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

• Sponsor: Aragon Pharmaceuticals, Inc. (Industry)
• Overall Status: Completed
• CT.gov ID: NCT01822041
• Collaborator: (none)
• Enrollment: 12
• Location: 1
• Arms: 2
• Duration (Months): 3
• Patients Per Site Per Month: 4

Study Details

Study Description

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).

Condition or Disease	Intervention/Treatment	Phase
Healthy	Drug: ARN-509	Phase 1

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 Design

• Study Type: Interventional
• Actual Enrollment: 12 participants
• Allocation: Non-Randomized
• Intervention Model: Parallel Assignment
• Masking: None (Open Label)
• Primary Purpose: Treatment
• Official Title: 14C-ARN-509 Microdose Absolute Bioavailability and Microtracer Absorption, Metabolism, and Excretion Study in Healthy Volunteers
• Study Start Date: Mar 1, 2013
• Actual Primary Completion Date: Jun 1, 2013
• Actual Study Completion Date: Jun 1, 2013

Arms and Interventions

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

Outcome Measures

Primary Outcome Measures

1. Mass Balance [2 months 10 days]

   To determine the rate and routes of excretion of ARN-509 in urine, feces, and expired air

2. Absolute Oral Bioavailability [2 months 10 days]

   To determine absolute oral bioavailability of ARN-509

Secondary Outcome Measures

1. Metabolite Profile [2 months 10 days]

   To identify and quantify the ARN-509 metabolites in plasma, urine, and feces

Eligibility Criteria

Criteria

• Ages Eligible for Study: 50 Years to 80 Years
• Sexes Eligible for Study: Male
• Accepts Healthy Volunteers: Yes

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.

Contacts and Locations

Locations

	Site	City	State	Country	Postal Code
1	PRA - Clinical Research Unit, University Medical Centre Groningen	Groningen		Netherlands

Sponsors and Collaborators

• 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 Documents (Full-Text)

None provided.

More Information

Publications

None provided.

• Responsible Party: Aragon Pharmaceuticals, Inc.
• ClinicalTrials.gov Identifier: NCT01822041
• Other Study ID Numbers: ARN-509-006; 2012-004899-19
• First Posted: Apr 2, 2013
• Last Update Posted: Sep 13, 2013
• Last Verified: Sep 1, 2013

• Keywords provided by Aragon Pharmaceuticals, Inc.: healthy volunteers; mass balance study; Pharmacokinetics

Study Results

No Results Posted as of Sep 13, 2013