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

This study has been completed.
Sponsor:
Information provided by (Responsible Party):
Tioga Pharmaceuticals
ClinicalTrials.gov Identifier:
NCT01380561
First received: June 13, 2011
Last updated: October 14, 2011
Last verified: October 2011
  Purpose

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


Condition Intervention Phase
Healthy
Drug: asimadoline
Phase 1

Study Type: Interventional
Study Design: Allocation: Non-Randomized
Endpoint Classification: Pharmacokinetics Study
Intervention Model: Single Group Assignment
Masking: 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

Further study details as provided by Tioga Pharmaceuticals:

Primary Outcome Measures:
  • Amount of [14C]derived radioactivity in urine and feces after a single oral dose of [14C]asimadoline [ Time Frame: up to 1 month ] [ Designated as safety issue: No ]
  • Concentration of metabolites of asimadoline in plasma, urine, and feces after single and multiple oral doses of asimadoline. [ Time Frame: up to 1 month ] [ Designated as safety issue: No ]

Secondary Outcome Measures:
  • Determination of plasma pharmacokinetics (e.g., Cmax, AUC, tmax, t1/2) of asimadoline and major metabolites [ Time Frame: up to 1 month ] [ Designated as safety issue: No ]
  • Number of subjects with adverse events [ Time Frame: up to 1 month ] [ Designated as safety issue: No ]

Enrollment: 6
Study Start Date: June 2011
Study Completion Date: July 2011
Primary Completion Date: July 2011 (Final data collection date for primary outcome measure)
Arms Assigned Interventions
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

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.

  Eligibility

Ages Eligible for Study:   18 Years to 56 Years
Genders Eligible for Study:   Male
Accepts Healthy Volunteers:   Yes
Criteria

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
  Contacts and Locations
Please refer to this study by its ClinicalTrials.gov identifier: NCT01380561

Locations
United States, Kansas
Quintiles Phase 1 Unit
Overland Park, Kansas, United States, 66211
Sponsors and Collaborators
Tioga Pharmaceuticals
Investigators
Principal Investigator: Dr. Philip Leese Quintiles Phase 1 Unit
  More Information

No publications provided

Responsible Party: Tioga Pharmaceuticals
ClinicalTrials.gov Identifier: NCT01380561     History of Changes
Other Study ID Numbers: ASMP1001
Study First Received: June 13, 2011
Last Updated: October 14, 2011
Health Authority: United States: Food and Drug Administration

Keywords provided by Tioga Pharmaceuticals:
asimadoline
pharmacokinetic
excretion of 14C-derived radioactivity
metabolite profile
14C-asimadoline
metabolites
single and multiple oral doses

ClinicalTrials.gov processed this record on April 14, 2014