A Study to Evaluate the Pharmacokinetics (PK) of Darunavir (DRV) and Cobicistat (COBI) After a Single Oral Administration of Darunavir/Cobicistat Fixed-Dose Combination in Healthy Japanese Adult Participants

An Open-label Study to Evaluate the Pharmacokinetics (PK) of Darunavir (DRV) and Cobicistat (COBI) After a Single-oral Administration of Darunavir/Cobicistat Fixed-Dose Combination Tablet in Healthy Japanese Adult Subjects

The purpose of the study is to evaluate the pharmacokinetic (PK) and safety of darunavir (DRV) and cobicistat (COBI) after a single oral administration of Prezcobix (DRV/COBI fixed-dose combination tablet) in healthy Japanese adult participants.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: Darunavir/Cobicistat

• Study Type: Interventional
• Enrollment (Actual): 8
• Phase: Phase 4

Contacts and Locations

Study Locations

• Japan
  • Fukuoka, Japan, 8120025
    • Souseikai Hakata Clinic

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 20 years to 55 years (Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• Participants must be healthy on the basis of physical examination, medical history, vital signs, and 12-lead electrocardiogram (ECG) performed at screening. This determination must be recorded in the participants source documents and initialed by the investigator
• A woman of childbearing potential must have a negative serum (beta-human chorionic gonadotropin [hCG]) at screening and urine pregnancy test at the time of admission to the study site, hospitalization, and must not breast feed from screening onwards
• Contraceptive use by men or women should be consistent with local regulations regarding the use of contraceptive methods for participant participating in clinical studies
• A woman must agree not to donate eggs (ova, oocytes) for the purposes of assisted reproduction during the study and for a period of at least 30 days after intake of the study drug
• Nonsmoker or participant who habitually smokes no more than 10 cigarettes or equivalent of e-cigarettes, or 2 cigars, or 2 pipes of tobacco per day for at least 6 months before study drug administration

Exclusion Criteria:

• Participant has a history of or current clinically significant medical illness including (but not limited to) cardiac arrhythmias or other cardiac disease, hematologic disease, coagulation disorders (including any abnormal bleeding or blood dyscrasias), lipid abnormalities, significant pulmonary disease, including bronchospastic respiratory disease, diabetes mellitus, liver or renal insufficiency (estimated creatinine clearance below 80 milliliter per minute [mL/min]); thyroid disease, neurologic or psychiatric disease, infection, significant cardiac, vascular, pulmonary, gastrointestinal, endocrine, neurologic, hematologic, rheumatologic, psychiatric, metabolic disturbances or any other illness that the investigator considers should exclude the participant or that could interfere with the interpretation of the study results
• Participant has a history of malignancy before screening (exceptions are squamous and basal cell carcinomas of the skin and carcinoma in situ of the cervix, or malignancy, that is considered cured with minimal risk of recurrence)
• Participant has a history of or current clinically significant skin reactions (such as but not limited to Stevens-Johnson Syndrome [SJS], Toxic Epidermal Necrolysis (TEN), and/or erythema multiforme) or any history of allergies to drugs, such as, but not limited to, sulfonamides and penicillins
• Participant has been contraindicated DRV and COBI per local prescribing information
• Participant is a woman, who is pregnant, or breast-feeding, or planning to become pregnant while enrolled in this study

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Other
• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Darunavir/Cobicistat FDC (Prezcobix); Participants will receive one darunavir/cobicistat fixed-dose combination (FDC) tablet, containing 800 milligram (mg) of darunavir (DRV) and 150 mg of cobicistat (COBI) in the morning on Day 1.	Drug: Darunavir/Cobicistat; Participants will receive a FDC tablet of darunavir 800 mg and cobicistat 150 mg orally in the morning of Day 1.; Other Names: TMC114/JNJ-48763364-AAA

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Maximum Observed Plasma Concentration (Cmax)	The Cmax is the maximum observed plasma concentration.	Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 9, 12, 16, 20, 24, 36, 48, 60, 72 hours postdose
Concentration at Last Quantifiable Time Point (Clast)	Clast is defined as concentration at last quantifiable time point.	Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 9, 12, 16, 20, 24, 36, 48, 60, 72 hours postdose
Time to Reach the Maximum Plasma Concentration (Tmax)	Tmax is defined as the time to reach the maximum plasma concentration.	Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 9, 12, 16, 20, 24, 36, 48, 60, 72 hours postdose
Area Under the Plasma Concentration-Time Curve From Time Zero to Time the Last Quantifiable Time (AUC[0-last])	AUC(0-last) is defined as area under the plasma concentration-time curve from time zero to time the last quantifiable time, calculated by linear trapezoidal summation.	Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 9, 12, 16, 20, 24, 36, 48, 60, 72 hours postdose
Area Under the Plasma Concentration-Time Curve From Time Zero to Infinite Time (AUC0-infinity)	AUC(0-infinity) is defined as area under the plasma concentration-time curve from time zero to infinite time.	Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 9, 12, 16, 20, 24, 36, 48, 60, 72 hours postdose
Elimination Rate Constant (Lambda[z])	Lambda(z) is first-order rate constant associated with the terminal portion of the curve, determined as the negative slope of the terminal log-linear phase of the drug concentration-time curve.	Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 9, 12, 16, 20, 24, 36, 48, 60, 72 hours postdose
Terminal Elimination Half-Life (t1/2)	t1/2 is the time measured for the plasma concentration to decrease by 1 half to its original concentration. It is associated with the terminal slope of the semi logarithmic drug concentration-time curve, and is calculated as 0.693/lambda(z).	Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 9, 12, 16, 20, 24, 36, 48, 60, 72 hours postdose
Apparent Volume of Distribution (Vz/F)	Vz/F is defined as the apparent volume of distribution at the terminal phase after extravascular administration.	Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 9, 12, 16, 20, 24, 36, 48, 60, 72 hours postdose
Apparent Total Body Clearance of Drug at the Terminal Phase After Extravascular Administration (CL/F)	CL/F is the apparent total body clearance of drug at the terminal phase after extravascular administration.	Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 9, 12, 16, 20, 24, 36, 48, 60, 72 hours postdose

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Number of Participants With Adverse Events (AEs)	An AE is any untoward medical occurrence in a participant participating in a clinical study that does not necessarily have a causal relationship with the pharmaceutical/biological agent under study.	Up to approximately 1 month

Collaborators and Investigators

• Sponsor: Janssen Pharmaceutical K.K.

Study record dates

Study Major Dates

• Study Start (Actual): April 14, 2017
• Primary Completion (Actual): May 19, 2017
• Study Completion (Actual): May 19, 2017

Study Registration Dates

• First Submitted: April 19, 2017
• First Submitted That Met QC Criteria: April 19, 2017
• First Posted (Actual): April 21, 2017

Study Record Updates

• Last Update Posted (Actual): June 12, 2018
• Last Update Submitted That Met QC Criteria: May 15, 2018
• Last Verified: May 1, 2018

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Molecular Mechanisms of Pharmacological Action; Anti-Infective Agents; Antiviral Agents; Enzyme Inhibitors; Anti-HIV Agents; Anti-Retroviral Agents; Protease Inhibitors; Cytochrome P-450 CYP3A Inhibitors; Cytochrome P-450 Enzyme Inhibitors; HIV Protease Inhibitors; Viral Protease Inhibitors; Cobicistat; Darunavir; Cobicistat mixture with darunavir
• Other Study ID Numbers: CR108319; TMC114FD1HTX4002 (Other Identifier: Janssen Pharmaceutical K.K., Japan)

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: Yes
• Studies a U.S. FDA-regulated device product: No
• product manufactured in and exported from the U.S.: Yes