An Open-label Study to Evaluate the Absorption, Metabolism, and Excretion of [14C]-Telotristat Etiprate in Males (LX1606-104)

This study has been completed.
Information provided by (Responsible Party):
Lexicon Pharmaceuticals Identifier:
First received: August 27, 2013
Last updated: October 22, 2013
Last verified: October 2013

To evaluate the metabolism and routes and extent of elimination of telotristat etiprate and its primary metabolite LX1033.

Condition Intervention Phase
Carcinoid Syndrome
Drug: 500 mg [14C]-LX1606
Phase 1

Study Type: Interventional
Study Design: Endpoint Classification: Pharmacokinetics Study
Intervention Model: Single Group Assignment
Masking: Open Label
Primary Purpose: Treatment
Official Title: A Phase 1, Open-label, Non-randomised, Single-dose Study to Evaluate the Absorption, Metabolism, and Excretion of [14C]-Telotristat Etiprate (LX1606) in Healthy Male Subjects

Resource links provided by NLM:

Further study details as provided by Lexicon Pharmaceuticals:

Primary Outcome Measures:
  • Maximum plasma concentration of LX1606 and LX1033 [ Time Frame: 7 days ] [ Designated as safety issue: No ]

Secondary Outcome Measures:
  • Time to maximum plasma concentration of and LX1033 [ Time Frame: 7 days ] [ Designated as safety issue: No ]
  • Determination of total radioactivity in blood and plasma [ Time Frame: 7 days ] [ Designated as safety issue: No ]
  • Mass balance recovery of total radioactivity in urine and feces [ Time Frame: 7 days ] [ Designated as safety issue: No ]
  • Metabolite profiling and identification in plasma [ Time Frame: 7 days ] [ Designated as safety issue: No ]
  • Metabolic profiling and identification in urine [ Time Frame: 7 days ] [ Designated as safety issue: No ]
  • Metabolic profiling and identification in feces [ Time Frame: 7 days ] [ Designated as safety issue: No ]

Enrollment: 8
Study Start Date: August 2013
Primary Completion Date: September 2013 (Final data collection date for primary outcome measure)
Arms Assigned Interventions
Experimental: 500 mg LX606
All subjects will receive a single oral 500 mg dose of [14C]-LX1606.
Drug: 500 mg [14C]-LX1606
500 mg dose of LX1606 containing a target dose of 3.32 Megabecquerel (MBq) of radiation as [14C]-LX1606.


Ages Eligible for Study:   30 Years to 65 Years
Genders Eligible for Study:   Male
Accepts Healthy Volunteers:   Yes

Inclusion Criteria:

  • Healthy male subjects aged 30 to 65 years of age.
  • Male subjects and their partners must agree to use an adequate method of contraception
  • Historically able to produce a minimum of 1 bowel movement every day on most days

Exclusion Criteria:

  • Female subjects
  • Use of any medication or supplement within 5 days prior to Dosing
  • Radiation exposure exceeding 5 millisieverts (mSv) in the last 12 months or 10 mSv in the last 5 years
  • Current smokers or the use of cigarettes within 90 days prior to Screening
  • History or renal disease or abnormal kidney function
  • History of hepatic disease
  • Acute diarrhea or constipation within 7 days of dosing
  • Positive urine glucose at Screening
  Contacts and Locations
Please refer to this study by its identifier: NCT01932528

United Kingdom
Lexicon Investigational Site
Nottingham, United Kingdom, NG11 6JS
Sponsors and Collaborators
Lexicon Pharmaceuticals
Study Director: Doug Fleming, MD Lexicon Pharmaceuticals, Inc.
  More Information

No publications provided

Responsible Party: Lexicon Pharmaceuticals Identifier: NCT01932528     History of Changes
Other Study ID Numbers: LX1606.1-104-NRM
Study First Received: August 27, 2013
Last Updated: October 22, 2013
Health Authority: United Kingdom: Medicines and Healthcare Products Regulatory Agency
United States: Food and Drug Administration

Keywords provided by Lexicon Pharmaceuticals:

Additional relevant MeSH terms:
Malignant Carcinoid Syndrome
Serotonin Syndrome
Carcinoid Tumor
Neuroendocrine Tumors
Neuroectodermal Tumors
Neoplasms, Germ Cell and Embryonal
Neoplasms by Histologic Type
Neoplasms, Glandular and Epithelial
Neoplasms, Nerve Tissue
Drug Toxicity
Substance-Related Disorders processed this record on April 16, 2014