14C-ARN-509 Microtracer Label AME and Absolute BA Study

Phase 1

Completed

• Conditions: Healthy
• Interventions: Drug: ARN-509

• Registration Number: NCT01822041
• Lead Sponsor: Aragon Pharmaceuticals, Inc.

Brief Summary

This is study in healthy human volunteers to determine the absorption, metabolism, and excretion (AME) profile of ARN-509 as well as its absolute oral bioavailability (BA).

Detailed Description

Two cohorts of 6 healthy volunteers will be enrolled for the AME and absolute BA parts, respectively. The dose for both cohorts is 240 mg. The expected exposure of the dose is 7-fold lower than the steady state reached in patients with castration-resistant prostate cancer.

Study Timeline

• Study First Submitted: 2013-02-26
• Study Start: 2013-03
• Study First Submitted QC: 2013-03-27
• Study First Posted: 2013-04-02
• Primary Completion: 2013-06
• Study Completion: 2013-06
• Status Verified: 2013-09
• Last Update Submitted: 2013-09-12
• Last Update Posted: 2013-09-13

Recruitment & Eligibility

• Status: COMPLETED
• Sex: Male
• Target Recruitment: 12

Inclusion Criteria

1. Gender : male
2. Age : 50 - 80 years, inclusive
3. Body Mass Index (BMI) : 18.5-30.0 kg/m2
4. Ability and willingness to abstain from alcohol, methylxanthine-containing beverages or food (coffee, tea, cola, chocolate, "power drinks"), grapefruit (juice) and tobacco products from 48 h prior to entry in the clinical research center until discharge
5. Medical history without major pathology

Key

Exclusion Criteria

1. Evidence of clinically relevant pathology.
2. Mental handicap.
3. History of relevant drug and/or food allergies.
4. Regular/routine treatment with non-topical medications within 30 days prior to entry into the clinical research center.
5. Smoking.
6. History of alcohol abuse or drug addiction (including soft drugs like cannabis products).
7. Use of concomitant medication, except for acetaminophen (paracetamol) and topical medications
8. Irregular defecation pattern (less than once per 2 days).
9. Positive drug screen (opiates, methadone, cocaine, amphetamines, cannabinoids, barbiturates, benzodiazepines, and alcohol).
10. Intake of more than 24 units of alcohol per week (one unit of alcohol equals approximately 250 mL of beer, 100 mL of wine or 35 mL of spirits).
11. Positive screen on HBsAg, anti-HCV or anti-HIV 1/2.
12. Illness within five days prior to drug administration.

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: PARALLEL

Arm && Interventions

Group	Intervention	Description
Part A - 14C labeled ARN-509	ARN-509	Single oral dose of 240 mg ARN-509, followed after 2 hours (at the average tmax of ARN-509) by an intravenous (i.v.) microdose of 100 μg (9.25 kBq, 250 nCi) 14C-ARN-509
Part B: 14C labeled ARN-509	ARN-509	Single oral dose of 240 mg ARN-509, followed after 2 hours (at the average tmax of ARN-509) by an oral dose of 240 mg ARN-509 with 37 kBq (1000 nCi) of 14C-ARN-509

Primary Outcome Measures

Name	Time	Method
Mass Balance	2 months 10 days	To determine the rate and routes of excretion of ARN-509 in urine, feces, and expired air
Absolute Oral Bioavailability	2 months 10 days	To determine absolute oral bioavailability of ARN-509

Secondary Outcome Measures

Name	Time	Method
Metabolite Profile	2 months 10 days	To identify and quantify the ARN-509 metabolites in plasma, urine, and feces

Trial Locations

Locations (1)

PRA - Clinical Research Unit, University Medical Centre Groningen; 🇳🇱 Groningen, Netherlands