An Open-Label Food Effect Study of Telotristat Etiprate

Study Overview
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Brief Summary
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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.

Official Title
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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

Conditions
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Healthy

Intervention / Treatment
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* Drug: Telotristat etiprate
* Drug: Telotristat etiprate


Participation Criteria
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Eligibility Criteria
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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

Ages Eligible for Study
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Minimum Age: 18 Years
Maximum Age: 55 Years

Sexes Eligible for Study
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All

Accepts Healthy Volunteers
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Accepts Healthy Volunteers

Study Plan
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How is the study designed?
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Design Details

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


Arms and Interventions

| Participant Group/Arm | Intervention/Treatment |
| --- | --- |
| Experimental: Treatment A<br>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<br>* 2 × 250 mg (as free base) telotristat etiprate tablets (fed conditions /high-fat / high caloric meal)<br>|
| Experimental: Treatment B<br>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<br>* 2 × 250 mg (as free base) telotristat etiprate tablets (fasted conditions)<br>|

What is the study measuring?
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Primary Outcome Measures

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