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Study of Telotristat Etiprate (LX1606) in Participants With Symptomatic Carcinoid Syndrome Not Managed by Stable-Dose Octreotide Therapy

Phase 2
Completed
Conditions
Carcinoid Syndrome
Interventions
Registration Number
NCT00853047
Lead Sponsor
Lexicon Pharmaceuticals
Brief Summary

The purpose of this study is to evaluate the safety and tolerability of telotristat etiprate (LX1606) versus a placebo control in participants with symptomatic carcinoid syndrome not managed by stable-dose long-acting octreotide therapy. Following determination of the maximally tolerated or effective dose, cohort expansion will occur to confirm effect on symptoms and safety profile.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
23
Inclusion Criteria
  • Males and females, aged 18 and older
  • Biopsy-proven metastatic carcinoid tumor of the gastrointestinal (GI) tract with disease extent confirmed by computed tomography (CT), magnetic resonance imaging (MRI), or radionuclide imaging
  • Symptoms not managed by stable-dose long-acting octreotide therapy (≥4 bowel movements per day)
  • Ability to provide written informed consent
Exclusion Criteria
  • ≥12 high volume, watery bowel movements per day associated with a clinical syndrome of volume contraction, dehydration, or hypotension compatible with a "pancreatic cholera"-type clinical syndrome
  • Sponsor-unacceptable clinical laboratory values for hematology and liver function tests at screening
  • Karnofsky status ≤70% - unable to care for self
  • Surgery within 60 days prior to screening
  • A history of short bowel syndrome
  • Life expectancy <12 months
  • History of substance or alcohol abuse within 2 years prior to screening
  • Previous exposure to a tryptophan hydroxylase (TPH) inhibitor
  • Administration of any investigational drug within 30 days of screening or any therapeutic protein or antibody within 90 days of screening

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Telotristat Etiprate 150 mg Core PhaseTelotristat etiprateTelotristat etiprate capsules,150 mg orally 3 times daily for 28 days in the double-blind treatment period (core phase) in combination with stable-dose octreotide long-acting release (LAR) depot therapy given once per month. Upon completion of 28-days of treatment, participants were eligible to enter the optional open-label extension period.
Telotristat Etiprate 250 mg Core PhaseOctreotide LAR DepotTelotristat etiprate capsules, 250 mg orally 3 times daily for 28 days in the double-blind treatment period in combination with stable-dose octreotide LAR depot therapy given once per month. Upon completion of 28-days of treatment, participants were eligible to enter the optional open-label extension period.
Telotristat Etiprate 350 mg Core PhaseOctreotide LAR DepotTelotristat etiprate capsules, 350 mg orally 3 times daily for 28 days in the double-blind treatment period in combination with stable-dose octreotide LAR depot therapy given once per month. Upon completion of 28-days of treatment, participants were eligible to enter the optional open-label extension period.
Telotristat Etiprate 500 mg Core PhaseOctreotide LAR DepotTelotristat etiprate capsules, 500 mg orally 3 times daily for 28 days in the double-blind treatment period in combination with a stable-dose octreotide LAR depot therapy given once per month. Upon completion of 28-days of treatment, participants were eligible to enter the optional open-label extension period.
Placebo Core PhasePlaceboPlacebo-matching telotristat etiprate capsules, orally 3 times daily for 28 days in the double-blind treatment period in combination with stable-dose octreotide LAR depot therapy given once per month. Upon completion of 28-days of treatment, participants were eligible to receive telotristat etiprate in the optional open-label extension period.
Telotristat Etiprate 250 mg Core PhaseTelotristat etiprateTelotristat etiprate capsules, 250 mg orally 3 times daily for 28 days in the double-blind treatment period in combination with stable-dose octreotide LAR depot therapy given once per month. Upon completion of 28-days of treatment, participants were eligible to enter the optional open-label extension period.
Telotristat Etiprate 350 mg Core PhaseTelotristat etiprateTelotristat etiprate capsules, 350 mg orally 3 times daily for 28 days in the double-blind treatment period in combination with stable-dose octreotide LAR depot therapy given once per month. Upon completion of 28-days of treatment, participants were eligible to enter the optional open-label extension period.
Telotristat Etiprate 500 mg Core PhaseTelotristat etiprateTelotristat etiprate capsules, 500 mg orally 3 times daily for 28 days in the double-blind treatment period in combination with a stable-dose octreotide LAR depot therapy given once per month. Upon completion of 28-days of treatment, participants were eligible to enter the optional open-label extension period.
Telotristat Etiprate Open-Label Extension PhaseTelotristat etiprateTelotristat etiprate at assigned dose level for 8 weeks in combination with stable-dose octreotide LAR depot therapy given once per month in the open-label extension period. Upon completion of the 8-week period, participants could enter an additional extension period of 172 weeks, receiving telotristat etiprate at the assigned dose or maximum tolerated dose (500 mg 3 times daily).
Telotristat Etiprate 150 mg Core PhaseOctreotide LAR DepotTelotristat etiprate capsules,150 mg orally 3 times daily for 28 days in the double-blind treatment period (core phase) in combination with stable-dose octreotide long-acting release (LAR) depot therapy given once per month. Upon completion of 28-days of treatment, participants were eligible to enter the optional open-label extension period.
Placebo Core PhaseOctreotide LAR DepotPlacebo-matching telotristat etiprate capsules, orally 3 times daily for 28 days in the double-blind treatment period in combination with stable-dose octreotide LAR depot therapy given once per month. Upon completion of 28-days of treatment, participants were eligible to receive telotristat etiprate in the optional open-label extension period.
Telotristat Etiprate Open-Label Extension PhaseOctreotide LAR DepotTelotristat etiprate at assigned dose level for 8 weeks in combination with stable-dose octreotide LAR depot therapy given once per month in the open-label extension period. Upon completion of the 8-week period, participants could enter an additional extension period of 172 weeks, receiving telotristat etiprate at the assigned dose or maximum tolerated dose (500 mg 3 times daily).
Primary Outcome Measures
NameTimeMethod
Number of Participants With Any Treatment-emergent Adverse Event (TEAE) and Any Drug-related TEAE in the Core PhaseUp to 4 Weeks Core Phase

An adverse event (AE) was defined as any untoward medical occurrence associated with the use of a drug in humans, whether or not considered drug-related. A TEAE was an AE reported after the first dose of randomized treatment on Day 1.

Number of Participants With Any TEAE in the Open-Label Extension PhaseUp to 180 weeks in the open-label extension phase

An AE was defined as any untoward medical occurrence associated with the use of a drug in humans, whether or not considered drug related. A TEAE was an AE reported after receiving treatment.

Secondary Outcome Measures
NameTimeMethod
Change From Baseline in Weekly Mean Stool FormBaseline to Week 4

Participants recorded stool form in a daily diary using a 6-point scale (0-none,1-hard, 2-firm, 3-soft, 4-loose, 5-watery). A negative change from Baseline indicates improvement.

Change From Baseline in Number of Cutaneous Flushing EpisodesBaseline to Week 4

Participants recorded the number of daily flushing episodes per day in a daily diary. The total number of flushing episodes per day were averaged over the 4-week period. A negative change from Baseline indicates improvement.

Number of Participants Reporting Improvement in the Subjective Global Assessment of Symptoms Associated With Carcinoid SyndromeWeek 4

Participants were asked to answer the following question: "In the past 7 days, have you had adequate relief of your carcinoid syndrome bowel complaints such as diarrhea, urgent need to have a bowel movement, abdominal pain, or discomfort?". The number of participants who answered Yes are reported.

Number of Participants Experiencing Complete Response at Week 4Baseline to Week 4

Complete Response to treatment was defined as one of the following: 1. Less than 4 bowel movements per day; or 2. A decrease in daily bowel movements that is ≥ 50% from baseline; or 3. A positive response to the global assessment question ("In the past 7 days, have you had adequate relief of your carcinoid syndrome bowel complaints such as diarrhea, urgent need to have a bowel movement, abdominal pain or discomfort?") for each of the last 2 weeks of the Treatment Period.

Change From Baseline in Mean Number of Bowel Movements (BMs) Per DayBaseline to Week 4

Participants recorded the number of BMs per day in a daily diary. The total number of BMs per day were averaged over the 4-week period. A negative change from Baseline indicates improvement.

Change From Baseline in Chromogranin ABaseline to Week 4

Blood samples were collected for assessment of Chromogranin A level. A negative change from Baseline indicates improvement.

Change From Baseline in Frequency of Rescue for Short-acting Octreotide Use/DayBaseline to Week 4

Participants recorded details (location and frequency of injection) of subcutaneous injections of rescue, short-acting octreotide, if taken, in the daily diary. A negative change from Baseline indicates improvement.

Time to First Rescue, Short-acting OctreotideBaseline to Week 4

Time to the first subcutaneous injections of rescue, short-acting octreotide was determined from the participant's daily diary.

Change From Baseline in Percentage of Days Per Week Experiencing a Sensation of Urgency to DefecateBaseline to Week 4

Participants recorded the sensation of urgency to defecate (Yes or No) in a daily diary. A negative change from Baseline indicates improvement.

Change From Baseline in Severity of Abdominal Pain or DiscomfortBaseline to Week 4

Participants recorded the severity of abdominal pain or discomfort in a daily diary assessed using a 4-point scale (0-none, 1-mild, 2-moderate, 3-severe). A negative change from Baseline indicates improvement.

Change From Baseline in Urinary 5-hydroxyindoleacetic Acid (u5-HIAA)Baseline to Week 4

u5-HIAA is a standard test used in clinical practice to assess the neuroendocrine tumor (NET) activity and is collected as a 24-hour urine specimen. A negative change from Baseline indicates improvement.

Trial Locations

Locations (9)

University of Iowa

🇺🇸

Iowa City, Iowa, United States

Texas Oncology - Weslaco

🇺🇸

Weslaco, Texas, United States

Nebraska Methodist Hospital

🇺🇸

Omaha, Nebraska, United States

UCSF Helen Diller Family Comprehensive Cancer Center

🇺🇸

San Francisco, California, United States

Hematology Oncology Services of Arkansas

🇺🇸

Little Rock, Arkansas, United States

St. Francis Medical Group Oncology and Hematology Specialists

🇺🇸

Indianapolis, Indiana, United States

UT M.D. Anderson Cancer Center

🇺🇸

Houston, Texas, United States

Texas Oncology - McAllen

🇺🇸

McAllen, Texas, United States

Dana Farber Cancer Institute

🇺🇸

Boston, Massachusetts, United States

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