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Bioavailability of Doravirine (MK-1439) Experimental Nano Formulations in Healthy Adults (MK-1439-046)

The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Read our disclaimer for details.
 
ClinicalTrials.gov Identifier: NCT02549040
Recruitment Status : Completed
First Posted : September 14, 2015
Results First Posted : February 22, 2019
Last Update Posted : January 7, 2021
Sponsor:
Information provided by (Responsible Party):
Merck Sharp & Dohme Corp.

Study Type Interventional
Study Design Allocation: N/A;   Intervention Model: Single Group Assignment;   Masking: None (Open Label);   Primary Purpose: Treatment
Condition Human Immunodeficiency Virus-1 (HIV-1)
Interventions Drug: Treatment A: Doravirine 100 mg film coated tablet
Drug: Treatment B: Doravirine 150 mg tablet (40% drug loaded granule)
Drug: Treatment C: Doravirine 150 mg tablet (30% drug loaded granule)
Drug: Treatment D: Doravirine 150 mg tablet (50% drug loaded granule)
Drug: Treatment E: Doravirine 100 mg tablet (30% drug loaded granule)
Enrollment 16
Recruitment Details  
Pre-assignment Details  
Arm/Group Title MK-1439 Fixed Sequence Treatment
Hide Arm/Group Description After a minimum 10 hour overnight fast, participants received a single oral dose during each of 5 periods. During Period 1, participants received Treatment B: MK-1439 Type 1 dose (150 mg tablet [40% drug loaded granule]). During Period 2, participants received Treatment A: MK-1439 100 mg film coated tablet. During Period 3, participants received Treatment C: MK-1439 Type 2 dose (150 mg tablet [30% drug loaded granule]). During Period 4, participants received Treatment D: MK-1439 Type 3 dose (150 mg tablet [50% drug loaded granule]. During Period 5, participants received Treatment E: MK-1439 Type 4 dose (100 mg tablet [30% drug loaded granule]). Each period was separated by a 14 day washout.
Period Title: Period 1
Started 16
Completed 16
Not Completed 0
Period Title: Period 2
Started 16
Completed 16
Not Completed 0
Period Title: Period 3
Started 16
Completed 16
Not Completed 0
Period Title: Period 4
Started 16
Completed 16
Not Completed 0
Period Title: Period 5
Started 16
Completed 16
Not Completed 0
Arm/Group Title MK-1439 Fixed Sequence Treatment
Hide Arm/Group Description After a minimum 10 hour overnight fast, participants received a single oral dose during each of 5 periods. During Period 1, participants received Treatment B: MK-1439 Type 1 dose (150 mg tablet [40% drug loaded granule]). During Period 2, participants received Treatment A: MK-1439 100 mg film coated tablet. During Period 3, participants received Treatment C: MK-1439 Type 2 dose (150 mg tablet [30% drug loaded granule]). During Period 4, participants received Treatment D: MK-1439 Type 3 dose (150 mg tablet [50% drug loaded granule]. During Period 5, participants received Treatment E: MK-1439 Type 4 dose (100 mg tablet [30% drug loaded granule]). Each period was separated by a 14 day washout.
Overall Number of Baseline Participants 16
Hide Baseline Analysis Population Description
[Not Specified]
Age, Continuous  
Mean (Standard Deviation)
Unit of measure:  Years
Number Analyzed 16 participants
41.8  (9.48)
Sex: Female, Male  
Measure Type: Count of Participants
Unit of measure:  Participants
Number Analyzed 16 participants
Female
6
  37.5%
Male
10
  62.5%
1.Primary Outcome
Title Area Under the Plasma Concentration-time Curve From Time 0 to Infinity (AUC0-inf) of MK-1439 Following a Single Administration of MK-1439
Hide Description During each of the 5 treatment periods, blood samples were collected pre-dose and at 0.5, 1, 1.5, 2, 3, 4, 6, 12, 24, 48, and 72 hours post-dose to determine AUC0-inf after a single administration of MK-1439.
Time Frame Periods 1 to 5 at the following time points: pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 12, 24, 48, and 72 hours post-dose
Hide Outcome Measure Data
Hide Analysis Population Description
Participants who complied with the protocol sufficiently to ensure that the data exhibited the effects of treatment, according to the underlying scientific model. Participants were excluded from descriptive statistics for AUC0-inf if there were insufficient data in the terminal phase to characterize half-life (t1/2).
Arm/Group Title Treatment B: MK-1439 150 mg Tablet (40% Drug Loaded Granule) Treatment A: MK-1439 100 mg Film Coated Tablet Treatment C: MK-1439 150 mg Tablet (30% Drug Loaded Granule) Treatment D: MK-1439 150 mg Tablet (50% Drug Loaded Granule) Treatment E: MK-1439 100 mg Tablet (30% Drug Loaded Granule)
Hide Arm/Group Description:
Participants received a single MK-1439 Type 1 dose (150 mg tablet [40% drug loaded granule]) administered orally at the start of Period 1
Participants received a single MK-1439 100 mg film coated tablet administered orally at the start of Period 2
Participants received a single MK-1439 Type 2 dose (150 mg tablet [30% drug loaded granule]) administered orally at the start of Period 3
Participants received a single MK-1439 Type 3 dose (150 mg tablet [50% drug loaded granule]) administered orally at the start of Period 4
Participants received a single MK-1439 Type 4 dose (100 mg tablet [30% drug loaded granule]) administered orally at the start of Period 5
Overall Number of Participants Analyzed 13 16 15 12 15
Geometric Mean (Geometric Coefficient of Variation)
Unit of Measure: µM*h
28.6
(34.6%)
31.9
(33.9%)
35.5
(29.6%)
29.1
(30.3%)
28.0
(27.5%)
Hide Statistical Analysis 1
Statistical Analysis Overview Comparison Group Selection Treatment B: MK-1439 150 mg Tablet (40% Drug Loaded Granule), Treatment A: MK-1439 100 mg Film Coated Tablet
Comments Comparison of Treatment B: MK-1439 150 mg tablet (40% drug loaded granule) vs. Treatment A: MK-1439 100 mg film coated tablet
Type of Statistical Test Other
Comments [Not Specified]
Method of Estimation Estimation Parameter Geometric mean ratio
Estimated Value 0.96
Confidence Interval (2-Sided) 90%
0.85 to 1.09
Estimation Comments [Not Specified]
Hide Statistical Analysis 2
Statistical Analysis Overview Comparison Group Selection Treatment A: MK-1439 100 mg Film Coated Tablet, Treatment C: MK-1439 150 mg Tablet (30% Drug Loaded Granule)
Comments Comparison of Treatment C: MK-1439 150 mg tablet (30% drug loaded granule) vs. Treatment A: MK-1439 100 mg film coated tablet
Type of Statistical Test Other
Comments [Not Specified]
Method of Estimation Estimation Parameter Geometric mean ratio
Estimated Value 1.13
Confidence Interval (2-Sided) 90%
1.02 to 1.26
Estimation Comments [Not Specified]
Hide Statistical Analysis 3
Statistical Analysis Overview Comparison Group Selection Treatment A: MK-1439 100 mg Film Coated Tablet, Treatment D: MK-1439 150 mg Tablet (50% Drug Loaded Granule)
Comments Comparison of Treatment D: MK-1439 150 mg tablet (50% drug loaded granule) vs. Treatment A: MK-1439 100 mg film coated tablet
Type of Statistical Test Other
Comments [Not Specified]
Method of Estimation Estimation Parameter Geometric mean ratio
Estimated Value 0.99
Confidence Interval (2-Sided) 90%
0.88 to 1.11
Estimation Comments [Not Specified]
Hide Statistical Analysis 4
Statistical Analysis Overview Comparison Group Selection Treatment A: MK-1439 100 mg Film Coated Tablet, Treatment E: MK-1439 100 mg Tablet (30% Drug Loaded Granule)
Comments Comparison of Treatment E: MK-1439 100 mg tablet (30% drug loaded granule) vs. Treatment A: MK-1439 100 mg film coated tablet
Type of Statistical Test Other
Comments [Not Specified]
Method of Estimation Estimation Parameter Geometric mean ratio
Estimated Value 0.89
Confidence Interval (2-Sided) 90%
0.80 to 0.99
Estimation Comments [Not Specified]
2.Primary Outcome
Title Area Under the Plasma Concentration-time Curve From Time 0 to Last Time (AUC0-last) With Quantifiable MK-1439 Following a Single Administration of MK-1439
Hide Description During each of the 5 treatment periods, blood samples were collected pre-dose and at 0.5, 1, 1.5, 2, 3, 4, 6, 12, 24, 48, and 72 hours post-dose to determine AUC0-last after a single administration of MK-1439.
Time Frame Periods 1 to 5 at the following time points: pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 12, 24, 48, and 72 hours post-dose
Hide Outcome Measure Data
Hide Analysis Population Description
Participants who complied with the protocol sufficiently to ensure that the data exhibited the effects of treatment, according to the underlying scientific model.
Arm/Group Title Treatment B: MK-1439 150 mg Tablet (40% Drug Loaded Granule) Treatment A: MK-1439 100 mg Film Coated Tablet Treatment C: MK-1439 150 mg Tablet (30% Drug Loaded Granule) Treatment D: MK-1439 150 mg Tablet (50% Drug Loaded Granule) Treatment E: MK-1439 100 mg Tablet (30% Drug Loaded Granule)
Hide Arm/Group Description:
Participants received a single MK-1439 Type 1 dose (150 mg tablet [40% drug loaded granule]) administered orally at the start of Period 1
Participants received a single MK-1439 100 mg film coated tablet administered orally at the start of Period 2
Participants received a single MK-1439 Type 2 dose (150 mg tablet [30% drug loaded granule]) administered orally at the start of Period 3
Participants received a single MK-1439 Type 3 dose (150 mg tablet [50% drug loaded granule]) administered orally at the start of Period 4
Participants received a single MK-1439 Type 4 dose (100 mg tablet [30% drug loaded granule]) administered orally at the start of Period 5
Overall Number of Participants Analyzed 16 16 16 16 16
Geometric Mean (Geometric Coefficient of Variation)
Unit of Measure: μM*h
26.3
(29.3%)
29.9
(31.1%)
32.7
(26.3%)
27.0
(28.4%)
26.3
(27.0%)
Hide Statistical Analysis 1
Statistical Analysis Overview Comparison Group Selection Treatment B: MK-1439 150 mg Tablet (40% Drug Loaded Granule), Treatment A: MK-1439 100 mg Film Coated Tablet
Comments Comparison of Treatment B: MK-1439 150 mg tablet (40% drug loaded granule) vs. Treatment A: MK-1439 100 mg film coated tablet
Type of Statistical Test Other
Comments [Not Specified]
Method of Estimation Estimation Parameter Geometric mean ratio
Estimated Value 0.88
Confidence Interval (2-Sided) 90%
0.79 to 0.98
Estimation Comments [Not Specified]
Hide Statistical Analysis 2
Statistical Analysis Overview Comparison Group Selection Treatment A: MK-1439 100 mg Film Coated Tablet, Treatment C: MK-1439 150 mg Tablet (30% Drug Loaded Granule)
Comments Comparison of Treatment C: MK-1439 150 mg tablet (30% drug loaded granule) vs. Treatment A: MK-1439 100 mg film coated tablet
Type of Statistical Test Other
Comments [Not Specified]
Method of Estimation Estimation Parameter Geometric mean ratio
Estimated Value 1.09
Confidence Interval (2-Sided) 90%
0.98 to 1.21
Estimation Comments [Not Specified]
Hide Statistical Analysis 3
Statistical Analysis Overview Comparison Group Selection Treatment A: MK-1439 100 mg Film Coated Tablet, Treatment D: MK-1439 150 mg Tablet (50% Drug Loaded Granule)
Comments Comparison of Treatment D: MK-1439 150 mg tablet (50% drug loaded granule) vs. Treatment A: MK-1439 100 mg film coated tablet
Type of Statistical Test Other
Comments [Not Specified]
Method of Estimation Estimation Parameter Geometric mean ratio
Estimated Value 0.90
Confidence Interval (2-Sided) 90%
0.81 to 1.00
Estimation Comments [Not Specified]
Hide Statistical Analysis 4
Statistical Analysis Overview Comparison Group Selection Treatment A: MK-1439 100 mg Film Coated Tablet, Treatment E: MK-1439 100 mg Tablet (30% Drug Loaded Granule)
Comments Comparison of Treatment E: MK-1439 100 mg tablet (30% drug loaded granule) vs. Treatment A: MK-1439 100 mg film coated tablet
Type of Statistical Test Other
Comments [Not Specified]
Method of Estimation Estimation Parameter Geometric mean ratio
Estimated Value 0.88
Confidence Interval (2-Sided) 90%
0.79 to 0.97
Estimation Comments [Not Specified]
3.Primary Outcome
Title Maximum Plasma Concentration (Cmax) of MK-1439 Following a Single Administration of MK-1439
Hide Description During each of the 5 treatment periods, blood samples were collected pre-dose and at 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, and 72 hours post-dose to determine Cmax after a single administration of MK-1439.
Time Frame Periods 1 to 5 at the following time points: pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 12, 24, 48, and 72 hours post-dose
Hide Outcome Measure Data
Hide Analysis Population Description
Participants who complied with the protocol sufficiently to ensure that the data exhibited the effects of treatment, according to the underlying scientific model.
Arm/Group Title Treatment B: MK-1439 150 mg Tablet (40% Drug Loaded Granule) Treatment A: MK-1439 100 mg Film Coated Tablet Treatment C: MK-1439 150 mg Tablet (30% Drug Loaded Granule) Treatment D: MK-1439 150 mg Tablet (50% Drug Loaded Granule) Treatment E: MK-1439 100 mg Tablet (30% Drug Loaded Granule)
Hide Arm/Group Description:
Participants received a single MK-1439 Type 1 dose (150 mg tablet [40% drug loaded granule]) administered orally at the start of Period 1
Participants received a single MK-1439 100 mg film coated tablet administered orally at the start of Period 2
Participants received a single MK-1439 Type 2 dose (150 mg tablet [30% drug loaded granule]) administered orally at the start of Period 3
Participants received a single MK-1439 Type 3 dose (150 mg tablet [50% drug loaded granule]) administered orally at the start of Period 4
Participants received a single MK-1439 Type 4 dose (100 mg tablet [30% drug loaded granule]) administered orally at the start of Period 5
Overall Number of Participants Analyzed 16 16 16 16 16
Geometric Mean (Geometric Coefficient of Variation)
Unit of Measure: nM
1070
(26.5%)
1520
(32.5%)
1320
(27.8%)
1060
(27.0%)
1160
(24.2%)
Hide Statistical Analysis 1
Statistical Analysis Overview Comparison Group Selection Treatment B: MK-1439 150 mg Tablet (40% Drug Loaded Granule), Treatment A: MK-1439 100 mg Film Coated Tablet
Comments Comparison of Treatment B: MK-1439 150 mg tablet (40% drug loaded granule) vs. Treatment A: MK-1439 100 mg film coated tablet
Type of Statistical Test Other
Comments [Not Specified]
Method of Estimation Estimation Parameter Geometric mean ratio
Estimated Value 0.70
Confidence Interval (2-Sided) 90%
0.61 to 0.82
Estimation Comments [Not Specified]
Hide Statistical Analysis 2
Statistical Analysis Overview Comparison Group Selection Treatment A: MK-1439 100 mg Film Coated Tablet, Treatment C: MK-1439 150 mg Tablet (30% Drug Loaded Granule)
Comments Comparison of Treatment C: MK-1439 150 mg tablet (30% drug loaded granule) vs. Treatment A: MK-1439 100 mg film coated tablet
Type of Statistical Test Other
Comments [Not Specified]
Method of Estimation Estimation Parameter Geometric mean ratio
Estimated Value 0.87
Confidence Interval (2-Sided) 90%
0.75 to 1.01
Estimation Comments [Not Specified]
Hide Statistical Analysis 3
Statistical Analysis Overview Comparison Group Selection Treatment A: MK-1439 100 mg Film Coated Tablet, Treatment D: MK-1439 150 mg Tablet (50% Drug Loaded Granule)
Comments Comparison of Treatment D: MK-1439 150 mg tablet (50% drug loaded granule) vs. Treatment A: MK-1439 100 mg film coated tablet
Type of Statistical Test Other
Comments [Not Specified]
Method of Estimation Estimation Parameter Geometric mean ratio
Estimated Value 0.70
Confidence Interval (2-Sided) 90%
0.60 to 0.81
Estimation Comments [Not Specified]
Hide Statistical Analysis 4
Statistical Analysis Overview Comparison Group Selection Treatment A: MK-1439 100 mg Film Coated Tablet, Treatment E: MK-1439 100 mg Tablet (30% Drug Loaded Granule)
Comments Comparison of Treatment E: MK-1439 100 mg tablet (30% drug loaded granule) vs. Treatment A: MK-1439 100 mg film coated tablet
Type of Statistical Test Other
Comments [Not Specified]
Method of Estimation Estimation Parameter Geometric mean ratio
Estimated Value 0.76
Confidence Interval (2-Sided) 90%
0.66 to 0.86
Estimation Comments [Not Specified]
4.Primary Outcome
Title Plasma Concentration of MK-1439 at 24 Hours Post-dose (C24hr) Following a Single Administration of MK-1439
Hide Description During each of the 5 treatment periods, blood samples were collected 24 hours after dosing to determine C24hr after a single administration of MK-1439.
Time Frame Periods 1 to 5: 24 hours post-dose
Hide Outcome Measure Data
Hide Analysis Population Description
Participants who complied with the protocol sufficiently to ensure that the data exhibited the effects of treatment, according to the underlying scientific model.
Arm/Group Title Treatment B: MK-1439 150 mg Tablet (40% Drug Loaded Granule) Treatment A: MK-1439 100 mg Film Coated Tablet Treatment C: MK-1439 150 mg Tablet (30% Drug Loaded Granule) Treatment D: MK-1439 150 mg Tablet (50% Drug Loaded Granule) Treatment E: MK-1439 100 mg Tablet (30% Drug Loaded Granule)
Hide Arm/Group Description:
Participants received a single MK-1439 Type 1 dose (150 mg tablet [40% drug loaded granule]) administered orally at the start of Period 1
Participants received a single MK-1439 100 mg film coated tablet administered orally at the start of Period 2
Participants received a single MK-1439 Type 2 dose (150 mg tablet [30% drug loaded granule]) administered orally at the start of Period 3
Participants received a single MK-1439 Type 3 dose (150 mg tablet [50% drug loaded granule]) administered orally at the start of Period 4
Participants received a single MK-1439 Type 4 dose (100 mg tablet [30% drug loaded granule]) administered orally at the start of Period 5
Overall Number of Participants Analyzed 16 16 16 16 16
Geometric Mean (Geometric Coefficient of Variation)
Unit of Measure: nM
395
(31.9%)
483
(33.3%)
508
(23.2%)
412
(28.0%)
402
(32.0%)
Hide Statistical Analysis 1
Statistical Analysis Overview Comparison Group Selection Treatment B: MK-1439 150 mg Tablet (40% Drug Loaded Granule), Treatment A: MK-1439 100 mg Film Coated Tablet
Comments Comparison of Treatment B: MK-1439 150 mg tablet (40% drug loaded granule) vs. Treatment A: MK-1439 100 mg film coated tablet
Type of Statistical Test Other
Comments [Not Specified]
Method of Estimation Estimation Parameter Geometric mean ratio
Estimated Value 0.82
Confidence Interval (2-Sided) 90%
0.72 to 0.93
Estimation Comments [Not Specified]
Hide Statistical Analysis 2
Statistical Analysis Overview Comparison Group Selection Treatment A: MK-1439 100 mg Film Coated Tablet, Treatment C: MK-1439 150 mg Tablet (30% Drug Loaded Granule)
Comments Comparison of Treatment C: MK-1439 150 mg tablet (30% drug loaded granule) vs. Treatment A: MK-1439 100 mg film coated tablet
Type of Statistical Test Other
Comments [Not Specified]
Method of Estimation Estimation Parameter Geometric mean ratio
Estimated Value 1.05
Confidence Interval (2-Sided) 90%
0.94 to 1.18
Estimation Comments [Not Specified]
Hide Statistical Analysis 3
Statistical Analysis Overview Comparison Group Selection Treatment A: MK-1439 100 mg Film Coated Tablet, Treatment D: MK-1439 150 mg Tablet (50% Drug Loaded Granule)
Comments Comparison of Treatment D: MK-1439 150 mg tablet (50% drug loaded granule) vs. Treatment A: MK-1439 100 mg film coated tablet
Type of Statistical Test Other
Comments [Not Specified]
Method of Estimation Estimation Parameter Geometric mean ratio
Estimated Value 0.85
Confidence Interval (2-Sided) 90%
0.76 to 0.96
Estimation Comments [Not Specified]
Hide Statistical Analysis 4
Statistical Analysis Overview Comparison Group Selection Treatment A: MK-1439 100 mg Film Coated Tablet, Treatment E: MK-1439 100 mg Tablet (30% Drug Loaded Granule)
Comments Comparison of Treatment E: MK-1439 100 mg tablet (30% drug loaded granule) vs. Treatment A: MK-1439 100 mg film coated tablet
Type of Statistical Test Other
Comments [Not Specified]
Method of Estimation Estimation Parameter Geometric mean ratio
Estimated Value 0.83
Confidence Interval (2-Sided) 90%
0.74 to 0.94
Estimation Comments [Not Specified]
5.Primary Outcome
Title Number of Participants Who Experienced at Least One Adverse Event
Hide Description An adverse event is defined as any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with the use of a study drug, whether or not it is considered related to the study drug.
Time Frame Up to 16 days after last dose of study treatment (up to approximately 92 days)
Hide Outcome Measure Data
Hide Analysis Population Description
All participants who received at least 1 administration of the trial drug.
Arm/Group Title Treatment B: MK-1439 150 mg Tablet (40% Drug Loaded Granule) Treatment A: MK-1439 100 mg Film Coated Tablet Treatment C: MK-1439 150 mg Tablet (30% Drug Loaded Granule) Treatment D: MK-1439 150 mg Tablet (50% Drug Loaded Granule) Treatment E: MK-1439 100 mg Tablet (30% Drug Loaded Granule)
Hide Arm/Group Description:
Participants received a single MK-1439 Type 1 dose (150 mg tablet [40% drug loaded granule]) administered orally at the start of Period 1
Participants received a single MK-1439 100 mg film coated tablet administered orally at the start of Period 2
Participants received a single MK-1439 Type 2 dose (150 mg tablet [30% drug loaded granule]) administered orally at the start of Period 3
Participants received a single MK-1439 Type 3 dose (150 mg tablet [50% drug loaded granule]) administered orally at the start of Period 4
Participants received a single MK-1439 Type 4 dose (100 mg tablet [30% drug loaded granule]) administered orally at the start of Period 5
Overall Number of Participants Analyzed 16 16 16 16 16
Measure Type: Count of Participants
Unit of Measure: Participants
2
  12.5%
5
  31.3%
4
  25.0%
6
  37.5%
1
   6.3%
6.Primary Outcome
Title Number of Participants Who Discontinued Study Treatment Due to an Adverse Event
Hide Description An adverse event is defined as any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with the use of a study drug, whether or not it is considered related to the study drug.
Time Frame Up to 4 days after last dose of study treatment (up to approximately 76 days)
Hide Outcome Measure Data
Hide Analysis Population Description
All participants who received at least 1 administration of the trial drug.
Arm/Group Title Treatment B: MK-1439 150 mg Tablet (40% Drug Loaded Granule) Treatment A: MK-1439 100 mg Film Coated Tablet Treatment C: MK-1439 150 mg Tablet (30% Drug Loaded Granule) Treatment D: MK-1439 150 mg Tablet (50% Drug Loaded Granule) Treatment E: MK-1439 100 mg Tablet (30% Drug Loaded Granule)
Hide Arm/Group Description:
Participants received a single MK-1439 Type 1 dose (150 mg tablet [40% drug loaded granule]) administered orally at the start of Period 1
Participants received a single MK-1439 100 mg film coated tablet administered orally at the start of Period 2
Participants received a single MK-1439 Type 2 dose (150 mg tablet [30% drug loaded granule]) administered orally at the start of Period 3
Participants received a single MK-1439 Type 3 dose (150 mg tablet [50% drug loaded granule]) administered orally at the start of Period 4
Participants received a single MK-1439 Type 4 dose (100 mg tablet [30% drug loaded granule]) administered orally at the start of Period 5
Overall Number of Participants Analyzed 16 16 16 16 16
Measure Type: Count of Participants
Unit of Measure: Participants
0
   0.0%
0
   0.0%
0
   0.0%
0
   0.0%
0
   0.0%
7.Secondary Outcome
Title Area Under the Plasma Concentration-time Curve From Time 0 to 48 Hours (AUC0-48 hr) Post-dose of MK-1439 Following a Single Administration of MK-1439
Hide Description During each of the 5 treatment periods, blood samples were collected pre-dose and at 0.5, 1, 1.5, 2, 3, 4, 6, 12, 24, 48 hours after dosing to determine AUC0-48hr after a single administration of MK-1439.
Time Frame Periods 1 to 5 at the following time points: pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 12, 24, and 48 hours post-dose
Hide Outcome Measure Data
Hide Analysis Population Description
Participants who complied with the protocol sufficiently to ensure that the data exhibited the effects of treatment, according to the underlying scientific model.
Arm/Group Title Treatment B: MK-1439 150 mg Tablet (40% Drug Loaded Granule) Treatment A: MK-1439 100 mg Film Coated Tablet Treatment C: MK-1439 150 mg Tablet (30% Drug Loaded Granule) Treatment D: MK-1439 150 mg Tablet (50% Drug Loaded Granule) Treatment E: MK-1439 100 mg Tablet (30% Drug Loaded Granule)
Hide Arm/Group Description:
Participants received a single MK-1439 Type 1 dose (150 mg tablet [40% drug loaded granule]) administered orally at the start of Period 1
Participants received a single MK-1439 100 mg film coated tablet administered orally at the start of Period 2
Participants received a single MK-1439 Type 2 dose (150 mg tablet [30% drug loaded granule]) administered orally at the start of Period 3
Participants received a single MK-1439 Type 3 dose (150 mg tablet [50% drug loaded granule]) administered orally at the start of Period 4
Participants received a single MK-1439 Type 4 dose (100 mg tablet [30% drug loaded granule]) administered orally at the start of Period 5
Overall Number of Participants Analyzed 16 16 16 16 16
Geometric Mean (Geometric Coefficient of Variation)
Unit of Measure: µM*h
22.8
(27.5%)
27.2
(29.2%)
28.8
(24.8%)
23.2
(27.3%)
23.3
(25.9%)
Hide Statistical Analysis 1
Statistical Analysis Overview Comparison Group Selection Treatment B: MK-1439 150 mg Tablet (40% Drug Loaded Granule), Treatment A: MK-1439 100 mg Film Coated Tablet
Comments Comparison of Treatment B: MK-1439 150 mg tablet (40% drug loaded granule) vs. Treatment A: MK-1439 100 mg film coated tablet
Type of Statistical Test Other
Comments [Not Specified]
Method of Estimation Estimation Parameter Geometric mean ratio
Estimated Value 0.84
Confidence Interval (2-Sided) 90%
0.75 to 0.94
Estimation Comments [Not Specified]
Hide Statistical Analysis 2
Statistical Analysis Overview Comparison Group Selection Treatment A: MK-1439 100 mg Film Coated Tablet, Treatment C: MK-1439 150 mg Tablet (30% Drug Loaded Granule)
Comments Comparison of Treatment C: MK-1439 150 mg tablet (30% drug loaded granule) vs. Treatment A: MK-1439 100 mg film coated tablet
Type of Statistical Test Other
Comments [Not Specified]
Method of Estimation Estimation Parameter Geometric mean ratio
Estimated Value 1.06
Confidence Interval (2-Sided) 90%
0.95 to 1.18
Estimation Comments [Not Specified]
Hide Statistical Analysis 3
Statistical Analysis Overview Comparison Group Selection Treatment A: MK-1439 100 mg Film Coated Tablet, Treatment D: MK-1439 150 mg Tablet (50% Drug Loaded Granule)
Comments Comparison of Treatment D: MK-1439 150 mg tablet (50% drug loaded granule) vs. Treatment A: MK-1439 100 mg film coated tablet
Type of Statistical Test Other
Comments [Not Specified]
Method of Estimation Estimation Parameter Geometric mean ratio
Estimated Value 0.85
Confidence Interval (2-Sided) 90%
0.76 to 0.95
Estimation Comments [Not Specified]
Hide Statistical Analysis 4
Statistical Analysis Overview Comparison Group Selection Treatment A: MK-1439 100 mg Film Coated Tablet, Treatment E: MK-1439 100 mg Tablet (30% Drug Loaded Granule)
Comments Comparison of Treatment E: MK-1439 100 mg tablet (30% drug loaded granule) vs. Treatment A: MK-1439 100 mg film coated tablet
Type of Statistical Test Other
Comments [Not Specified]
Method of Estimation Estimation Parameter Geometric mean ratio
Estimated Value 0.86
Confidence Interval (2-Sided) 90%
0.77 to 0.96
Estimation Comments [Not Specified]
Time Frame Up to 16 days following the last dose of study treatment (up to approximately 92 days)
Adverse Event Reporting Description [Not Specified]
 
Arm/Group Title Treatment B: MK-1439 150 mg Tablet (40% Drug Loaded Granule) Treatment A: MK-1439 100 mg Film Coated Tablet Treatment C: MK-1439 150 mg Tablet (30% Drug Loaded Granule) Treatment D: MK-1439 150 mg Tablet (50% Drug Loaded Granule) Treatment E: MK-1439 100 mg Tablet (30% Drug Loaded Granule)
Hide Arm/Group Description Participants received a single MK-1439 Type 1 dose (150 mg tablet [40% drug loaded granule]) administered orally at the start of Period 1 Participants received a single MK-1439 100 mg film coated tablet administered orally at the start of Period 2 Participants received a single MK-1439 Type 2 dose (150 mg tablet [30% drug loaded granule]) administered orally at the start of Period 3 Participants received a single MK-1439 Type 3 dose (150 mg tablet [50% drug loaded granule]) administered orally at the start of Period 4 Participants received a single MK-1439 Type 4 dose (100 mg tablet [30% drug loaded granule]) administered orally at the start of Period 5
All-Cause Mortality
Treatment B: MK-1439 150 mg Tablet (40% Drug Loaded Granule) Treatment A: MK-1439 100 mg Film Coated Tablet Treatment C: MK-1439 150 mg Tablet (30% Drug Loaded Granule) Treatment D: MK-1439 150 mg Tablet (50% Drug Loaded Granule) Treatment E: MK-1439 100 mg Tablet (30% Drug Loaded Granule)
Affected / at Risk (%) Affected / at Risk (%) Affected / at Risk (%) Affected / at Risk (%) Affected / at Risk (%)
Total   0/16 (0.00%)      0/16 (0.00%)      0/16 (0.00%)      0/16 (0.00%)      0/16 (0.00%)    
Hide Serious Adverse Events
Treatment B: MK-1439 150 mg Tablet (40% Drug Loaded Granule) Treatment A: MK-1439 100 mg Film Coated Tablet Treatment C: MK-1439 150 mg Tablet (30% Drug Loaded Granule) Treatment D: MK-1439 150 mg Tablet (50% Drug Loaded Granule) Treatment E: MK-1439 100 mg Tablet (30% Drug Loaded Granule)
Affected / at Risk (%) # Events Affected / at Risk (%) # Events Affected / at Risk (%) # Events Affected / at Risk (%) # Events Affected / at Risk (%) # Events
Total   0/16 (0.00%)      0/16 (0.00%)      0/16 (0.00%)      0/16 (0.00%)      0/16 (0.00%)    
Hide Other (Not Including Serious) Adverse Events
Frequency Threshold for Reporting Other Adverse Events 5%
Treatment B: MK-1439 150 mg Tablet (40% Drug Loaded Granule) Treatment A: MK-1439 100 mg Film Coated Tablet Treatment C: MK-1439 150 mg Tablet (30% Drug Loaded Granule) Treatment D: MK-1439 150 mg Tablet (50% Drug Loaded Granule) Treatment E: MK-1439 100 mg Tablet (30% Drug Loaded Granule)
Affected / at Risk (%) # Events Affected / at Risk (%) # Events Affected / at Risk (%) # Events Affected / at Risk (%) # Events Affected / at Risk (%) # Events
Total   2/16 (12.50%)      5/16 (31.25%)      4/16 (25.00%)      6/16 (37.50%)      1/16 (6.25%)    
Eye disorders           
Vision blurred  1  0/16 (0.00%)  0 1/16 (6.25%)  1 0/16 (0.00%)  0 0/16 (0.00%)  0 0/16 (0.00%)  0
Gastrointestinal disorders           
Diarrhoea  1  0/16 (0.00%)  0 0/16 (0.00%)  0 1/16 (6.25%)  1 0/16 (0.00%)  0 1/16 (6.25%)  1
Toothache  1  0/16 (0.00%)  0 1/16 (6.25%)  1 0/16 (0.00%)  0 0/16 (0.00%)  0 0/16 (0.00%)  0
General disorders           
Feeling of body temperture change  1  0/16 (0.00%)  0 0/16 (0.00%)  0 0/16 (0.00%)  0 1/16 (6.25%)  1 0/16 (0.00%)  0
Infections and infestations           
Nasopharyngitis  1  0/16 (0.00%)  0 2/16 (12.50%)  2 0/16 (0.00%)  0 0/16 (0.00%)  0 0/16 (0.00%)  0
Injury, poisoning and procedural complications           
Laceration  1  0/16 (0.00%)  0 0/16 (0.00%)  0 2/16 (12.50%)  2 0/16 (0.00%)  0 0/16 (0.00%)  0
Skin abrasion  1  0/16 (0.00%)  0 0/16 (0.00%)  0 0/16 (0.00%)  0 1/16 (6.25%)  1 0/16 (0.00%)  0
Musculoskeletal and connective tissue disorders           
Back pain  1  0/16 (0.00%)  0 0/16 (0.00%)  0 0/16 (0.00%)  0 1/16 (6.25%)  1 0/16 (0.00%)  0
Nervous system disorders           
Headache  1  1/16 (6.25%)  1 2/16 (12.50%)  2 2/16 (12.50%)  2 3/16 (18.75%)  4 0/16 (0.00%)  0
Reproductive system and breast disorders           
Dysmenorrhoea  1  0/16 (0.00%)  0 1/16 (6.25%)  1 0/16 (0.00%)  0 0/16 (0.00%)  0 0/16 (0.00%)  0
Menstrual discomfort  1  0/16 (0.00%)  0 0/16 (0.00%)  0 0/16 (0.00%)  0 1/16 (6.25%)  1 0/16 (0.00%)  0
Respiratory, thoracic and mediastinal disorders           
Cough  1  0/16 (0.00%)  0 0/16 (0.00%)  0 0/16 (0.00%)  0 2/16 (12.50%)  2 0/16 (0.00%)  0
Vascular disorders           
Hot flush  1  1/16 (6.25%)  1 0/16 (0.00%)  0 0/16 (0.00%)  0 0/16 (0.00%)  0 0/16 (0.00%)  0
1
Term from vocabulary, MedDRA 18.0
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.
The Sponsor must have the opportunity to review all proposed abstracts, manuscripts or presentations regarding this trial 45 days prior to submission for publication/presentation. Any information identified by the Sponsor as confidential must be deleted prior to submission; this confidentiality does not include efficacy and safety results.
Results Point of Contact
Layout table for Results Point of Contact information
Name/Title: Senior Vice President, Global Clinical Development
Organization: Merck Sharp & Dohme Corp.
Phone: 1-800-672-6372
EMail: ClinicalTrialsDisclosure@merck.com
Layout table for additonal information
Responsible Party: Merck Sharp & Dohme Corp.
ClinicalTrials.gov Identifier: NCT02549040    
Other Study ID Numbers: 1439-046
2015-002702-36 ( EudraCT Number )
MK-1439-046 ( Other Identifier: Merck Protocol Number )
First Submitted: September 11, 2015
First Posted: September 14, 2015
Results First Submitted: September 27, 2018
Results First Posted: February 22, 2019
Last Update Posted: January 7, 2021