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A Open-Label Drug-Drug Interaction Study of Telotristat Etiprate and Midazolam in Healthy Subjects

Phase 1
Completed
Conditions
Drug Interactions
Interventions
Registration Number
NCT02147808
Lead Sponsor
Lexicon Pharmaceuticals
Brief Summary

This study is designed to evaluate the effects of telotristat ethyl on the pharmacokinetics of midazolam in healthy male and female subjects.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
24
Inclusion Criteria
  • Healthy adult males and females ≥18 to ≤55 years of age at Screening.
  • Body mass index ≥18.0 to ≤2.0 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
  • Willingness to adhere to the restrictions outlines 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
  • Receipt of any investigational agent or study drug within 30 days or 5 half-lives of study start
  • Receipt of any protein- or antibody-based therapeutic agent within 3 months of study start
  • Prior exposure to telotristat etiprate
  • Use of tobacco, smoking cessation products, or nicotine products within 3 months of study start
  • History of major surgery within 6 months of study start
  • History of acute narrow angle glaucoma
  • 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
  • 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 first dosing
  • 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
  • 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
  • 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
  • Use of any drugs or substances that are known to be substrates, inducers, or inhibitors of CYP3A4 within 30 days prior to the first dose

Study & Design

Study Type
INTERVENTIONAL
Study Design
SINGLE_GROUP
Arm && Interventions
GroupInterventionDescription
All subjectsTelotristat etiprateAll subjects will receive a single oral midazolam dose on Day 1 while fasting. Days 2 to 4 will be Washout days. On Day 5, subjects will begin a 5-day regimen of telotristat etiprate. On Day 9, subjects will receive a morning dose of telotristat etiprate with a single dose of midazolam while fasting.
All subjectsMidazolamAll subjects will receive a single oral midazolam dose on Day 1 while fasting. Days 2 to 4 will be Washout days. On Day 5, subjects will begin a 5-day regimen of telotristat etiprate. On Day 9, subjects will receive a morning dose of telotristat etiprate with a single dose of midazolam while fasting.
Primary Outcome Measures
NameTimeMethod
Midazolam plasma concentration in combination with steady state telotristat etiprateDay 9
Secondary Outcome Measures
NameTimeMethod
Number of treatment emergent adverse events12 days

Trial Locations

Locations (1)

Lexicon Investigational Site

🇺🇸

Madison, Wisconsin, United States

Lexicon Investigational Site
🇺🇸Madison, Wisconsin, United States

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