) 5.0  (14.14)
Triglycerides, Day 4 -19.8  (16.47) 5.5  (4.95)
Triglycerides, Day 7 5.2  (21.44) 20.5  (27.58)
Triglycerides, Day 8 20.8  (63.05) 34.0  (21.21)
Triglycerides, Follow-up -3.0  (12.63) 114.0  (8.49)
Glucose, Day 2 1.3  (9.18) 6.0  (4.24)
Glucose, Day 4 0.0  (10.92) -0.5  (12.02)
Glucose, Day 7 -1.8  (7.86) -1.0  (1.41)
Glucose, Day 8 -5.2  (10.72) -5.0  (2.83)
Glucose, Follow-up 3.0  (5.76) 10.0  (4.24)
Creatinine, Day 2 -0.048  (0.0770) 0.000  (0.0000)
Creatinine, Day 4 0.025  (0.0586) 0.025  (0.0071)
Creatinine, Day 7 -0.003  (0.0455) 0.035  (0.0919)
Creatinine, Day 8 -0.060  (0.0569) -0.040  (0.1273)
Creatinine, Follow-up -0.003  (0.1183) 0.060  (0.1273)
Calcium, Day 2 -0.25  (0.176) -0.25  (0.071)
Calcium, Day 4 -0.13  (0.301) 0.05  (0.071)
Calcium, Day 7 -0.40  (0.322) -0.20  (0.141)
Calcium, Day 8 -0.47  (0.418) -0.45  (0.354)
Calcium, Follow-up 0.08  (0.299) 0.05  (0.071)
Cholesterol, Day 2 -11.8  (13.92) -12.0  (8.49)
Cholesterol, Day 4 -15.3  (28.72) -17.5  (10.61)
Cholesterol, Day 7 -12.0  (35.25) -20.5  (7.78)
Cholesterol, Day 8 -8.3  (41.15) -13.5  (0.71)
Cholesterol, Follow-up -5.5  (33.44) -0.5  (17.68)
Total bilirubin, Day 2 -0.12  (0.160) -0.10  (0.141)
Total bilirubin, Day 4 -0.08  (0.133) -0.15  (0.071)
Total bilirubin, Day 7 -0.03  (0.121) -0.05  (0.071)
Total bilirubin, Day 8 -0.08  (0.075) -0.10  (0.000)
Total bilirubin, Follow-up 0.08  (0.240) 0.00  (0.000)
Direct bilirubin, Day 2 -0.08  (0.041) 0.00  (0.000)
Direct bilirubin, Day 4 -0.08  (0.041) 0.00  (0.000)
Direct bilirubin, Day 7 -0.05  (0.055) 0.05  (0.071)
Direct bilirubin, Day 8 -0.05  (0.055) 0.00  (0.000)
Direct bilirubin, Follow-up 0.02  (0.075) 0.10  (0.000)
13.Primary Outcome
Title Change From Baseline in Clinical Chemistry Paramaters- Alkaline Phosphatase, Alanine Amino Transferase, Aspartate Amino Transferase
Hide Description The data for clinical chemistry paramaters- alkaline phosphatase, alanine amino transferase, aspartate amino transferase, the change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise.
Time Frame Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)
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Safety population.
Arm/Group Title GSK2248761 30 mg Placebo
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Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Eligible participants matching placebo capsules to GSK2248761 10 mg capsules orally once daily dosed with 360 mL water after a standard breakfast upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Overall Number of Participants Analyzed 6 2
Mean (Standard Deviation)
Unit of Measure: International units (IU) per liter
Alkaline phosphatase, Day 2 -5.8  (7.14) -16.0  (0.00)
Alkaline phosphatase, Day 4 -1.5  (10.33) -16.0  (8.49)
Alkaline phosphatase, Day 7 1.8  (10.83) -7.5  (4.95)
Alkaline phosphatase, Day 8 3.3  (14.88) -14.5  (6.36)
Alkaline phosphatase, Follow-up 4.2  (24.96) -9.5  (0.71)
Alanine amino transferase, Day 2 -3.0  (6.63) 0.5  (6.36)
Alanine amino transferase, Day 4 -2.0  (15.02) -3.5  (4.95)
Alanine amino transferase, Day 7 1.7  (21.81) -3.5  (4.95)
Alanine amino transferase, Day 8 3.7  (24.40) 0.0  (5.66)
Alanine amino transferase, Follow-up -7.2  (21.81) -1.5  (6.36)
Aspartate amino transferase, Day 2 0.8  (4.17) 1.0  (1.41)
Aspartate amino transferase, Day 4 -0.2  (7.31) -4.5  (3.54)
Aspartate amino transferase, Day 7 -0.3  (7.69) -3.0  (8.49)
Aspartate amino transferase, Day 8 1.7  (9.40) 0.0  (5.66)
Aspartate amino transferase, Follow-up -0.2  (8.40) 2.5  (4.95)
14.Primary Outcome
Title Change From Baseline in Clinical Chemistry Paramaters-sodium, Potassium and Carbondioxide or Bicarbonate
Hide Description The data for clinical chemistry parameters- sodium, potassium and carbon dioxide or bicarbonate, the change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise.
Time Frame Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)
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Safety population.
Arm/Group Title GSK2248761 30 mg Placebo
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Eligible participants matching placebo capsules to GSK2248761 10 mg capsules orally once daily dosed with 360 mL water after a standard breakfast upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days.
Overall Number of Participants Analyzed 6 2
Mean (Standard Deviation)
Unit of Measure: milliequivalents per liter
Sodium, Day 2 -1.2  (1.17) -0.5  (2.12)
Sodium, Day 4 -0.8  (1.60) 1.0  (1.41)
Sodium, Day 7 -1.5  (1.64) 0.0  (0.00)
Sodium, Day 8 -1.7  (1.51) -0.5  (0.71)
Sodium, Follow-up 2.3  (1.63) 1.0  (1.41)
Potassium, Day 2 -0.02  (0.293) -0.25  (0.071)
Potassium, Day 4 0.10  (0.434) 0.10  (0.566)
Potassium, Day 7 -0.17  (0.314) -0.10  (0.000)
Potassium, Day 8 -0.18  (0.371) -0.00  (0.141)
Potassium, Follow-up -0.08  (0.360) -0.30  (0.424)
Carbondioxide, Day 2 -0.80  (2.384) -1.35  (2.051)
Carbondioxide, Day 4 3.17  (1.488) 2.70  (4.101)
Carbondioxide, Day 7 2.93  (1.850) 3.60  (2.121)
Carbondioxide, Day 8 0.87  (2.471) 1.65  (1.768)
Carbondioxide, Follow-up 2.03  (2.187) -0.30  (1.131)
15.Primary Outcome
Title Change From Baseline in Clinical Chemistry Paramaters- Phosphorus
Hide Description The data for clinical chemistry paramaters- phosphorous, the change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise.
Time Frame Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)
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Safety population.
Arm/Group Title GSK2248761 30 mg Placebo
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Eligible participants matching placebo capsules to GSK2248761 10 mg capsules orally once daily dosed with 360 mL water after a standard breakfast upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Overall Number of Participants Analyzed 6 2
Mean (Standard Deviation)
Unit of Measure: millimole per liter
Phosphorus, Day 2 -0.05  (0.524) -0.80  (0.707)
Phosphorus, Day 4 0.07  (0.799) 0.25  (0.212)
Phosphorus, Day 7 -0.17  (0.628) -0.00  (0.141)
Phosphorus, Day 8 -0.27  (0.662) -0.35  (0.071)
Phosphorus, Follow-up -0.58  (0.634) -0.95  (0.071)
16.Primary Outcome
Title Change From Baseline in Clinical Chemistry Paramaters- Uric Acid
Hide Description The data for clinical chemistry parameters Uric acid, the change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise.
Time Frame Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)
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Safety population.
Arm/Group Title GSK2248761 30 mg Placebo
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Eligible participants matching placebo capsules to GSK2248761 10 mg capsules orally once daily dosed with 360 mL water after a standard breakfast upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Overall Number of Participants Analyzed 6 2
Mean (Standard Deviation)
Unit of Measure: Micromole per liter
Uric acid, Day 2 0.27  (0.250) -0.55  (0.212)
Uric acid, Day 4 0.17  (0.408) -0.70  (0.283)
Uric acid, Day 7 -0.15  (0.561) -0.80  (0.707)
Uric acid, Day 8 -0.60  (0.970) -1.05  (0.071)
Uric acid, Follow-up -0.53  (0.784) -0.80  (0.566)
17.Primary Outcome
Title Change From Baseline in Clinical Chemistry Paramaters- Thyroxine, Free
Hide Description The data for clinical chemistry parameters Thyroxine, free the change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise.
Time Frame Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)
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Safety population.
Arm/Group Title GSK2248761 30 mg Placebo
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days.
Eligible participants matching placebo capsules to GSK2248761 10 mg capsules orally once daily dosed with 360 mL water after a standard breakfast upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Overall Number of Participants Analyzed 6 2
Mean (Standard Deviation)
Unit of Measure: Picomole per liter
Thyroxine free, Day 2 -0.018  (0.0768) 0.015  (0.0636)
Thyroxine free, Day 4 0.108  (0.1320) 0.190  (0.0283)
Thyroxine free, Day 7 0.065  (0.1011) 0.120  (0.1414)
Thyroxine free, Day 8 0.117  (0.1221) 0.130  (0.0424)
Thyroxine free, Follow- up 0.072  (0.1332) 0.135  (0.1485)
18.Primary Outcome
Title Change From Baseline in Clinical Chemistry Paramaters- Thyroxine Total, Thyroxine Binding Globulin, Total T3.
Hide Description The data for clinical chemistry parameters Thyroxine total, thyroxine binding globulin, Total T3 the change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise.
Time Frame Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)
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Safety population.
Arm/Group Title GSK2248761 30 mg Placebo
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Eligible participants matching placebo capsules to GSK2248761 10 mg capsules orally once daily dosed with 360 mL water after a standard breakfast upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Overall Number of Participants Analyzed 6 2
Mean (Standard Deviation)
Unit of Measure: Nanomoles per liter
Thyroxine total, Day 2 -0.60  (0.648) -0.40  (0.707)
Thyroxine total, Day 4 -0.08  (0.979) 0.50  (0.283)
Thyroxine total, Day 7 -0.28  (0.773) 0.10  (0.707)
Thyroxine total, Day 8 0.00  (0.874) 0.00  (0.141)
Thyroxine total, Follow-up -0.37  (1.019) 0.05  (1.202)
Thyroxine binding globulin, Day 2 -0.33  (5.645) 2.00  (2.828)
Thyroxine binding globulin, Day 4 -5.00  (3.688) -6.50  (3.536)
Thyroxine binding globulin, Day 7 -0.67  (7.005) -3.00  (8.485)
Thyroxine binding globulin, Day 8 0.17  (1.169) -1.00  (2.828)
Thyroxine binding globulin, Follow-up -1.83  (2.787) -1.00  (8.485)
Total T3, Day 2 -0.013  (0.1334) 0.170  (0.2404)
Total T3, Day 4 0.068  (0.2180) 0.310  (0.2687)
Total T3, Day 7 -0.055  (0.1435) 0.225  (0.2333)
Total T3, Day 8 -0.035  (0.1252) 0.190  (0.0141)
Total T3, Follow-up -0.005  (0.1945) 0.375  (0.1344)
19.Primary Outcome
Title Number of Participants With Abnormal Electrocardiogram (ECG) Findings
Hide Description Triplicate 12-lead ECGs were collected at different timepoints, after participants were supine for 5 minutes, during the study using an ECG machine that automatically calculated the heart rate (HR) and measures PR, QRS, QT, and QTc intervals. The three consecutive determinations were collected 5 plus or minus 2 minutes apart and all three tracings were recorded. The participants with abnormal values categorized as abnormal clinically significant (CS) and not clinically significant (NCS) were reported.
Time Frame Day 1, Day 4, Day 7, Day 8 and follow-up
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Safety population.
Arm/Group Title GSK2248761 30 mg Placebo
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Eligible participants matching placebo capsules to GSK2248761 10 mg capsules orally once daily dosed with 360 mL water after a standard breakfast upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Overall Number of Participants Analyzed 6 2
Measure Type: Count of Participants
Unit of Measure: Participants
Day 1, Pre-dose, NCS
3
  50.0%
0
   0.0%
Day 1, 4 hour, NCS
2
  33.3%
0
   0.0%
Day 1, 8 hour, NCS
2
  33.3%
0
   0.0%
Day 4, Pre-dose, NCS
2
  33.3%
0
   0.0%
Day 4, 4 hour, NCS
2
  33.3%
0
   0.0%
Day 4, 8 hour, NCS
3
  50.0%
0
   0.0%
Day 7, Pre-dose, NCS
3
  50.0%
0
   0.0%
Day 7, 4 hour, NCS
3
  50.0%
0
   0.0%
Day 7, 8 hour, NCS
2
  33.3%
0
   0.0%
Day 8, Pre-dose, NCS
3
  50.0%
0
   0.0%
Follow-up, NCS
3
  50.0%
0
   0.0%
20.Primary Outcome
Title Change From Baseline in Vital Signs-systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP)
Hide Description Vital sign measurements for SBP and DBP after sitting for 5 minutes were measured. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise.
Time Frame Baseline (pre-dose at Day -1 or Day 1) and Day 1, 4, 7 , Day 8 and Follow-up (Day 14)
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Safety population.
Arm/Group Title GSK2248761 30 mg Placebo
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Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Eligible participants matching placebo capsules to GSK2248761 10 mg capsules orally once daily dosed with 360 mL water after a standard breakfast upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Overall Number of Participants Analyzed 6 2
Mean (Standard Deviation)
Unit of Measure: millimeters of mercury
SBP, Day 1, 4 hour 4.3  (6.35) -4.5  (14.85)
SBP, Day 4, Pre-dose -0.7  (5.92) 0.5  (17.68)
SBP, Day 4, 4 hour 3.0  (11.70) 12.5  (14.85)
SBP, Day 7, Pre-dose 6.2  (6.94) 6.5  (9.19)
SBP, Day 7, 4 hour 9.8  (2.71) 14.5  (12.02)
SBP, Day 8 8.5  (7.48) 13.5  (19.09)
SBP, Follow-up 5.8  (7.33) 14.5  (6.36)
DBP, Day 1, 4 hour 8.2  (8.16) 1.0  (1.41)
DBP, Day 4, Pre-dose 5.8  (16.58) 1.0  (15.56)
DBP, Day 4, 4 hour 9.7  (10.21) 3.0  (12.73)
DBP, Day 7, Pre-dose 8.2  (10.96) 7.0  (7.07)
DBP, Day 7, 4 hour 6.0  (9.80) 8.0  (2.83)
DBP, Day 8 5.2  (10.25) 15.0  (9.90)
DBP, Follow-up 4.5  (9.07) 8.0  (5.66)
21.Primary Outcome
Title Change From Baseline in HR
Hide Description Vital sign measurements for HR after sitting for 5 minutes were measured. The average mean values were measured. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise.
Time Frame Baseline (pre-dose at Day -1 or Day 1) and Day 1 (4-hour), Day 4 (Pre-dose and 4 hour), Day 7 (pre-dose and 4-hour), Day 8 and follow up (Day 14)
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Safety population.
Arm/Group Title GSK2248761 30 mg Placebo
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Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Eligible participants matching placebo capsules to GSK2248761 10 mg capsules orally once daily dosed with 360 mL water after a standard breakfast upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Overall Number of Participants Analyzed 6 2
Mean (Standard Deviation)
Unit of Measure: Beats per minute
HR , Day 1, 4 hour -2.5  (6.50) -3.0  (4.24)
HR, Day 4, Pre-dose -2.7  (6.12) -6.0  (11.31)
HR, Day 4, 4 hour -2.2  (3.92) -6.0  (21.21)
HR, Day 7, Pre-dose 3.0  (7.54) -1.0  (22.63)
HR, Day 7, 4 hour -0.3  (4.63) -2.5  (17.68)
HR, Day 8 3.7  (7.42) 0.0  (12.73)
HR, Follow-up -0.3  (5.99) 5.0  (11.31)
22.Primary Outcome
Title Change From Baseline Through Day 8 in Plasma HIV-1 RNA
Hide Description The quantitative analysis of plasma was done to evaluate the amount of HIV-1 RNA at Day 1,2,3,4,5,6,7, 8 and End of treatment visit. The quantification was done using a Polymerase chain reactor (PCR). The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose Day 1) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise.
Time Frame Baseline (pre-dose Day 1) to Day 8
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The Intent-to-treat Exposed (ITT) Population was defined as all participants who met the study criteria and were randomized into the study with documented evidence of having received at least 1 dose of randomized treatment and at least one post-baseline HIV-1 RNA measurement and have Day 1 HIV-RNA>1500 copies/mL.
Arm/Group Title GSK2248761 30 mg Placebo
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Eligible participants matching placebo capsules to GSK2248761 10 mg capsules orally once daily dosed with 360 mL water after a standard breakfast upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Overall Number of Participants Analyzed 6 2
Mean (Standard Deviation)
Unit of Measure: log 10 copies per milliliter (mL)
-0.967  (0.3988) -0.036  (0.2495)
Show Statistical Analysis 1 Hide Statistical Analysis 1
Statistical Analysis Overview Comparison Group Selection GSK2248761 30 mg, Placebo
Comments [Not Specified]
Type of Statistical Test Superiority
Comments [Not Specified]
Statistical Test of Hypothesis P-Value 0.042
Comments [Not Specified]
Method ANCOVA
Comments [Not Specified]
Method of Estimation Estimation Parameter Mean Difference (Final Values)
Estimated Value -0.932
Confidence Interval (2-Sided) 95%
-1.812 to -0.053
Estimation Comments [Not Specified]
23.Primary Outcome
Title Change From Baseline to Nadir in Plasma HIV-1 RNA
Hide Description The quantification of plasma HIV-1 RNA, was conducted for the change from baseline to on treatment nadir (maximum change) before starting HAART or Kaletra monotherapy on Day 8. The quantification was done using a PCR. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise.
Time Frame Baseline (pre-dose Day 1) to Day 8
Hide Outcome Measure Data
Hide Analysis Population Description
ITT population.
Arm/Group Title GSK2248761 30 mg Placebo
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days.
Eligible participants matching placebo capsules to GSK2248761 10 mg capsules orally once daily dosed with 360 mL water after a standard breakfast upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Overall Number of Participants Analyzed 6 2
Mean (Standard Deviation)
Unit of Measure: log10 copies/mL
-1.019  (0.3687) -0.580  (0.0157)
Show Statistical Analysis 1 Hide Statistical Analysis 1
Statistical Analysis Overview Comparison Group Selection GSK2248761 30 mg, Placebo
Comments [Not Specified]
Type of Statistical Test Superiority
Comments [Not Specified]
Statistical Test of Hypothesis P-Value 0.221
Comments [Not Specified]
Method ANCOVA
Comments [Not Specified]
Method of Estimation Estimation Parameter Mean Difference (Final Values)
Estimated Value -0.413
Confidence Interval (2-Sided) 95%
-1.173 to 0.347
Estimation Comments [Not Specified]
24.Primary Outcome
Title HIV-1 Rate of Decline by Treatment
Hide Description The rate of decrease in the viral load of HIV-1 virus in response to individual treatment was measured. The viral load data was assumed to have a log normal prior distribution and followed linear decline with non-informative conjugate prior densities. The rate of decline (slope of the day) for each treatment was measured using a PCR from Day 1 to Day 8. The slope has been reported as mean.
Time Frame Day 1 to Day 8
Hide Outcome Measure Data
Hide Analysis Population Description
ITT population.
Arm/Group Title GSK2248761 30 mg Placebo
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Eligible participants matching placebo capsules to GSK2248761 10 mg capsules orally once daily dosed with 360 mL water after a standard breakfast upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Overall Number of Participants Analyzed 6 2
Mean (90% Confidence Interval)
Unit of Measure: log10 copies/mL
-0.1243
(-0.1478 to -0.1008)
0.0189
(-0.0645 to 0.1023)
Show Statistical Analysis 1 Hide Statistical Analysis 1
Statistical Analysis Overview Comparison Group Selection GSK2248761 30 mg
Comments Day 1 to Day 8
Type of Statistical Test Superiority or Other
Comments [Not Specified]
Statistical Test of Hypothesis P-Value <0.0001
Comments The p-value is the value for GSK2248761 30 mg, at Day 1 to Day 8
Method Mixed Models Analysis
Comments [Not Specified]
Show Statistical Analysis 2 Hide Statistical Analysis 2
Statistical Analysis Overview Comparison Group Selection Placebo
Comments Placebo, Day 1 to Day 8
Type of Statistical Test Superiority or Other
Comments [Not Specified]
Statistical Test of Hypothesis P-Value 0.6922
Comments The p-value is the value for placebo, at Day 1 to Day 8
Method Mixed Models Analysis
Comments [Not Specified]
25.Primary Outcome
Title GSK2248761 Pharmacokinetic (PK) Parameters Following Dose Administration on Day 1: Area Under the Plasma Concentration Time Curve 0 to Infinite (AUC[0-∞]) and Area Under the Plasma Concentration Time Curve (AUC [0-24])
Hide Description AUC (0-24), measured the plasma concentration of GSK2248761 against time, from time zero (pre-dose) to 24 hrs post-dose AUC (0-24) and from time zero to extrapolated infinite time AUC (0-∞). Serial blood samples were collected on Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours postdose on Day 1 and used for analysis.
Time Frame Day 1 (Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours post-dose)
Hide Outcome Measure Data
Hide Analysis Population Description
The PK Concentration Population included all participants who received GSK22648761 and underwent plasma PK sampling during the study. Participants for whom a plasma PK sample was obtained and assayed were included in the listing of plasma GSK2248761 concentration-time data.
Arm/Group Title GSK2248761 30 mg
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Overall Number of Participants Analyzed 6
Geometric Mean (Geometric Coefficient of Variation)
Unit of Measure: hours*nanograms (ng)/mL
AUC(0-inf)
2217.73
(45%)
AUC(0-24)
1842.19
(41%)
26.Primary Outcome
Title GSK2248761 PK Parameters Following Dose Administration on Day 1: Maximum Observed Concentration (Cmax) and Concentration at 24 Hours Post Dose (C24)
Hide Description Cmax represents the maximum concentration of GSK2248761 in the plasma. C24 is defined as the measure of plasma drug concentration of GSK2248761, 24 hours post dose, determined on Day 1. Serial blood samples were collected on Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours postdose on Day 1 and used for analysis.Data for dose normalized Cmax and C24 was reported.
Time Frame Day 1 (Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours)
Hide Outcome Measure Data
Hide Analysis Population Description
PK population.
Arm/Group Title GSK2248761 30 mg
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Overall Number of Participants Analyzed 6
Geometric Mean (Geometric Coefficient of Variation)
Unit of Measure: ng/mL
Cmax
585.43
(39%)
C24
103.40
(61%)
27.Primary Outcome
Title GSK2248761 PK Parameters Following Dose Administration on Day 7: Predose Concentration (C0), Concentration at End of Dosing Interval (Cτ), Minimum Observed Concentration During One Dosing Interval (Cmin) and Cmax
Hide Description The C0 was defined as the concentration of drug in plasma, before dose administration on Day 7. Cτ, was defined as the concentration of drug in the plasma at the end of dosing interval. The Cmin was defined as the minimum concentration of the drug in plasma during one dosing interval on Day 7. Cmax represents the maximum concentration of GSK2248761 in the plasma on Day 7. Serial blood samples were collected on Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours postdose on Day 7 and used for analysis.
Time Frame Day 7 (Pre -dose, 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours post-dose)
Hide Outcome Measure Data
Hide Analysis Population Description
PK population.
Arm/Group Title GSK2248761 30 mg
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Overall Number of Participants Analyzed 6
Geometric Mean (Geometric Coefficient of Variation)
Unit of Measure: ng/mL
C0, Day 7
57.47
(83%)
Cτ, Day 7
54.27
(75%)
Cmin, Day 7
46.37
(83%)
Cmax, Day 7
212.93
(41%)
28.Primary Outcome
Title GSK2248761 PK Parameters Following Dose Administration on Day 1: Time to Maximum Observed Concentration (Tmax), Terminal Half-life (t1/2), Absorption Lag Time (Tlag)
Hide Description Tmax is defined as the, time of maximum measured GSK2248761 concentration in the plasma, on Day 1. The t1/2 was defined as the time measured for plasma concentration to decrease by one half. The tlag was defined as the time taken for the drug GSK2248761, to appear in the systemic circulation following administration. Serial blood samples were collected on Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours postdose on Day 1 and used for analysis.
Time Frame Day 1 (Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours postdose)
Hide Outcome Measure Data
Hide Analysis Population Description
PK population.
Arm/Group Title GSK2248761 30 mg
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Overall Number of Participants Analyzed 6
Median (Full Range)
Unit of Measure: hour
tmax
4.00
(3.0 to 6.0)
t1/2
7.99
(6.3 to 9.8)
tlag
0.49
(0.0 to 1.0)
29.Primary Outcome
Title GSK2248761 PK Parameters Following Dose Administration on Day 1: Apparent Clearance (CL/F)
Hide Description The Clearance factor was defined as the volume of plasma cleared of the drug GSK2248761, per unit time. Serial blood samples were collected on Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours postdose on Day 1 and used for analysis.
Time Frame Day 1 (Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours post-dose)
Hide Outcome Measure Data
Hide Analysis Population Description
PK population.
Arm/Group Title GSK2248761 30 mg
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Overall Number of Participants Analyzed 6
Geometric Mean (Geometric Coefficient of Variation)
Unit of Measure: liter per hour
13.53
(45%)
30.Primary Outcome
Title GSK2248761 PK Parameters Following Dose Administration on Day 7: AUC(0-τ)
Hide Description AUC(0-τ) is the AUC to the end of dosing period. For Day 7, it is the AUC measured at the end of the dosing period at Day 7. Serial blood samples were collected on Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours postdose on Day 7 and used for analysis.
Time Frame Day 7 (Pre-dose, 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours postdose)
Hide Outcome Measure Data
Hide Analysis Population Description
PK population.
Arm/Group Title GSK2248761 30 mg
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days.
Overall Number of Participants Analyzed 6
Geometric Mean (Geometric Coefficient of Variation)
Unit of Measure: hour*ng/mL
9679.71
(54%)
31.Primary Outcome
Title GSK2248761 PK Parameters Following Dose Administration on Day 7: Tmax
Hide Description Tmax is defined as the, time of maximum measured GSK2248761 concentration in the plasma, on Day 7. Serial blood samples were collected on Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours postdose on Day 7 and used for analysis
Time Frame Day 7 (Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours post dose)
Hide Outcome Measure Data
Hide Analysis Population Description
PK population.
Arm/Group Title GSK2248761 30 mg
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Overall Number of Participants Analyzed 6
Median (Full Range)
Unit of Measure: hours
4.01
(3.0 to 6.0)
32.Primary Outcome
Title GSK2248761 PK Parameters Following Dose Administration on Day 7: t1/2
Hide Description The t1/2 was defined as the time measured for plasma concentration to decrease by one half. Serial blood samples were collected on Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours postdose on Day 7 and used for analysis
Time Frame Day 7 (Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours post dose)
Hide Outcome Measure Data
Hide Analysis Population Description
PK population
Arm/Group Title GSK2248761 30 mg
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Overall Number of Participants Analyzed 6
Geometric Mean (Geometric Coefficient of Variation)
Unit of Measure: hour
9.69
(25%)
33.Primary Outcome
Title Change From Baseline in CD4+ and CD8+ T-lymphocyte Cell Count at Day1 and Day 8.
Hide Description Whole venous blood samples were obtained from each participant for the analysis of lymphocyte subsets by flow cytometry (total lymphocyte counts, percentage, CD4+ cell counts, and CD8+ cell counts) at Screening, Day 1 and Day 8. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values (Day 1 and Day 8). Baseline was defined as Screening.
Time Frame Baseline (Screening), Day 1 and Day 8
Hide Outcome Measure Data
Hide Analysis Population Description
ITT population.
Arm/Group Title GSK2248761 30 mg Placebo
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Eligible participants matching placebo capsules to GSK2248761 10 mg capsules orally once daily dosed with 360 mL water after a standard breakfast upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Overall Number of Participants Analyzed 6 2
Mean (Standard Deviation)
Unit of Measure: per cubic millimeter
CD4+ cells, Day 1 1.2  (76.32) 76.0  (5.66)
CD4+ cells, Day 8 87.5  (58.49) 102.0  (107.48)
CD8+ cells, Day 1 123.5  (348.90) 526.0  (169.71)
CD8+ cells, Day 8 313.3  (218.85) 531.5  (539.52)
34.Secondary Outcome
Title Percent Change From Baseline in CD4+ and CD8+ T-lymphocyte Cell Count at Day 1 and Day 8
Hide Description Data for CD4+ and CD8+ cells was collected at Screening, Day 1 and Day 8. The percent change from baseline was reported at Day 1 and Day 8. Baseline was defined as Screening. The percent change from baseline was calculated as post-randomization value minus the baseline value.
Time Frame Baseline (Screening), Day 1 and Day 8
Hide Outcome Measure Data
Hide Analysis Population Description
ITT population.
Arm/Group Title GSK2248761 30 mg Placebo
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Eligible participants matching placebo capsules to GSK2248761 10 mg capsules orally once daily dosed with 360 mL water after a standard breakfast upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Overall Number of Participants Analyzed 6 2
Mean (Standard Deviation)
Unit of Measure: Percent change
CD4+, Day 1 -3.2  (1.78) -2.9  (1.27)
CD4+, Day 8 -2.4  (1.49) -1.7  (0.42)
CD8+, Day 1 -2.8  (7.31) 2.8  (3.82)
CD8+, Day 8 -0.4  (2.56) 0.4  (1.41)
35.Secondary Outcome
Title Accumulation Ratio for AUC , Cmax, Cτ, and Time Invariance Ratio Following Repeat Administration
Hide Description The accumulation ratio is based on the parameters, Cmax, AUC(0-tau), AUC(0-24), C(tau), C24, AND AUC(0-inf). The accumulation ratio Ro was the ratio of AUC(0-tau) on Day 7 to that of AUC(0-24) on Day 1; the accumulation ratio R (Cmax) was the ratio of Cmax on Day 7 to that of Cmax on Day 1; the accumulation ratio R(Ctau) was the ratio of Ctau on Day 7 to the ratio of C24 on Day 1 and the Time Invariance Ratio Rs was defined as the ratio of AUC(0-tau) on Day 7 to that of AUC(0-inf) on Day 1. The ratio has been reported as number.
Time Frame (Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours post-dose ) on Day 1 and Day 7
Hide Outcome Measure Data
Hide Analysis Population Description
PK population.
Arm/Group Title GSK2248761 30 mg
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days.
Overall Number of Participants Analyzed 6
Measure Type: Number
Number (90% Confidence Interval)
Unit of Measure: ratio
Accumulation Ratio Ro
1.576
(1.321 to 1.880)
Accumulation Ratio R [Cmax]
1.212
(1.009 to 1.456)
Accumulation Ratio R[Ctau]
1.750
(1.170 to 2.617)
Time Invariance Ratio Rs
1.309
(1.094 to 1.567)
36.Secondary Outcome
Title Change From Baseline in Reverse Transcriptase Sequences of HIV-1 at Day 8
Hide Description None of the participants had non-nucleoside reverse transcriptase inhibitor (NNRTI) resistance mutations at codons 90, 98, 100, 101, 103, 106, 108, 138, 179, 181, 188, 190, 225, or 230 at either Day 1 or Day 8. No mutation selected by GSK2248761 in vitro was observed for any participant at either Day 1 or Day 8. This data for "Change from baseline in reverse transcriptase sequences of HIV-1 at Day 8" not collected.
Time Frame Baseline (Screening) and Day 8
Hide Outcome Measure Data
Hide Analysis Population Description
ITT population. Data not collected for "Change from baseline reverse transcriptase sequence"
Arm/Group Title GSK2248761 30 mg Placebo
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Eligible participants matching placebo capsules to GSK2248761 10 mg capsules orally once daily dosed with 360 mL water after a standard breakfast upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Overall Number of Participants Analyzed 0 0
No data displayed because Outcome Measure has zero total analyzed.
37.Secondary Outcome
Title Assessment of the Achievement of Pre-dose GSK2248761 Steady State Concentration Following Repeat Dose Administration on Day 2 Through 7
Hide Description The pre-dose GSK2248761 steady state concentration, following repeated dose administration from Day 2 through Day 7 was assessed. Serial dose sampling was done on each day of Day 2, 3, 4, 5 and Day 6 and for Day 7 (Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours postdose), before the administration of the study drug daily.
Time Frame Day 7 (Pre - dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours post-dose) and Days 2, 3, 4. 5 and 6: pre-dose only
Hide Outcome Measure Data
Hide Analysis Population Description
PK population.
Arm/Group Title GSK2248761 30 mg
Hide Arm/Group Description:
Eligible participants received 3 capsules of GSK2248761 10 mg orally once daily dosed with 360 mL water after a standard breakfast, upto 7-days. Participants were to have fasted 4 hours after dosing. Unless otherwise instructed participants were not to recline (remained upright) for the first 4 hours following oral administration. On Day 8 participants received either Kaletra or HAART for 28 days
Overall Number of Participants Analyzed 6
Mean (90% Confidence Interval)
Unit of Measure: ng/mL
Days 4, 5, 6 and 7
0.052
(0.012 to 0.093)
Days 5, 6 and 7
-0.019
(-0.075 to 0.037)
Days 6 and 7
-0.056
(-0.230 to 0.118)
38.Secondary Outcome
Title PK Data of Day 1 AUC(0-inf) and Day 7 AUC(0-tau) at Different Doses for the Assessment of Dose Proportionality
Hide Description Data for IDX899 100 mg, IDX899 200 mg, IDX899 400 mg and IDX899 800 mg for Day 1 and Day 2 were taken from the Idenix NV-05A-002 study which were combined with GSK2248761 30 mg once daily data from this study, to assess the dose proportionality. The dose proportionality occurred when increase in the administered doses were accompanied by proportional increases in measure of exposure of the drug in the plasma PK parameters like AUC, Cmax, Ctau and other factors. The dose proportionality effects of IDX899 100 mg, IDX899 200 mg, IDX899 400 mg and IDX899 800 mg, following repeat dose administration on Day 7 for the PK parameter AUC(0-tau) has been reported.
Time Frame (Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours post-dose ) From Day 1 to Up to Day 7
Hide Outcome Measure Data
Hide Analysis Population Description
PK population.
Arm/Group Title GSK2248761 30 mg IDX899 100 mg IDX899 200 mg IDX899 400 mg IDX899 800 mg
Hide Arm/Group Description:
The eligible participants in this arm received GSK2248761 as 30 mg once daily for up to 7-days daily. On Day 8 participants received either Kaletra or HAART for 28 days.
The eligible participants in this arm received IDX899 100 mg, once daily orally for upto 7-days daily. The dose was accompanied with 360 mL of water. On Day 8 participants received either Kaletra or HAART for 28 days. Data was taken from the Idenix NV-05A-002 study.
The eligible participants in this arm received IDX899 200 mg, once daily orally for upto 7-days daily. The dose was accompanied with 360 mL of water . On Day 8 participants received either Kaletra or HAART for 28 days. Data was taken from the Idenix NV-05A-002 study.
The eligible participants in this arm received IDX899 400 mg, once daily orally for upto 7-days daily. The dose was accompanied with 360 mL of water. On Day 8 participants received either Kaletra or HAART for 28 days. Data was taken from the Idenix NV-05A-002 study.
The eligible participants in this arm received IDX899 800 mg, once daily orally for upto 7-days daily. The dose was accompanied with 360 mL of water. On Day 8 participants received either Kaletra or HAART for 28 days. Data was taken from the Idenix NV-05A-002 study.
Overall Number of Participants Analyzed 6 8 8 8 8
Geometric Mean (Geometric Coefficient of Variation)
Unit of Measure: hour*ng/mL
AUC(0-inf), Day 1
2217.73
(45%)
9908
(21.07%)
23817
(46.77%)
33820
(58.30%)
37812
(81.37%)
AUC(0-tau), Day 7
2903.91
(54%)
11650
(31.02%)
27209
(47.46%)
49649
(26.55%)
53683
(72.34%)
39.Secondary Outcome
Title PK Data of Cmax and Ctau at Different Doses for the Assessment of Dose Proportionality
Hide Description Data for IDX899 100 mg, IDX899 200 mg, IDX899 400 mg and IDX899 800 mg for Day 1 and Day 2 were taken from the Idenix NV-05A-002 study which were combined with GSK2248761 30 mg once daily data from this study, to assess the dose proportionality. The dose proportionality occurred when increase in the administered doses were accompanied by proportional increases in measure of exposure of the drug in the plasma PK parameters like AUC, Cmax, Ctau and other factors. Data for Ctau on Day 1 is presented for concentration at 24 hours post-dose on Day 1.
Time Frame (Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours post-dose ) From Day 1 to Up to Day 7
Hide Outcome Measure Data
Hide Analysis Population Description
PK population.
Arm/Group Title GSK2248761 30 mg IDX899 100 mg IDX899 200 mg IDX899 400 mg IDX899 800 mg
Hide Arm/Group Description:
The eligible participants in this arm received GSK2248761 as 30 mg once daily for up to 7-days daily. On Day 8 participants received either Kaletra or HAART for 28 days.
The eligible participants in this arm received IDX899 100 mg, once daily orally for upto 7-days daily. The dose was accompanied with 360 mL of water. On Day 8 participants received either Kaletra or HAART for 28 days. Data was taken from the Idenix NV-05A-002 study.
The eligible participants in this arm received IDX899 200 mg, once daily orally for upto 7-days daily. The dose was accompanied with 360 mL of water . On Day 8 participants received either Kaletra or HAART for 28 days. Data was taken from the Idenix NV-05A-002 study.
The eligible participants in this arm received IDX899 400 mg, once daily orally for upto 7-days daily. The dose was accompanied with 360 mL of water. On Day 8 participants received either Kaletra or HAART for 28 days. Data was taken from the Idenix NV-05A-002 study.
The eligible participants in this arm received IDX899 800 mg, once daily orally for upto 7-days daily. The dose was accompanied with 360 mL of water. On Day 8 participants received either Kaletra or HAART for 28 days. Data was taken from the Idenix NV-05A-002 study.
Overall Number of Participants Analyzed 6 8 8 8 8
Geometric Mean (Geometric Coefficient of Variation)
Unit of Measure: ng/mL
Cmax, Day 1
175.63
(39%)
797.8
(32.19%)
1686.2
(24.67%)
2625.9
(34.20%)
3406.4
(31.31%)
Cmax, Day 7
212.93
(41%)
960.1
(22.62%)
2158.9
(35.96%)
4140.7
(21.54%)
5394.5
(46.36%)
Ctau, Day 1
31.02
(61%)
128.9
(37.36%)
325.6
(60.93%)
422.9
(81.23%)
364.5
(123.77%)
Ctau, Day 7
54.27
(75%)
204.7
(48.36%)
469.2
(63.17%)
864.5
(47.44%)
540.3
(124.71%)
Time Frame Up to 38 Days
Adverse Event Reporting Description Safety population
 
Arm/Group Title GSK2248761 30 mg Placebo
Hide Arm/Group Description The eligible participants in this arm received GSK2248761 as 30 mg once daily for up to 7-days daily . On Day 8 participants received either Kaletra or HAART for 28 days. The eligible participants in this arm received matching placebo once daily for 7-days. On Day 8 participants received either Kaletra or HAART for 28 days
All-Cause Mortality
GSK2248761 30 mg Placebo
Affected / at Risk (%) Affected / at Risk (%)
Total   0/6 (0.00%)   0/2 (0.00%) 
Show Serious Adverse Events Hide Serious Adverse Events
GSK2248761 30 mg Placebo
Affected / at Risk (%) Affected / at Risk (%)
Total   0/6 (0.00%)   0/2 (0.00%) 
Show Other (Not Including Serious) Adverse Events Hide Other (Not Including Serious) Adverse Events
Frequency Threshold for Reporting Other Adverse Events 0%
GSK2248761 30 mg Placebo
Affected / at Risk (%) Affected / at Risk (%)
Total   4/6 (66.67%)   1/2 (50.00%) 
Gastrointestinal disorders     
Diarrhoea  1  2/6 (33.33%)  0/2 (0.00%) 
Nausea  1  0/6 (0.00%)  1/2 (50.00%) 
General disorders     
Pyrexia  1  0/6 (0.00%)  1/2 (50.00%) 
Infections and infestations     
Nasopharyngitis  1  1/6 (16.67%)  1/2 (50.00%) 
Nervous system disorders     
Dizziness  1  1/6 (16.67%)  0/2 (0.00%) 
Headache  1  0/6 (0.00%)  1/2 (50.00%) 
Psychiatric disorders     
Anxiety  1  1/6 (16.67%)  0/2 (0.00%) 
Vascular disorders     
Hypertension  1  1/6 (16.67%)  0/2 (0.00%) 
1
Term from vocabulary, MedDRA 12.1
Indicates events were collected by systematic assessment
Certain Agreements
Principal Investigators are NOT employed by the organization sponsoring the study.
There IS an agreement between Principal Investigators and the Sponsor (or its agents) that restricts the PI's rights to discuss or publish trial results after the trial is completed.
GSK agreements may vary with individual investigators, but will not prohibit any investigator from publishing. GSK supports the publication of results from all centers of a multi-center trial but requests that reports based on single-site data not precede the primary publication of the entire clinical trial.
Results Point of Contact
Layout table for Results Point of Contact information
Name/Title: GSK Response Center
Organization: ViiV Healthcare
Phone: 866-435-7343
Layout table for additonal information
Responsible Party: ViiV Healthcare
ClinicalTrials.gov Identifier: NCT00945282     History of Changes
Other Study ID Numbers: 113020
First Submitted: July 23, 2009
First Posted: July 24, 2009
Results First Submitted: August 22, 2017
Results First Posted: November 29, 2018
Last Update Posted: November 29, 2018