Effect of Food on Pharmacokinetics of Obeticholic Acid (OCA)

Phase 1

Completed

• Conditions: Healthy
• Interventions: Drug: OCA 25 mg; Drug: OCA 10 mg

• Registration Number: NCT01914562
• Lead Sponsor: Intercept Pharmaceuticals

Brief Summary

This is an open label, randomized, balanced, single center, single dose, trial to assess the pharmacokinetic (PK) profile of OCA, glyco-OCA and tauro-OCA on an empty stomach (fasted condition) and following a high fat, high calorie meal (fed condition) in a 2-period, 2-sequence, crossover manner.

Detailed Description

Not available

Study Timeline

• Study First Submitted: 2013-07-31
• Study First Submitted QC: 2013-07-31
• Study Start: 2013-08
• Study First Posted: 2013-08-02
• Primary Completion: 2013-11
• Study Completion: 2013-11
• Status Verified: 2014-08
• Last Update Submitted: 2014-08-07
• Last Update Posted: 2014-08-08

Recruitment & Eligibility

• Status: COMPLETED
• Sex: All
• Target Recruitment: 32

Inclusion Criteria

Subjects are required to meet the following criteria in order to be included in the trial.

1. Male or female subjects from 18 to 55 years

2. Contraception: Female subjects must be postmenopausal, surgically sterile, or if premenopausal, be prepared to use more than 1 effective (≤ 1% failure rate) method of contraception during the trial and until at least 30 days after the last dose of OCA. Effective methods of contraception are considered to be:

   1. Double barrier method, ie, (a) condom (male or female) with spermicide or (b) diaphragm with spermicide
   2. Intrauterine device (IUD)
   3. Vasectomy

3. Good general health as determined by medical history, and by results of physical examination, vital signs, electrocardiogram (ECG), and clinical laboratory tests obtained within 14 days prior to Day 0

4. Body mass index (BMI) of 18 to 28; BMI is determined by the following equation: BMI = weight/height2 (kg/m2).

5. Willing to abstain from alcohol, caffeine, and xanthine-containing food and beverages for 72 hours prior to each period check in and during participation of the inpatient periods of the trial

6. Willing and able to give written informed consent

Exclusion Criteria

Subjects meeting the following criteria will be excluded from the trial.

1. Prior participation in a clinical trial of OCA (INT-747; 6-ECDCA)
2. History or presence of any disease or condition known to interfere with the absorption, distribution, metabolism, or excretion of drugs including bile salt metabolism in the large intestine, eg, inflammatory bowel disease
3. History of gastrointestinal surgeries or gall bladder removal (cholecystectomy)
4. History or presence of a clinically significant cardiovascular, hepatic, diabetic, gastrointestinal, metabolic, neurologic, pulmonary, endocrine, psychiatric, or neoplastic disorder(s)
5. History of known or suspected clinically significant hypersensitivity to any drug, aside from penicillin
6. Ingestion of a prescription medication within 14 days prior to Day 0 or ingestion of an over the counter medication within 7 days prior to Day 0
7. Participation in radiologic examinations involving parenteral administration of iodinated contrast materials within 2 weeks prior to screening, or subsequently, through the end of trial participation
8. History or presence of alcohol abuse (defined as consumption of more than 210 mL of alcohol per week; or the equivalent of fourteen 4 ounces (oz) glasses of wine, or fourteen 12 oz cans/bottles of beer or wine coolers per week)
9. History or presence of substance abuse within the past 2 years or positive drug screen tests
10. Smoker or user of tobacco or nicotine products
11. Any screening laboratory test for which the results are not within the normal reference range and considered clinically significant
12. Participation in another investigational drug trial within 30 days prior to Day 0
13. History of noncompliance to medical regimens, or subjects who are considered to be potentially unreliable
14. Blood or plasma donation within 30 days prior to Day 0
15. Mental instability or incompetence
16. Presence of human immunodeficiency virus (HIV), hepatitis C virus (HCV) or hepatitis B virus (HBV) at screening

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: CROSSOVER

Arm && Interventions

Group	Intervention	Description
OCA 25 mg while Fed	OCA 25 mg	OCA 25 mg orally in the fed state
OCA 10 mg while Fed	OCA 10 mg	OCA 10 mg orally in the fed state
OCA 25 mg while fasted	OCA 25 mg	OCA 25 mg orally in the fasting state
OCA 10 mg while fasted	OCA 10 mg	OCA 10 mg orally in the fasting state

Primary Outcome Measures

Name	Time	Method
Time to maximum concentration (Tmax)	24 hours	Time to maximum concentration
Maximum concentration (Cmax) - fed and fasted	Day 1 and Day 14: 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, and 14 hours	maximum concentration (observed)
Area under the concentration versus time (AUCt)	216 hours	Area under the concentration versus time curve from time 0 to the last sampling time with measurable analyte concentration.
Area under the concentration versus time curve from 0 to 24 hours (AUC 0-24)	24 hours	Area under the concentration versus time curve from 0 to 24 hours with measurable analyte concentration

Trial Locations

Locations (1)

Celerion, Inc.; 🇺🇸 Tempe, Arizona, United States