Bioavailability Study of 3 Tablet Formulations vs. Capsule Formulation of JNJ-56021927 in Fasting Healthy Male Participants

NCT02160756 | Completed Phase 1

• 2 other identifiers: CR10482456021927PCR1011
• Study Type: interventional
• Target: 75
• Locations: 0 countries
• Sites: N/A

Brief Summary

The purpose of this study is to evaluate the pharmacokinetics (PK - the study of the way a drug enters and leaves the blood and tissues over time) and relative bioavailability (the extent to which a drug or other substance becomes available to the body) of JNJ-56021927, when administered as 3 tablet formulations (test) compared with JNJ-54781532 softgel capsule formulation (reference) in healthy male participants under fasted conditions at a single dose of 240 milligram (mg).

Conditions

Healthy

Keywords

Healthy; JNJ-56021927; JNJ-56142060; ARN-509

Outcome Measures

Primary Outcomes (14)

• Maximum Plasma Concentration (Cmax)

  The Cmax is the maximum observed plasma concentration.

  Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 , 24, 48, 72, 96, 120, 144, 168, 336, 504, 672, 840, 1008, 1176, 1344 hours post-administration of drug on Day 1

• Time to Reach Maximum Concentration (Tmax)

  The Tmax is time to reach the maximum observed plasma concentration.

  Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 , 24, 48, 72, 96, 120, 144, 168, 336, 504, 672, 840, 1008, 1176, 1344 hours post-administration of drug on Day 1

• Area Under the Plasma Concentration-Time Curve From Time Zero to Time 72 Hours (AUC [0-72])

  Area Under the Plasma Concentration-Time Curve From Time Zero to Time 72 Hours (AUC \[0-72\]) will be evaluated.

  Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 , 24, 48, 72 hours post-administration of drug on Day 1

• Area Under the Plasma Concentration-Time Curve From Time Zero to Time 168 Hours (AUC [0-168])

  Area Under the Plasma Concentration-Time Curve From Time Zero to Time 168 Hours (AUC \[0-168\]) will be evaluated.

  Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 , 24, 48, 72, 96, 120, 144, 168 hours post-administration of drug on Day 1

• Area Under the Plasma Concentration-Time Curve From Time Zero to Last Quantifiable Time (AUC [0-last])

  Area under the plasma concentration-time curve from time zero to time of last quantifiable concentration (AUC \[0-last\]) will be evaluated.

  Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 , 24, 48, 72, 96, 120, 144, 168, 336, 504, 672, 840, 1008, 1176, 1344 hours post-administration of drug on Day 1

• Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0-infinity)]

  The AUC (0-infinity) is the area under the plasma concentration-time curve from time zero to infinite time, calculated as the sum of AUC (0-last) and Clast/lambda(z), wherein AUC (0-last) is area under the plasma concentration-time curve from time zero to last quantifiable time; Clast is the last observed quantifiable concentration; and lambda(z) is elimination rate constant.

  Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 , 24, 48, 72, 96, 120, 144, 168, 336, 504, 672, 840, 1008, 1176, 1344 hours post-administration of drug on Day 1

• Extrapolated Area Under the Curve (AUC Percent [%] Extrap)

  The AUC%extrap is the percentage of AUC \[0-infinity\] obtained by forward extrapolation. It is calculated as (AUC \[0-infinity\] minus AUC \[0-last\])\*100/ AUC \[0-infinity\], where AUC \[0-infinity\] = Area under the plasma concentration versus time curve from time zero (pre-dose) to extrapolated infinite time and AUClast is area under the plasma concentration time-curve from zero (pre-dose) to the last measured concentration.

  Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 , 24, 48, 72, 96, 120, 144, 168, 336, 504, 672, 840, 1008, 1176, 1344 hours post-administration of drug on Day 1

• Elimination Half-Life (t1/2)

  Elimination half-life (t1/2) is the time measured for the plasma concentration to decrease by one half. Elimination half-life associated with the terminal slope of the semi-logarithmic drug concentration-time curve, calculated as 0.693/elimination rate constant (lambda\[z\]).

  Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 , 24, 48, 72, 96, 120, 144, 168, 336, 504, 672, 840, 1008, 1176, 1344 hours post-administration of drug on Day 1

• Elimination Rate Constant (lambda[z])

  Elimination rate constant is the fraction of a drug that is removed from the body per unit time.

  Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 , 24, 48, 72, 96, 120, 144, 168, 336, 504, 672, 840, 1008, 1176, 1344 hours post-administration of drug on Day 1

• Time to Last Quantifiable Plasma Concentration (Tlast)

  The Tlast is time to reach the last quantifiable plasma concentration.

  Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 , 24, 48, 72, 96, 120, 144, 168, 336, 504, 672, 840, 1008, 1176, 1344 hours post-administration of drug on Day 1

• Relative Bioavailability

  Bioavailability means the extent to which the active ingredient of a drug dosage form becomes available at the site of drug action or in a biological medium believed to reflect accessibility to a site of action. Relative bioavailability is the percentage of the administered dose that is systemically available, calculated as: (AUC \[0-infinity\] of test divided by AUC \[0-infinity\] of reference) multiplied by 100, where the reference treatment is a non-intravenous administration.

  Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 , 24, 48, 72, 96, 120, 144, 168, 336, 504, 672, 840, 1008, 1176, 1344 hours post-administration of drug on Day 1

• Metabolite to Parent Drug Ratio for Maximum Observed Plasma Concentration (MPR Cmax)

  The (MPR Cmax) is metabolite to parent drug ratio for maximum observed plasma concentration.

  Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 , 24, 48, 72, 96, 120, 144, 168, 336, 504, 672, 840, 1008, 1176, 1344 hours post-administration of drug on Day 1

• Metabolite to Parent Drug Ratio for Area Under the Plasma Concentration-Time Curve From Time 0 to Last Observed Quantifiable Concentration (MPR AUC[0-last])

  The MPR AUClast is metabolite to parent drug ratio for area under the plasma concentration-time curve from time 0 to last quantifiable concentration (AUC \[0-last\]).

  Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 , 24, 48, 72, 96, 120, 144, 168, 336, 504, 672, 840, 1008, 1176, 1344 hours post-administration of drug on Day 1

• Metabolite to Parent Drug Ratio for Area Under the Plasma Concentration-Time Curve From Time Zero to Extrapolated Infinite Time (MPR AUC [0-infinity])

  The MPR AUC \[0-infinity\] is metabolite to parent drug ratio for area under the plasma concentration-time curve from time zero to extrapolated infinite time (AUC \[0-infinity\]).

  Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 , 24, 48, 72, 96, 120, 144, 168, 336, 504, 672, 840, 1008, 1176, 1344 hours post-administration of drug on Day 1

Secondary Outcomes (1)

• Number of Participants With Treatment-Emergent Adverse Events (AEs) or Serious Adverse Events (SAEs)

  Screening up to Day 57 or early withdrawal

Study Arms (4)

Treatment A

ACTIVE COMPARATOR

Single oral dose of JNJ-56021927 240 milligram (mg) softgel capsule on Day 1.

Drug: JNJ-56021927 Softgel Capsule

Treatment B

EXPERIMENTAL

Single oral dose of JNJ-56021927 240 mg Tablet Formulation 1 on Day 1.

Drug: JNJ-56021927 Tablet Formulation 1

Treatment C

EXPERIMENTAL

Single oral dose of JNJ-56021927 240 mg Tablet Formulation 2 on Day 1.

Drug: JNJ-56021927 Tablet Formulation 2

Treatment D

EXPERIMENTAL

Single oral dose of JNJ-56021927 240 mg Tablet Formulation 3 on Day 1.

Drug: JNJ-56021927 Tablet Formulation 3

Interventions

JNJ-56021927 Softgel Capsule DRUG

Single oral dose of JNJ-56021927 240 mg softgel capsule on Day 1.

Also known as: ARN-509

Treatment A

JNJ-56021927 Tablet Formulation 1 DRUG

Single oral dose of JNJ-56021927 240 mg Tablet Formulation 1 on Day 1.

Treatment B

JNJ-56021927 Tablet Formulation 2 DRUG

Single oral dose of JNJ-56021927 240 mg Tablet Formulation 2 on Day 1.

Treatment C

JNJ-56021927 Tablet Formulation 3 DRUG

Single oral dose of JNJ-56021927 240 mg Tablet Formulation 3 on Day 1.

Treatment D

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Must agree to use an adequate contraception method as deemed appropriate by the investigator, always use a condom during sexual intercourse, and to not donate sperm during the study and for 3 months after receiving the study drug
• Body mass index between 18 and 30 kilogram (kg) per square meter, and body weight not less than 50 kg
• Blood pressure (supine for 5 minutes) between 90 and 140 millimeter of mercury (mm Hg) systolic, and no higher than 90 mm Hg diastolic
• A 12-lead electrocardiogram (ECG) consistent with normal cardiac conduction and function, including pulse rate between 45 and 99 beats per minute (bpm), QT corrected Fridericia (QTcF) interval less than or equal to 450 milliseconds (msec), QRS interval of less than 120 msec, PR interval less than 220 msec, morphology consistent with healthy cardiac conduction and function
• Nonsmoker within the previous 2 months

You may not qualify if:

• 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, hepatic or renal insufficiency, thyroid disease, neurologic or psychiatric disease, infection
• Known hypersensitivity to Vitamin E
• History of stomach or intestinal surgery or resection that would potentially alter absorption or excretion of orally administered drugs
• Known allergy to the study drug or any of the excipients of the formulation
• Unable to swallow solid, oral dosage forms whole with the aid of water

Sponsors & Collaborators

• Aragon Pharmaceuticals, Inc.: lead

MeSH Terms

Interventions

apalutamide

Study Officials

• Janssen Research & Development, LLC Clinical Trial

  Janssen Research & Development, LLC

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: June 9, 2014
• First Posted: June 11, 2014
• Study Start: June 1, 2014
• Primary Completion: November 1, 2014
• Study Completion: November 1, 2014
• Last Updated: February 3, 2025

Record last verified: 2025-01