Clinical trial NCT02157584: An Open-Label Food Effect Study of Telotristat Etiprate
Official title: 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
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy
Lead sponsor: Lexicon Pharmaceuticals
Sponsor class: INDUSTRY
First posted: 2014-06-06
Enrollment: 22
Sex: ALL
Minimum age (years): 18
Maximum age (years): 55
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: RANDOMIZED
Intervention model: CROSSOVER
Primary purpose: TREATMENT

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.


Eligibility criteria: 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

Primary outcomes:
measure: Plasma concentrations of telotristat ethyl
timeFrame: Days 1, 2, 3, 6, 7, 8
measure: Plasma concentration of metabolite LP-778902
timeFrame: Days 1, 2, 3, 6, 7, 8
Secondary outcomes:
measure: Number of treatment emergent adverse events
timeFrame: 10 days
Other outcomes:
Locations:
city: Madison
country: United States
facility: Lexicon Investigational Site
state: Wisconsin
Study officials:
affiliation: Lexicon Pharmaceuticals, Inc.
name: Suman Wason, MD
role: STUDY_DIRECTOR
References: