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

14C-ARN-509 Microdose Absolute Bioavailability and Microtracer Absorption, Metabolism, and Excretion Study in Healthy Volunteers

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).

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: ARN-509

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 Type: Interventional
• Enrollment (Actual): 12
• Phase: Phase 1

Contacts and Locations

Study Locations

• Netherlands
  • Groningen, Netherlands
    • PRA - Clinical Research Unit, University Medical Centre Groningen

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 50 years to 80 years (ADULT, OLDER_ADULT)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

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.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: TREATMENT
• Allocation: NON_RANDOMIZED
• Interventional Model: PARALLEL
• Masking: NONE

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
ACTIVE_COMPARATOR: Part A - 14C labeled 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	Drug: ARN-509; Single oral dose of 240 mg ARN-509
ACTIVE_COMPARATOR: Part B: 14C labeled 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	Drug: ARN-509; Single oral dose of 240 mg ARN-509

What is the study measuring?

Primary Outcome Measures

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

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Metabolite Profile	To identify and quantify the ARN-509 metabolites in plasma, urine, and feces	2 months 10 days

Collaborators and Investigators

• Sponsor: Aragon Pharmaceuticals, Inc.
• Investigators: Principal Investigator: Nada al Kotbi, MD, PRA International Group BV; Study Director: Helen Pruim-Tait, MA, MSc, PRA International Group BV

Study record dates

Study Major Dates

• Study Start: March 1, 2013
• Primary Completion (ACTUAL): June 1, 2013
• Study Completion (ACTUAL): June 1, 2013

Study Registration Dates

• First Submitted: February 26, 2013
• First Submitted That Met QC Criteria: March 27, 2013
• First Posted (ESTIMATE): April 2, 2013

Study Record Updates

• Last Update Posted (ESTIMATE): September 13, 2013
• Last Update Submitted That Met QC Criteria: September 12, 2013
• Last Verified: September 1, 2013

More Information

Terms related to this study

• Keywords: Pharmacokinetics; healthy volunteers; mass balance study
• Other Study ID Numbers: ARN-509-006; 2012-004899-19 (EUDRACT_NUMBER)