An Open-Label Food Effect Study of Telotristat Etiprate

Phase 1

Completed

• Conditions: Healthy
• Interventions: Drug: Telotristat etiprate

• Registration Number: NCT02157584
• Lead Sponsor: Lexicon Pharmaceuticals

Brief Summary

This study is designed to evaluate the effect of food on the pharmacokinetics (PK) of telotristat ethyl and its metabolite LP-778902 relative to administration of single dose telotristat etiprate in the fasted state in healthy adult male and female subjects.

Detailed Description

Not available

Study Timeline

• Study Start: 2014-06
• Study First Submitted: 2014-06-04
• Study First Submitted QC: 2014-06-05
• Study First Posted: 2014-06-06
• Primary Completion: 2014-07
• Status Verified: 2014-09
• Last Update Submitted: 2014-09-05
• Last Update Posted: 2014-09-08

Recruitment & Eligibility

• Status: COMPLETED
• Sex: All
• Target Recruitment: 22

Inclusion Criteria

• Healthy adult subjects aged ≥18 to ≤55 years of age at screening
• Body mass index ≥18.0 to ≤32.0 kg/m^2
• Acceptable vital signs at Screening: Systolic blood pressure = 90-140 mm Hg, Diastolic blood pressure = 50-90 mm Hg, Heart rate = 40-100 beats per minute
• Able and willing to ingest an entire high fat/high caloric breakfast meal within 30 minutes
• Willingness to adhere to the restrictions outlined in the protocol
• Able to comprehend and sign the Informed Consent Form

Exclusion Criteria

• Presence of any clinically significant physical, laboratory, or ECG finding that may interfere with the study in the opinion of the Investigator
• Use of any medications, herbal tea, energy drink, herbal products, or supplements within 14 days of study start
• Receipt of any investigational agent or study drug within 30 days or 5 half-lives prior to Screening
• Receipt of any protein- or antibody-based therapeutic agent within 3 months prior to Screening
• Prior exposure to telotristat etiprate
• Use of tobacco, smoking cessation products, or nicotine products within 3 months prior to Screening
• History of major surgery within 6 months prior to Screening
• History of any GI surgery that may induce malabsorption
• History of renal disease, or significantly abnormal glomerular filtration rate (<90 mL/min as calculated using the Cockcroft-Gault equation) at Screening
• History of hepatic disease, or significantly abnormal liver function tests at Screening
• History of any clinically significant psychiatric, renal, hepatic, pancreatic, cardiovascular, neurological, endocrinologic, hematological, or GI abnormality
• History of any active infection within 14 days prior to Screening
• History of alcohol or substance abuse within 2 years prior to Screening
• Positive hepatitis panel (including hepatitis B surface antigen and hepatitis C virus antibody) or positive human immunodeficiency virus antibody screens
• Concurrent conditions that could interfere with safety and/or tolerability measurements
• Donation or loss of >500 mL of blood or blood product within 3 months prior to Screening
• Women who are breastfeeding or are planning to become pregnant during the study
• Positive serum pregnancy test (females only)
• Positive urine screen for selected drugs of abuse and cotinine
• Consumption of alcohol within 48 hours prior to study start
• Consumption of caffeine- and/or xanthine-containing products within 72 hours of study start
• Consumption of grapefruit, Seville oranges, and grapefruit- or Seville orange-containing products within 72 hours prior to study start
• Unable or unwilling to communicate or cooperate with the Investigator for any reason

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: CROSSOVER

Arm && Interventions

Group	Intervention	Description
Treatment B	Telotristat etiprate	Subjects will receive a single 500 mg (as free base) dose of telotristat etiprate (as 2 × 250 mg tablets) on Day 1 in a fasted condition. Days 2 to 5 will be Washout Days. On Day 6, subjects will receive a single 500 mg (as free base) dose of telotristat etiprate (as 2 × 250 mg tablets) 1 in a fed condition.
Treatment A	Telotristat etiprate	Subjects will receive a single 500 mg (as free base) dose of telotristat etiprate (as 2 × 250 mg tablets) on Day 1 in a fed condition. Days 2 to 5 will be Washout Days. On Day 6, subjects will receive a single 500 mg (as free base) dose of telotristat etiprate (as 2 × 250 mg tablets) 1 in a fasted condition.

Primary Outcome Measures

Name	Time	Method
Plasma concentrations of telotristat ethyl	Days 1, 2, 3, 6, 7, 8
Plasma concentration of metabolite LP-778902	Days 1, 2, 3, 6, 7, 8

Secondary Outcome Measures

Name	Time	Method
Number of treatment emergent adverse events	10 days

Trial Locations

Locations (1)

Lexicon Investigational Site; 🇺🇸 Madison, Wisconsin, United States