An Open-Label Food Effect Study of Telotristat Etiprate

A Phase 1, Randomized, Single Center, Open Label, 2 Sequence, 2 Period, Crossover Study to Evaluate the Effect of Food on the Single Dose Pharmacokinetics of Telotristat Etiprate (LX1606 Hippurate) in Healthy Male and Female Subjects

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.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: Telotristat etiprate; Drug: Telotristat etiprate

• Study Type: Interventional
• Enrollment (Actual): 22
• Phase: Phase 1

Contacts and Locations

Study Locations

• United States
  • Wisconsin
    • Madison, Wisconsin, United States, 53704
      • Lexicon Investigational Site

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 55 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: All

Description

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 Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Treatment A; 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.	Drug: Telotristat etiprate; 2 × 250 mg (as free base) telotristat etiprate tablets (fed conditions /high-fat / high caloric meal); Drug: Telotristat etiprate; 2 × 250 mg (as free base) telotristat etiprate tablets (fasted conditions)
Experimental: Treatment B; 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.	Drug: Telotristat etiprate; 2 × 250 mg (as free base) telotristat etiprate tablets (fed conditions /high-fat / high caloric meal); Drug: Telotristat etiprate; 2 × 250 mg (as free base) telotristat etiprate tablets (fasted conditions)

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
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

Outcome Measure	Time Frame
Number of treatment emergent adverse events	10 days

Collaborators and Investigators

• Sponsor: Lexicon Pharmaceuticals

Study record dates

Study Major Dates

• Study Start: June 1, 2014
• Primary Completion (Actual): July 1, 2014

Study Registration Dates

• First Submitted: June 4, 2014
• First Submitted That Met QC Criteria: June 5, 2014
• First Posted (Estimate): June 6, 2014

Study Record Updates

• Last Update Posted (Estimate): September 8, 2014
• Last Update Submitted That Met QC Criteria: September 5, 2014
• Last Verified: September 1, 2014

More Information

Terms related to this study

• Other Study ID Numbers: LX1606.1-107-NRM; LX1606.107 (Other Identifier: Lexicon Pharmaceuticals, Inc.)