Phase 1 Completed N=24 Treatment

The Pharmacokinetics of Grazoprevir (MK-5172) and Elbasvir (MK-8742) in Participants With Renal Insufficiency (MK-5172-050)

Source: ClinicalTrials.gov NCT01937975 ↗

Enrolled (actual)

Serious AEs

0.0%

Results posted

Mar 2016

Primary outcomePrimary: Area Under the Concentration-time Curve From 0 to 24 Hours Postdose (AUC0-24hr) of Grazoprevir — 0.969; NA; NA; 0.944 uM*hr

Summary

Grazoprevir (MK-5172) and Elbasvir (MK-8742) were studied as the principal components of combination oral therapy for hepatitis C virus (HCV). The study examined the pharmacokinetic (PK) profiles of Grazoprevir and Elbasvir following 10 days of dosing in participants with end stage renal disease (ESRD) on hemodialysis (HD) or participants with severe renal impairment. Both groups were compared to healthy matched controls.

Outcome Measures

Outcome	Result	p-value
PRIMARY Area Under the Concentration-time Curve From 0 to 24 Hours Postdose (AUC0-24hr) of Grazoprevir	0.969; NA; NA; 0.944; 1.88; 1.14	—
PRIMARY Plasma Concentration at 24 Hours Postdose (C24hr) of Grazoprevir	11.4; NA; NA; 11.3; 23.3; 14.5	—
PRIMARY Maximum Plasma Concentration (Cmax) of Grazoprevir	0.141; NA; NA; 0.135; 0.255; 0.154	—
PRIMARY Time of Maximum Plasma Concentration (Tmax) of Grazoprevir	2.00; NA; NA; 2.50; 3.00; 2.50	—
PRIMARY Apparent Terminal Half-life (T1/2) of Grazoprevir	28.38; 36.30; 35.18	—
PRIMARY Apparent Clearance After Extravascular Administration (CL/F) of Grazoprevir	135; NA; NA; 138; 69.4; 114	—
PRIMARY Apparent Volume of Distribution After Extravascular Administration (Vz/F) of Grazoprevir	5430; 3490; 5760	—
PRIMARY Area Under the Concentration-time Curve From 0 to 24 Hours Postdose (AUC0-24hr) of Elbasvir	1.89; NA; NA; 2.16; 4.07; 2.19	—
PRIMARY Plasma Concentration at 24 Hours Postdose (C24hr) of Elbasvir	46.9; NA; NA; 58.2; 126; 60.9	—
PRIMARY Maximum Plasma Concentration (Cmax) of Elbasvir	0.137; NA; NA; 0.154; 0.271; 0.163	—
PRIMARY Time of Maximum Plasma Concentration (Tmax) of Elbasvir	4.00; NA; NA; 5.00; 4.00; 4.00	—
PRIMARY Apparent Terminal Half-life (T1/2) of Elbasvir	23.04; 28.97; 25.02	—
PRIMARY Apparent Clearance After Extravascular Administration (CL/F) of Elbasvir	29.9; NA; NA; 26.2; 13.9; 25.9	—
PRIMARY Apparent Volume of Distribution After Extravascular Administration (Vz/F) of Elbasvir	857; 569; 901	—

Eligibility Criteria

Inclusion Criteria

All Participants

For a female of childbearing potential: either be sexually inactive (abstinent) for 14 days prior to the first dose and throughout the study or be using an acceptable birth control method. Females of non-childbearing potential must have undergone a sterilization procedure at least 6 months prior to the first dose
Non-vasectomized male participants must agree to use a condom with spermicide or abstain from sexual intercourse during the trial and for 90 days after stopping the study medication and agree not to donate sperm during this time period Participants with ESRD on HD
Maintained on a stable regimen of HD within 3 months prior to first dosing Participants with Severe Renal Impairment
Estimated glomerular filtration rate (eGFR) at screening is =80 mL/min/1.73m^2

Exclusion Criteria

All Participants

History or presence of significant cardiovascular, pulmonary, hepatic, renal, hematological, gastrointestinal, endocrine, immunologic, dermatologic, or neurological disease whose current condition is considered unstable
History or presence of alcoholism and drug abuse within the past 6 months
Female participants who are pregnant or lactating
Regular user of any medication (including over the counter) that would significantly alter GFR
Donation of blood or significant blood loss within 56 days prior to the first dose of study medication(s)
Plasma donation within 7 days prior to the first dose of study medication(s)
A renal transplant or nephrectomy Participants with ESRD or Severe Renal Impairment
Rapidly fluctuating renal function

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Data sourced from ClinicalTrials.gov (NCT01937975). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.