A Study to Assess the Relative Bioavailability of 7 Test Tablet Formulations of JNJ-56021927 With Respect to the Capsule Formulation of JNJ-56021927 in Healthy Male Participants

NCT02031666 | Completed Phase 1

• 2 other identifiers: CR10329956021927PCR1007
• Study Type: interventional
• Target: 120
• Locations: 1 country
• Sites: 1

Brief Summary

The purpose of this study is to evaluate the pharmacokinetics (what the body does to the medication) and relative bioavailability (the extent to which a medication or other substance becomes available to the body) of JNJ-56021927 when administered as 7 test tablet formulations of JNJ-56021927 compared with the softgel capsule formulation of JNJ-56021927 in healthy male participants under fasted conditions at a single dose of 240 mg.

Conditions

Healthy

Keywords

Healthy; JNJ-56021927; ARN-509; Bioavailability

Outcome Measures

Primary Outcomes (14)

• Maximum Observed Plasma Concentration (Cmax) of JNJ-56021927

  The Plasma Concentration (Cmax) is defined as maximum observed analyte concentration.

  Pre-dose, and post-dose Day 1 (0.5, 1, 1.5, 2, 4, 6, 8, 12, 24 hours), Day 2, 3, 4, 5, 6, 7, 8, 15, 22, 29, 36, 43, 50, 57

• Time to Reach Maximum Observed Plasma Concentration (Tmax) of JNJ-56021927

  Tmax is defined as actual sampling time to reach maximum observed analyte concentration.

  Pre-dose, and post-dose Day 1 (0.5, 1, 1.5, 2, 4, 6, 8, 12, 24 hours), Day 2, 3, 4, 5, 6, 7, 8, 15, 22, 29, 36, 43, 50, 57

• Area Under the Plasma Concentration-Time Curve From Time of Administration to 72 hours After Dosing (AUC 0-72h) of JNJ-56021927

  The AUC 0-72h is a measure of the plasma concentration of the drug over time. It is used to characterize drug absorption.

  Pre-dose, and post-dose Day 1 (0.5, 1, 1.5, 2, 4, 6, 8, 12, 24 hours), Day 2, 3, 4, 5, 6, 7, 8, 15, 22, 29, 36, 43, 50, 57

• Area Under the Plasma Concentration-Time Curve From Time of Administration to 168 hours After Dosing (AUC 0-168h) of JNJ-56021927

  The AUC 0-168h is a measure of the plasma concentration of the drug over time. It is used to characterize drug absorption.

  Pre-dose, and post-dose Day 1 (0.5, 1, 1.5, 2, 4, 6, 8, 12, 24 hours), Day 2, 3, 4, 5, 6, 7, 8, 15, 22, 29, 36, 43, 50, 57

• Area Under the Plasma Concentration-Time Curve From Time Zero to Time at Last Observed Quantifiable Concentration (AUClast) of JNJ-56021927

  The AUClast is area under the plasma concentration-time curve from time zero to the last quantifiable concentration.

  Pre-dose, and post-dose Day 1 (0.5, 1, 1.5, 2, 4, 6, 8, 12, 24 hours), Day 2, 3, 4, 5, 6, 7, 8, 15, 22, 29, 36, 43, 50, 57

• Area Under the Plasma Concentration-Time Curve From Time Zero to Infinite Time (AUC[0-infinity]) of JNJ-56021927

  The AUC(0-infinity) is area under the plasma concentration-time curve from time zero to infinite time, calculated as the sum of Area under Curve (AUC) last and C(last)/lambda(z), in which C(last) is the last observed quantifiable concentration and lambda\[z\] is the terminal rate-constant of the semi logarithmic drug concentration-time curve.

  Pre-dose, and post-dose Day 1 (0.5, 1, 1.5, 2, 4, 6, 8, 12, 24 hours), Day 2, 3, 4, 5, 6, 7, 8, 15, 22, 29, 36, 43, 50, 57

• Elimination Half-Life Period (T1/2) of JNJ-56021927

  The Elimination Half-Life Period (T1/2) is the time measured for the plasma concentration to decrease by 1 half of its original concentration. It is associated with the terminal rate-constant (lambda\[z\]) of the semi logarithmic drug concentration-time curve, and is calculated as 0.693/lambda(z).

  Pre-dose, and post-dose Day 1 (0.5, 1, 1.5, 2, 4, 6, 8, 12, 24 hours), Day 2, 3, 4, 5, 6, 7, 8, 15, 22, 29, 36, 43, 50, 57

• First-order Rate Constant of JNJ-56021927

  The 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.

  Pre-dose, and post-dose Day 1 (0.5, 1, 1.5, 2, 4, 6, 8, 12, 24 hours), Day 2, 3, 4, 5, 6, 7, 8, 15, 22, 29, 36, 43, 50, 57

• Time to Last Quantifiable Plasma Concentration (tlast) of JNJ-56021927

  Pre-dose, and post-dose Day 1 (0.5, 1, 1.5, 2, 4, 6, 8, 12, 24 hours), Day 2, 3, 4, 5, 6, 7, 8, 15, 22, 29, 36, 43, 50, 57

• Relative Bioavailability (Frel) of JNJ-56021927

  Relative bioavailability is the percentage of the administered dose that is systemically available.

  Pre-dose, and post-dose Day 1 (0.5, 1, 1.5, 2, 4, 6, 8, 12, 24 hours), Day 2, 3, 4, 5, 6, 7, 8, 15, 22, 29, 36, 43, 50, 57

• Metabolite to Parent Drug Ratio for Cmax of JNJ-56021927

  Metabolite to parent drug ratio for maximum observed plasma concentration.

  Pre-dose, and post-dose Day 1 (0.5, 1, 1.5, 2, 4, 6, 8, 12, 24 hours), Day 2, 3, 4, 5, 6, 7, 8, 15, 22, 29, 36, 43, 50, 57

• Metabolite to Parent Drug Ratio for AUClast of JNJ-56021927

  Metabolite to parent drug ratio for area under the plasma concentration time curve from time 0 to time of the last observed quantifiable concentration (Clast).

  Pre-dose, and post-dose Day 1 (0.5, 1, 1.5, 2, 4, 6, 8, 12, 24 hours), Day 2, 3, 4, 5, 6, 7, 8, 15, 22, 29, 36, 43, 50, 57

• Metabolite to Parent Drug Ratio for AUCinfinity of JNJ-56021927

  Metabolite to parent drug ratio for area under the plasma concentration time curve from time 0 to infinite time, calculated as the sum of AUClast and Clast/ first-order rate constant, in which Clast is the last observed quantifiable concentration.

  Pre-dose, and post-dose Day 1 (0.5, 1, 1.5, 2, 4, 6, 8, 12, 24 hours), Day 2, 3, 4, 5, 6, 7, 8, 15, 22, 29, 36, 43, 50, 57

• Number of Participants With Adverse Events as a Measure of Safety and Tolerabilty

  Up to Day 57

Study Arms (8)

Treatment A

ACTIVE COMPARATOR

15 participants will receive 240-mg dose as Softgel Capsule Formulation of JNJ-56021927.

Drug: JNJ-56021927 capsule

Treatment B

EXPERIMENTAL

15 participants will receive 240-mg dose as Tablet Formulation number 1 of JNJ-56021927.

Drug: JNJ-56021927 tablet

Treatment C

EXPERIMENTAL

15 participants will receive 240-mg dose as Tablet Formulation number 2 of JNJ-56021927.

Drug: JNJ-56021927 tablet

Treatment D

EXPERIMENTAL

15 participants will receive 240-mg dose as Tablet Formulation number 3 of JNJ-56021927.

Drug: JNJ-56021927 tablet

Treatment E

EXPERIMENTAL

15 participants will receive 240-mg dose as Tablet Formulation number 4 of JNJ-56021927.

Drug: JNJ-56021927 tablet

Treatment F

EXPERIMENTAL

15 participants will receive 240-mg dose as Tablet Formulation number 5 of JNJ-56021927.

Drug: JNJ-56021927 tablet

Treatment G

EXPERIMENTAL

15 participants will receive 240-mg dose as Tablet Formulation number 6 of JNJ-56021927.

Drug: JNJ-56021927 tablet

Treatment H

EXPERIMENTAL

15 participants will receive 240-mg dose as Tablet Formulation number 7 of JNJ-56021927.

Drug: JNJ-56021927 tablet

Interventions

JNJ-56021927 capsule DRUG

Participants will receive oral soft gel capsules providing a total dose of 240 mg JNJ-56021927 on Day 1.

Also known as: ARN-509

Treatment A

JNJ-56021927 tablet DRUG

Participants will receive oral tablets providing a total dose of 240 mg JNJ-56021927 on Day 1.

Treatment B; Treatment C; Treatment D; Treatment E; Treatment F; Treatment G; Treatment H

Eligibility Criteria

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

You may qualify if:

• During the study and for 3 months after receiving study medication, must agree to use an adequate contraception method (eg, vasectomy, double-barrier, partner using effective contraception), always use a condom during sexual intercourse and to not donate sperm
• Body mass index (weight \[kg\]/height \[m\]2) between 18 and 30 kg/m2 and body weight not less than 50 kg
• Blood pressure (after the participant is supine for 5 minutes) between 90 and 140 mmHg systolic, inclusive, and no higher than 90 mmHg diastolic
• A 12-lead electrocardiogram (ECG) consistent with normal cardiac conduction and function
• Non-smoker for 2 months prior to study participation

You may not qualify if:

• History of or current clinically significant medical illness including cardiac arrhythmias or other cardiac disease, hematologic disease, coagulation disorders, lipid abnormalities, significant pulmonary disease (including bronchospastic respiratory disease), diabetes mellitus, renal or hepatic insufficiency, thyroid disease, neurologic or psychiatric disease, and infection
• Clinically significant abnormal values for hematology, clinical chemistry or urinalysis, physical examination, vital signs or 12-lead ECG at screening or at admission to the study center as deemed appropriate by the investigator
• Presence of sexual dysfunction (eg, abnormal libido or erectile dysfunction) or any medical condition that would affect sexual function
• Use of any prescription or nonprescription medication (including vitamins and herbal supplements), except for acetaminophen within 14 days before the first dose of the study drug is scheduled
• History of clinically significant allergies or known hypersensitivity to vitamin E

Sponsors & Collaborators

• Aragon Pharmaceuticals, Inc.: lead

Study Sites (1)

Unknown Facility

Tempe, Arizona, United States

Location

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: January 7, 2014
• First Posted: January 9, 2014
• Study Start: December 1, 2013
• Primary Completion: April 1, 2014
• Study Completion: April 1, 2014
• Last Updated: October 20, 2016

Record last verified: 2016-10

Locations

US (1)