Trial Outcomes & Findings for 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 (NCT NCT03123848)

NCT ID: NCT03123848

Last Updated: 2025-02-04

Results Overview

The Cmax is the maximum observed plasma concentration.

Recruitment status

COMPLETED

Study phase

PHASE4

Target enrollment

8 participants

Primary outcome timeframe

Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 9, 12, 16, 20, 24, 36, 48, 60, 72 hours postdose

Results posted on

2025-02-04

Participant Flow

Participant milestones

Participant milestones
Measure	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.
Overall Study STARTED	8
Overall Study COMPLETED	8
Overall Study NOT COMPLETED	0

Reasons for withdrawal

Withdrawal data not reported

Baseline Characteristics

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

Baseline characteristics by cohort

Baseline characteristics by cohort
Measure	Darunavir 800 mg/Cobicistat 150 mg as FDC (Prezcobix) n=8 Participants 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.
Age, Continuous	33.1 years STANDARD_DEVIATION 6.10 • n=5 Participants
Sex/Gender, Customized Male	8 Participants n=5 Participants
Ethnicity (NIH/OMB) Hispanic or Latino	0 Participants n=5 Participants
Ethnicity (NIH/OMB) Not Hispanic or Latino	8 Participants n=5 Participants
Ethnicity (NIH/OMB) Unknown or Not Reported	0 Participants n=5 Participants
Race/Ethnicity, Customized Asian	8 Participants n=5 Participants
Region of Enrollment JAPAN	8 Participants n=5 Participants

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 9, 12, 16, 20, 24, 36, 48, 60, 72 hours postdose

Population: Pharmacokinetic (PK) analysis set included all participants who received the study drug and had at least one plasma concentration data-point after administration. Cmax for each analyte (Darunavir and Cobicistat) of fixed dose combination has been reported separately in each arm as per planned analysis.

The Cmax is the maximum observed plasma concentration.

Outcome measures

Outcome measures
Measure	Darunavir 800 mg (FDC: Darunavir 800/Cobicistat 150 mg) n=8 Participants Participants received darunavir 800 mg along with cobicistat 150 mg in a fixed-dose combination (FDC) as film-coated tablet formulation (PREZCOBIX) once orally on Day 1.	Cobicistat 150 mg (FDC: Darunavir 800/Cobicistat 150 mg) n=8 Participants Participants received darunavir 800 mg along with cobicistat 150 mg in a fixed-dose combination (FDC) as film-coated tablet formulation (PREZCOBIX) once orally on Day 1.
Maximum Observed Plasma Concentration (Cmax)	5496 nanogram per milliliter (ng/mL) Standard Deviation 952	832 nanogram per milliliter (ng/mL) Standard Deviation 265

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 9, 12, 16, 20, 24, 36, 48, 60, 72 hours postdose

Population: PK analysis set included all participants who received the study drug and had at least one plasma concentration data-point after administration. Clast for each analyte (Darunavir and Cobicistat) of fixed dose combination has been reported separately in each arm as per planned analysis.

Clast is defined as concentration at last quantifiable time point.

Outcome measures

Outcome measures
Measure	Darunavir 800 mg (FDC: Darunavir 800/Cobicistat 150 mg) n=8 Participants Participants received darunavir 800 mg along with cobicistat 150 mg in a fixed-dose combination (FDC) as film-coated tablet formulation (PREZCOBIX) once orally on Day 1.	Cobicistat 150 mg (FDC: Darunavir 800/Cobicistat 150 mg) n=8 Participants Participants received darunavir 800 mg along with cobicistat 150 mg in a fixed-dose combination (FDC) as film-coated tablet formulation (PREZCOBIX) once orally on Day 1.
Concentration at Last Quantifiable Time Point (Clast)	33.3 ng/mL Standard Deviation 60.3	8.59 ng/mL Standard Deviation 3.24

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 9, 12, 16, 20, 24, 36, 48, 60, 72 hours postdose

Population: PK analysis set included all participants who received the study drug and had at least one plasma concentration data-point after administration. Tmax for each analyte (Darunavir and Cobicistat) of fixed dose combination has been reported separately in each arm as per planned analysis.

Tmax is defined as the time to reach the maximum plasma concentration.

Outcome measures

Outcome measures
Measure	Darunavir 800 mg (FDC: Darunavir 800/Cobicistat 150 mg) n=8 Participants Participants received darunavir 800 mg along with cobicistat 150 mg in a fixed-dose combination (FDC) as film-coated tablet formulation (PREZCOBIX) once orally on Day 1.	Cobicistat 150 mg (FDC: Darunavir 800/Cobicistat 150 mg) n=8 Participants Participants received darunavir 800 mg along with cobicistat 150 mg in a fixed-dose combination (FDC) as film-coated tablet formulation (PREZCOBIX) once orally on Day 1.
Time to Reach the Maximum Plasma Concentration (Tmax)	4.00 hour (h) Interval 3.0 to 4.0	4.00 hour (h) Interval 2.0 to 4.0

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 9, 12, 16, 20, 24, 36, 48, 60, 72 hours postdose

Population: PK analysis set included all participants who received the study drug and had at least one plasma concentration data-point after administration time zero to time the last quantifiable time. AUC\[0-last\] for each analyte (Darunavir and Cobicistat) of fixed dose combination has been reported separately in each arm as per planned analysis.

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.

Outcome measures

Outcome measures
Measure	Darunavir 800 mg (FDC: Darunavir 800/Cobicistat 150 mg) n=8 Participants Participants received darunavir 800 mg along with cobicistat 150 mg in a fixed-dose combination (FDC) as film-coated tablet formulation (PREZCOBIX) once orally on Day 1.	Cobicistat 150 mg (FDC: Darunavir 800/Cobicistat 150 mg) n=8 Participants Participants received darunavir 800 mg along with cobicistat 150 mg in a fixed-dose combination (FDC) as film-coated tablet formulation (PREZCOBIX) once orally on Day 1.
Area Under the Plasma Concentration-Time Curve From Time Zero to Time the Last Quantifiable Time (AUC[0-last])	51274 hournanogram per milliliter (hng/mL) Standard Deviation 15983	5667 hournanogram per milliliter (hng/mL) Standard Deviation 3119

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 9, 12, 16, 20, 24, 36, 48, 60, 72 hours postdose

Population: PK analysis set included all participants who received the study drug and had at least one plasma concentration data-point after administration. AUC0-inf for each analyte (Darunavir and Cobicistat) of fixed dose combination has been reported separately in each arm as per planned analysis.

AUC(0-infinity) is defined as area under the plasma concentration-time curve from time zero to infinite time.

Outcome measures

Outcome measures
Measure	Darunavir 800 mg (FDC: Darunavir 800/Cobicistat 150 mg) n=8 Participants Participants received darunavir 800 mg along with cobicistat 150 mg in a fixed-dose combination (FDC) as film-coated tablet formulation (PREZCOBIX) once orally on Day 1.	Cobicistat 150 mg (FDC: Darunavir 800/Cobicistat 150 mg) n=8 Participants Participants received darunavir 800 mg along with cobicistat 150 mg in a fixed-dose combination (FDC) as film-coated tablet formulation (PREZCOBIX) once orally on Day 1.
Area Under the Plasma Concentration-Time Curve From Time Zero to Infinite Time (AUC0-infinity)	51460 h*ng/mL Standard Deviation 15836	5710 h*ng/mL Standard Deviation 3128

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 9, 12, 16, 20, 24, 36, 48, 60, 72 hours postdose

Population: PK analysis set included all participants who received the study drug and had at least one plasma concentration data-point after administration. Lambda\[z\] for each analyte (Darunavir and Cobicistat) of fixed dose combination has been reported separately in each arm as per planned analysis.

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.

Outcome measures

Outcome measures
Measure	Darunavir 800 mg (FDC: Darunavir 800/Cobicistat 150 mg) n=8 Participants Participants received darunavir 800 mg along with cobicistat 150 mg in a fixed-dose combination (FDC) as film-coated tablet formulation (PREZCOBIX) once orally on Day 1.	Cobicistat 150 mg (FDC: Darunavir 800/Cobicistat 150 mg) n=8 Participants Participants received darunavir 800 mg along with cobicistat 150 mg in a fixed-dose combination (FDC) as film-coated tablet formulation (PREZCOBIX) once orally on Day 1.
Elimination Rate Constant (Lambda[z])	0.173 per hour (1/h) Standard Deviation 0.0668	0.199 per hour (1/h) Standard Deviation 0.0233

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 9, 12, 16, 20, 24, 36, 48, 60, 72 hours postdose

Population: PK analysis set included all participants who received the study drug and had at least one plasma concentration data-point after administration. t1/2 for each analyte (Darunavir and Cobicistat) of fixed dose combination has been reported separately in each arm as per planned analysis.

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).

Outcome measures

Outcome measures
Measure	Darunavir 800 mg (FDC: Darunavir 800/Cobicistat 150 mg) n=8 Participants Participants received darunavir 800 mg along with cobicistat 150 mg in a fixed-dose combination (FDC) as film-coated tablet formulation (PREZCOBIX) once orally on Day 1.	Cobicistat 150 mg (FDC: Darunavir 800/Cobicistat 150 mg) n=8 Participants Participants received darunavir 800 mg along with cobicistat 150 mg in a fixed-dose combination (FDC) as film-coated tablet formulation (PREZCOBIX) once orally on Day 1.
Terminal Elimination Half-Life (t1/2)	4.4 Hour Standard Deviation 1.4	3.5 Hour Standard Deviation 0.4

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 9, 12, 16, 20, 24, 36, 48, 60, 72 hours postdose

Population: PK analysis set included all participants who received the study drug and had at least one plasma concentration data-point after administration. Vz/F for each analyte (Darunavir and Cobicistat) of fixed dose combination has been reported separately in each arm as per planned analysis.

Vz/F is defined as the apparent volume of distribution at the terminal phase after extravascular administration.

Outcome measures

Outcome measures
Measure	Darunavir 800 mg (FDC: Darunavir 800/Cobicistat 150 mg) n=8 Participants Participants received darunavir 800 mg along with cobicistat 150 mg in a fixed-dose combination (FDC) as film-coated tablet formulation (PREZCOBIX) once orally on Day 1.	Cobicistat 150 mg (FDC: Darunavir 800/Cobicistat 150 mg) n=8 Participants Participants received darunavir 800 mg along with cobicistat 150 mg in a fixed-dose combination (FDC) as film-coated tablet formulation (PREZCOBIX) once orally on Day 1.
Apparent Volume of Distribution (Vz/F)	111970 milliliter (mL) Standard Deviation 61217	166460 milliliter (mL) Standard Deviation 76366

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 9, 12, 16, 20, 24, 36, 48, 60, 72 hours postdose

Population: PK analysis set included all participants who received the study drug and had at least one plasma concentration data-point after administration. CL/F for each analyte (Darunavir and Cobicistat) of fixed dose combination has been reported separately in each arm as per planned analysis.

CL/F is the apparent total body clearance of drug at the terminal phase after extravascular administration.

Outcome measures

Outcome measures
Measure	Darunavir 800 mg (FDC: Darunavir 800/Cobicistat 150 mg) n=8 Participants Participants received darunavir 800 mg along with cobicistat 150 mg in a fixed-dose combination (FDC) as film-coated tablet formulation (PREZCOBIX) once orally on Day 1.	Cobicistat 150 mg (FDC: Darunavir 800/Cobicistat 150 mg) n=8 Participants Participants received darunavir 800 mg along with cobicistat 150 mg in a fixed-dose combination (FDC) as film-coated tablet formulation (PREZCOBIX) once orally on Day 1.
Apparent Total Body Clearance of Drug at the Terminal Phase After Extravascular Administration (CL/F)	16974 milliliter per hour (mL/h) Standard Deviation 5440	33573 milliliter per hour (mL/h) Standard Deviation 16699

SECONDARY outcome

Timeframe: Up to approximately 1 month

Population: Safety analysis set included all participants who received the study drug. AEs for each analyte (Darunavir and Cobicistat) of fixed dose combination has been reported separately as per planned analysis.

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.

Outcome measures

Outcome measures
Measure	Darunavir 800 mg (FDC: Darunavir 800/Cobicistat 150 mg) n=8 Participants Participants received darunavir 800 mg along with cobicistat 150 mg in a fixed-dose combination (FDC) as film-coated tablet formulation (PREZCOBIX) once orally on Day 1.	Cobicistat 150 mg (FDC: Darunavir 800/Cobicistat 150 mg) Participants received darunavir 800 mg along with cobicistat 150 mg in a fixed-dose combination (FDC) as film-coated tablet formulation (PREZCOBIX) once orally on Day 1.
Number of Participants With Adverse Events (AEs)	0 Participants	—

Adverse Events

Darunavir 800 mg/Cobicistat 150 mg as FDC (Prezcobix)

Serious events: 0 serious events

Other events: 0 other events

Deaths: 0 deaths

Serious adverse events

Adverse event data not reported

Other adverse events

Adverse event data not reported

Additional Information

Director, IDV Department

Janssen Pharmaceutical K.K.

Phone: 844-434-4210

Email: [email protected]

Results disclosure agreements

Principal investigator is a sponsor employee If an investigator wishes to publish information from the study, a copy of the manuscript must be provided to the sponsor for review at least 60 days before submission for publication or presentation. If requested in writing, such publication will be withheld for up to an additional 60 days.
Publication restrictions are in place

Restriction type: OTHER