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

Aragon Pharmaceuticals

Status and phase: Completed; Phase 1

Conditions: Healthy

Treatments: Drug: ARN-509

Study type: Interventional

Funder types: Industry

Identifiers

NCT01822041

ARN-509-006

2012-004899-19 (EudraCT Number)

Details and patient eligibility

About

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).

Full 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.

Enrollment: 12 patients

Sex: Male

Ages: 50 to 80 years old

Volunteers: Accepts Healthy Volunteers

Inclusion and exclusion criteria

Key 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.

Trial design

Primary purpose: Treatment

Allocation: Non-Randomized

Interventional model: Parallel Assignment

Masking: None (Open label)

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12 participants in 2 patient groups

Part A - 14C labeled ARN-509

Active Comparator group

Description:

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

Treatment:

Drug: ARN-509

Part B: 14C labeled ARN-509

Active Comparator group

Description:

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

Treatment:

Drug: ARN-509