Pharmacokinetics, Safety And Toleration Of Maraviroc Administered To Subjects With Various Degrees Of Renal Impaired And Normal Renal Function
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ClinicalTrials.gov Identifier: NCT00717067 |
Recruitment Status
:
Completed
First Posted
: July 16, 2008
Results First Posted
: December 21, 2009
Last Update Posted
: November 19, 2010
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Condition or disease | Intervention/treatment | Phase |
---|---|---|
Human Immunodeficiency Virus (HIV) Infection | Drug: Maraviroc Drug: Ritonavir Drug: Saquinavir | Phase 4 |
Study Type : | Interventional (Clinical Trial) |
Actual Enrollment : | 30 participants |
Allocation: | Non-Randomized |
Intervention Model: | Parallel Assignment |
Masking: | None (Open Label) |
Primary Purpose: | Treatment |
Official Title: | An Open-Label, Parallel Group, Single And Multiple Dose Study To Evaluate The Pharmacokinetics, Safety And Toleration Of Maraviroc Administered To Subjects With Various Degrees Of Renal Impaired And Normal Renal Function |
Study Start Date : | July 2008 |
Actual Primary Completion Date : | November 2008 |
Actual Study Completion Date : | November 2008 |

Arm | Intervention/treatment |
---|---|
Experimental: Healthy Subjects
Subjects with Normal Renal Function (Creatinine Clearance > 80mL/min) (I) Maraviroc single dose, followed by (II) Maraviroc + Saquinavir/Ritonavir
|
Drug: Maraviroc
Maraviroc 300 mg (150 mg x 2 tablets) x single dose
Drug: Maraviroc
Maraviroc 150 mg tablet twice daily x 7 days
Drug: Ritonavir
Ritonavir 100 mg capsule twice daily x 7 days
Drug: Saquinavir
Saquinavir 1000 mg (500 mg x 2 tablets) twice daily x 7 days
|
Experimental: Mild Renal Impairment
Subjects with Mild Renal Impairment (Creatinine Clearance >50 and ≤80 mL/min)
|
Drug: Maraviroc
Maraviroc 150 mg tablet once daily x 7 days
Drug: Ritonavir
Ritonavir 100 mg capsule twice daily x 7 days
Drug: Saquinavir
Saquinavir 1000 mg (500 mg x 2 tablets) twice daily x 7 days
|
Experimental: Moderate Renal Impairment
Subjects with Moderate Renal Impairment (Creatinine Clearance ≥30 and ≤50 mL/min)
|
Drug: Maraviroc
Maraviroc 150 mg tablet once every 48 hours x 7 days
Drug: Ritonavir
Ritonavir 100 mg capsule twice daily x 7 days
Drug: Saquinavir
Saquinavir 1000 mg (500 mg x 2 tablets) twice daily x 7 days
|
Experimental: Severe Renal Impairment
Subjects with Severe Renal Impairment (Creatinine Clearance <30 mL/min)
|
Drug: Maraviroc
Maraviroc 300 mg (150 mg x 2 tablets) x single dose
|
Experimental: ESRD on Hemodialysis
Subjects with End Stage Renal Impairment receiving Hemodialysis(Creatinine Clearance <30 mL/min) (I) Maraviroc single dose one hour following completion of hemodialysis, followed by (II) Maraviroc single dose three hours prior to start of hemodialysis
|
Drug: Maraviroc
Maraviroc 300 mg (150 mg x 2 tablets) x single dose one hour following completion of hemodialysis
Drug: Maraviroc
Maraviroc 300 mg (150 mg x 2 tablets) x single dose three hours prior to start of hemodialysis
|
- Area Under the Plasma Concentration Time-curve From Zero to the Last Measured Concentration (AUClast) [ Time Frame: Pre-dose, post-dose hours 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, and 72. ]Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast) measured in nanograms * hour divided by milliliters (ng*hr/mL).
- AUCtau [ Time Frame: Pre-dose, post-dose hours 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, and 72. ]AUCtau: area under the plasma concentration-time profile from time zero to the end of the dosing interval (tau); measured in nanograms * hours divided by milliliters (ng.hr/mL).
- Maximum Observed Plasma Concentration (Cmax) [ Time Frame: Pre-dose, post-dose hours 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, and 72. ]Maximum observed plasma concentration (Cmax) within the dosing interval; measured in nanograms per milliliter (ng/mL).
- Plasma Protein Binding [ Time Frame: 2 hours post-dose; normal Day -3 and Day 7; mild moderate: Day 7; severe and ESRD: Day 1 ]Percent protein binding (protein unbound maraviroc (MVC) fraction [percent free]) was determined by rapid equilibrium dialysis. Percent free = 100 - percent bound.
- Area Under the Time Curve From 0 to Infinity (AUCinf) [ Time Frame: Pre-dose, post-dose hours 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, and 72 ]Area under the plasma concentration-time profile from time zero to the time infinate in subjects who received single dose treatment; measured in nanograms * hour divided by millilters (ng*hr/mL).
- Time of First Occurrence (Tmax) [ Time Frame: Pre-dose, post-dose hours 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, and 72. ]Time (hours) of first occurrence (Tmax); time after dosing when Cmax (maximum plasma concentration) occured.
- Half-life (t1/2) [ Time Frame: Pre-dose, post-dose hours 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, and 72. ]Elimination half-life (t1/2) measured in hours: time required for half the quantity of maraviroc to be metabolized or eliminated by normal biological processes.
- Renal Clearance (CLR) in Subjects With Normal, Mild, Moderate and Severe Renal Function [ Time Frame: Hour 0 (prior to MVC dosing [single dose] or prior to last MVC dose [multiple dose]) to 72 hours post-dose ; hours 0, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, and 72. ]Renal clearance (CLR) measured in milliliters per minute (mL/min).
- Derivation of Renal Clearance in Subjects With Normal, Mild, Moderate and Severe Renal Function: Ae [ Time Frame: Hour 0 (prior to MVC dosing [single dose] or prior to last MVC dose [multiple dose]) to 72 hours post-dose ; hours 0, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, and 72. ]Ae: amount of drug excreted unchanged in the urine; measured in milligrams (mg).
- Hemodialysis Clearance of Maraviroc (MVC) in Subjects With End Stage Renal Disease (ESRD) Undergoing Hemodialysis: CLdD [ Time Frame: Before dialysis ]CLdD: dialysate clearance before dialysis; measured in milliliters per minute.
- Safety and Tolerability of Maraviroc in the Absence and Presence of a Potent CYP3A4 Inhibitor in Subjects With Various Degrees of Renal Impairment or Undergoing Hemodialysis: Number of Subjects With Maximum Increase and Decrease in Supine Blood Pressure [ Time Frame: Normal renal function: screening, Day -3 to Day -1; normal, mild and moderate RI: Day 7 to Day 10 and follow-up; severe RI: Day 1 to Day 4 and follow-up; ESRD: Day 1, Day 4, and follow-up ]Number of subjects with absolute values of supine systolic blood pressure (BP) measured in millimeters of mercury (mm/Hg), range: <90 mmHg; and supine diastolic blood pressure, range: <50 mmHg. Number of subjects with a maximum increase and decrease from Baseline in supine systolic BP ≥ 30 mmHg. Number of subjects with a maximum increase and decrease from Baseline in supine diastolic BP ≥ 20 mmHg.
- Safety and Tolerability of Maraviroc in the Absence and Presence of a Potent CYP3A4 Inhibitor in Subjects With Various Degrees of Renal Impairment or Undergoing Hemodialysis: Number of Subjects With Pulse Rate < 40 and > 120 Beats Per Minute [ Time Frame: Normal renal function: screening, Day -3 to Day -1; normal, mild and moderate RI: Day 7 to Day 10 and follow-up; severe RI: Day 1 to Day 4 and follow-up; ESRD: Day 1, Day 4, and follow-up ]Number of subjects with pulse rate < 40 beats per minute (BPM), number of subjects with pulse rate > 120 BPM.
- Safety and Tolerability of Maraviroc in the Absence and Presence of a Potent CYP3A4 Inhibitor in Subjects With Various Degrees of Renal Impairment or Undergoing Hemodialysis: Number of Subjects With Maximum EGC QTC, QTCB and QTCF Intervals [ Time Frame: Normal renal function: screening, Day -3 and Day -1; normal renal function, mild and moderate RI: Day 7 to Day 9 and follow-up; severe RI: screening, Day 1, Day 3, Day 4, and follow-up; ESRD: screening, Day 1, Day 3, Day 4, and follow-up ]Single 12-lead ECG: number of subjects with maximum QTC interval, maximum QTCB interval (Bazett's correction), and maximum QTCF interval (Friderica's correction) measured in milliseconds (msec); range: 450 to <480 msec, 480 to <500 msec, and >500 msec. Maximum QTC interval increase from Baseline; citeria: change = ≥ 30 msec to < 60 msec, and change = ≥ 60 msec.

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Ages Eligible for Study: | 18 Years to 85 Years (Adult, Senior) |
Sexes Eligible for Study: | All |
Accepts Healthy Volunteers: | Yes |
Inclusion Criteria:
- Stable Renal Function defined as ≤20% (25% for normal renal function) difference between 2 measurements of serum creatinine obtained on 2 occasions separated by at least 2 weeks.
- Body Mass Index (BMI) of approximately 18 to 40 kg/m2 inclusive.
- Total body weight >50 kg (110 lbs).
- Male or female subjects between the ages of 18 and 85 years.
Exclusion Criteria:
- Subjects with acute renal disease and/or history of renal transplant.
- Supine BP at Screening ≥160 mm Hg systolic or ≥95 mm Hg diastolic.
- Supine BP at Screening ≤80 mm Hg systolic or ≤40 mm Hg diastolic.

To learn more about this study, you or your doctor may contact the study research staff using the contact information provided by the sponsor.
Please refer to this study by its ClinicalTrials.gov identifier (NCT number): NCT00717067
Germany | |
Pfizer Investigational Site | |
Berlin, Germany, 10117 | |
Pfizer Investigational Site | |
Muenchen, Germany, 81241 |
Study Director: | Pfizer CT.gov Call Center | Pfizer |
Additional Information:
Responsible Party: | Director, Clinical Trial Disclosure Group, Pfizer, Inc. |
ClinicalTrials.gov Identifier: | NCT00717067 History of Changes |
Other Study ID Numbers: |
A4001075 |
First Posted: | July 16, 2008 Key Record Dates |
Results First Posted: | December 21, 2009 |
Last Update Posted: | November 19, 2010 |
Last Verified: | November 2010 |
Keywords provided by ViiV Healthcare:
maraviroc, pharmacokinetics, renal impairment |
Additional relevant MeSH terms:
Immunologic Deficiency Syndromes Acquired Immunodeficiency Syndrome HIV Infections Immune System Diseases Lentivirus Infections Retroviridae Infections RNA Virus Infections Virus Diseases Sexually Transmitted Diseases, Viral Sexually Transmitted Diseases Slow Virus Diseases Ritonavir Saquinavir |
Maraviroc HIV Protease Inhibitors Protease Inhibitors Enzyme Inhibitors Molecular Mechanisms of Pharmacological Action Anti-HIV Agents Anti-Retroviral Agents Antiviral Agents Anti-Infective Agents Cytochrome P-450 CYP3A Inhibitors Cytochrome P-450 Enzyme Inhibitors CCR5 Receptor Antagonists |