A Metabolite Identification, Mass Balance, and PK Study of [14C]-Asimadoline to Healthy Adult Male Volunteers

Sponsor

Tioga Pharmaceuticals (Industry)

Overall Status

Completed

CT.gov ID

NCT01380561

Collaborator

(none)

Enrollment

Location

Arm

Duration (Days)

6.1

Patients Per Site Per Month

Study Details

Study Description

Brief Summary

This is an open label, single center, metabolite identification, mass balance, and PK study in healthy male volunteers.

Condition or Disease	Intervention/Treatment	Phase
Healthy	Drug: asimadoline	Phase 1

Detailed Description

This is an open label, single center, metabolite identification, mass balance, and PK study in healthy male volunteers. The purposes of this study is to determine the excretion of total [14C] derived radioactivity and the metabolite profile after a single oral dose of [14C] asimadoline as well as to identify and quantitate the metabolites of asimadoline in plasma, urine, and feces after single and multiple oral doses of asimadoline.

Study Design

Study Type:

Interventional

Actual Enrollment :

6 participants

Allocation:

Non-Randomized

Intervention Model:

Single Group Assignment

Masking:

None (Open Label)

Primary Purpose:

Basic Science

Official Title:

A Metabolite Identification, Mass Balance, and Pharmacokinetic Study of a Single Oral Dose of [14C]-Asimadoline Followed by Twice Daily Oral Dosing of 0.5 mg Asimadoline to Healthy Adult Male Volunteers

Study Start Date :

Jun 1, 2011

Actual Primary Completion Date :

Jul 1, 2011

Actual Study Completion Date :

Jul 1, 2011

Arms and Interventions

Arm	Intervention/Treatment
Experimental: Single Arm Study asimadoline	Drug: asimadoline 10mg [14]C labelled asimadoline Day 1 then 7 doses 0.5 mg asimadoline bid beginning on Day 2 and ending on Day 5. Other Names: EMD 61 753 EMR 63 320

Arm

Intervention/Treatment

Experimental: Single Arm Study

asimadoline

Drug: asimadoline

10mg [14]C labelled asimadoline Day 1 then 7 doses 0.5 mg asimadoline bid beginning on Day 2 and ending on Day 5.

Other Names:

EMD 61 753

EMR 63 320

Outcome Measures

Primary Outcome Measures

Amount of [14C]derived radioactivity in urine and feces after a single oral dose of [14C]asimadoline [up to 1 month]
Concentration of metabolites of asimadoline in plasma, urine, and feces after single and multiple oral doses of asimadoline. [up to 1 month]

Secondary Outcome Measures

Determination of plasma pharmacokinetics (e.g., Cmax, AUC, tmax, t1/2) of asimadoline and major metabolites [up to 1 month]
Number of subjects with adverse events [up to 1 month]

Eligibility Criteria

Criteria

Ages Eligible for Study:

18 Years to 56 Years

Sexes Eligible for Study:

Male

Accepts Healthy Volunteers:

Yes

Inclusion Criteria:

Be informed of the nature of the study and have provided written informed voluntary consent
Be healthy males, at least 18 years of age or the legal age of consent (whichever is greater) and less than 56 years of age
Have a body mass index (BMI) >=18.0 and <32.0 kg/m2 and weigh at least 50 kg
Be in good general health with no clinically relevant abnormalities based on the medical history, physical examination, clinical laboratory evaluations (hematology, clinical chemistry, urinalysis), and 12 lead electrocardiogram (ECG) that, in the opinion of the Investigator, would affect subject safety
Agree to comply with the study procedures and restrictions.

Exclusion Criteria:

Any disease or condition that might affect drug absorption, metabolism, or excretion, or clinically significant cardiovascular, hematological, renal, hepatic, pulmonary, endocrine, gastrointestinal, immunological, dermatological, neurological, or psychiatric disease
Receipt of a radioisotope with an effective half-life of 30 days or more within the previous 12 months
Receipt of any diagnostic radiation procedures with an effective dose exceeding 1 rem in their lifetime
Occupational exposure to radiation (e.g., those routinely required to wear a radiation monitoring badge)
Receipt of any radiation treatments/therapy
History of constipation or infrequent bowel movements (<=6 bowel movements per week on average)
Known or suspected hypersensitivity or allergic reaction to asimadoline or similar chemical compounds or any of the components of asimadoline tablets
Chronic use of any systemic medications (with the exception of vitamins taken at standard supplement doses); use of a drug therapy (including herbal preparations, e.g., St. John's wort) known to induce or inhibit hepatic drug metabolism within 30 days before the first dose of study medication; use of prescription medication within 14 days before administration of study medication or over-the-counter products (including natural products) within 7 days before administration of study medication, except for topical products without systemic absorption, unless approved by the Sponsor
Have smoked cigarettes or used nicotine-containing products over the last 3 months and not able to abstain from smoking for the duration of the confinement period
If not sterile, cannot agree to use one of the following approved methods of contraception, from check-in until 3 months following Study Completion/Clinic Discharge: a male condom with spermicide; a sterile sexual partner; use by a female sexual partner of an intrauterine device with spermicide; a female condom with spermicide; contraceptive sponge with spermicide; a cervical cap with spermicide; or oral, implantable, transdermal, or injectable contraceptives with a reliable secondary back-up method
Current history or evidence of drug or alcohol abuse or a positive screen for substances of abuse or alcohol at screening or admission
Positive screen for hepatitis B surface antigen (HBsAg), hepatitis C antibody, or human immunodeficiency virus (HIV) antibody
Receipt of an investigational product or device, or participation in a drug research study within a period of 30 days (or 5 half lives of the drug, whichever is longer) before the first dose of study medication
Blood loss or blood donation of >550 mL within 90 days or plasma donation >500 mL within 30 days before administration of study drug
Any food allergy, intolerance, restriction, or special diet that, in the opinion of the Investigator, should preclude the subject's participation in this study