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

Status

Completed

Phases

Phase 4

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT03123848

Enrollment

Registered

2017-04-21

Start date

2017-04-14

Completion date

2017-05-19

Last updated

2025-02-04

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Healthy

Brief summary

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.

Interventions

DRUGDarunavir/Cobicistat

Participants will receive a FDC tablet of darunavir 800 mg and cobicistat 150 mg orally in the morning of Day 1.

Study design

Allocation

Intervention model

SINGLE_GROUP

Primary purpose

OTHER

Masking

NONE

Eligibility

Sex/Gender

ALL

Age

20 Years to 55 Years

Healthy volunteers

Yes

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

Design outcomes

Primary

Measure	Time frame	Description
Apparent Total Body Clearance of Drug at the Terminal Phase After Extravascular Administration (CL/F)	Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 9, 12, 16, 20, 24, 36, 48, 60, 72 hours postdose	CL/F is the apparent total body clearance of drug at the terminal phase after extravascular administration.
Maximum Observed Plasma Concentration (Cmax)	Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 9, 12, 16, 20, 24, 36, 48, 60, 72 hours postdose	The Cmax is the maximum observed plasma concentration.
Concentration at Last Quantifiable Time Point (Clast)	Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 9, 12, 16, 20, 24, 36, 48, 60, 72 hours postdose	Clast is defined as concentration at last quantifiable time point.
Time to Reach the Maximum Plasma Concentration (Tmax)	Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 9, 12, 16, 20, 24, 36, 48, 60, 72 hours postdose	Tmax is defined as the time to reach the maximum plasma concentration.
Area Under the Plasma Concentration-Time Curve From Time Zero to Time the Last Quantifiable Time (AUC[0-last])	Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 9, 12, 16, 20, 24, 36, 48, 60, 72 hours postdose	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.
Area Under the Plasma Concentration-Time Curve From Time Zero to Infinite Time (AUC0-infinity)	Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 9, 12, 16, 20, 24, 36, 48, 60, 72 hours postdose	AUC(0-infinity) is defined as area under the plasma concentration-time curve from time zero to infinite time.
Elimination Rate Constant (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	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.
Terminal Elimination Half-Life (t1/2)	Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 9, 12, 16, 20, 24, 36, 48, 60, 72 hours postdose	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).
Apparent Volume of Distribution (Vz/F)	Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 9, 12, 16, 20, 24, 36, 48, 60, 72 hours postdose	Vz/F is defined as the apparent volume of distribution at the terminal phase after extravascular administration.

Secondary

Measure	Time frame	Description
Number of Participants With Adverse Events (AEs)	Up to approximately 1 month	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.

Countries

Japan

Participant flow

Participants by arm

Arm	Count
Darunavir 800 mg/Cobicistat 150 mg as FDC (Prezcobix) Participants received darunavir 800 milligram (mg) and Cobicistat 150 mg in a fixed-dose combination (FDC) as film-coated tablet formulation (PREZCOBIX) once orally on Day 1.	8
Total	8

Baseline characteristics

Characteristic	Darunavir 800 mg/Cobicistat 150 mg as FDC (Prezcobix)
Age, Continuous	33.1 years STANDARD_DEVIATION 6.1
Ethnicity (NIH/OMB) Hispanic or Latino	0 Participants
Ethnicity (NIH/OMB) Not Hispanic or Latino	8 Participants
Ethnicity (NIH/OMB) Unknown or Not Reported	0 Participants
Race/Ethnicity, Customized Asian	8 Participants
Region of Enrollment JAPAN	8 Participants
Sex/Gender, Customized Male	8 Participants

Adverse events

Event type	EG000 affected / at risk
deaths Total, all-cause mortality	0 / 8
other Total, other adverse events	0 / 8
serious Total, serious adverse events	0 / 8

Outcome results

Primary

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.