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TELOTRISTAT ETIPRATE
Telotristat etiprate inhibits tryptophan hydroxylase, the rate-limiting enzyme in serotonin synthesis, thereby reducing serotonin levels in the body.
Telotristat etiprate is a serotonin synthesis inhibitor developed by Lexicon Pharmaceuticals for the treatment of carcinoid syndrome. It works by reducing the production of serotonin in the body, which can help manage symptoms such as flushing and diarrhea. The drug is approved for use in combination with somatostatin analogs in adults with carcinoid syndrome who have inadequately controlled symptoms. Despite its efficacy, telotristat etiprate has several side effects, including nausea, fatigue, and headache. The drug is not currently available as a generic, and it faces competition from other treatments for carcinoid syndrome.
At a glance
| Generic name | TELOTRISTAT ETIPRATE |
|---|---|
| Drug class | Serotonin Synthesis Inhibitor |
| Target | Tryptophan Hydroxylase-1 (TPH1) |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
| First approval | 2017 |
Mechanism of action
By inhibiting tryptophan hydroxylase, telotristat etiprate decreases the production of serotonin, which is often elevated in patients with carcinoid syndrome.
Approved indications
Common side effects
- Nausea
- Fatigue
- Headache
- Dizziness
- Decreased Appetite
- Constipation
- Abdominal Pain
Key clinical trials
- Telotristat Ethyl for the Treatment of Carcinoid Heart Disease in Patients With Metastatic Neuroendocrine Tumor (PHASE3)
- Telotristat Ethyl to Promote Weight Stability in Patients With Advanced Stage Pancreatic Cancer (PHASE2)
- AMT-PET in Monitoring Telotristat Etiprate Treatment in Participants With MetastaticNeuroendocrine Neoplasm (PHASE2)
- Real-world Evidence Study EvaLuating PAtient-Reported Outcomes With XERMELO
- Telotristat With Lutathera in Neuroendocrine Tumors (PHASE2)
- A Safety and Efficacy Study of XERMELO® + First-line Chemotherapy in Patients With Advanced Biliary Tract Cancer (PHASE2)
- Prospective Assessment of Patients With Neuroendocrine Tumors and Current or Prior History of Carcinoid Syndrome or Diarrhea Undergoing Peptide Receptor Radionuclide Therapy With or Without Telotristat Ethyl (PHASE2)
- Telotristat Ethyl for Reducing Intraoperative Carcinoid Crisis in Patients With Neuroendocrine Tumors (PHASE2)
Patents
| Patent | Expiry | Type |
|---|---|---|
| US9295701B2 | ||
| US9603879B2 | ||
| 7709493 | 2031-02-28 | Compound |
| 7968559 | 2027-12-11 | Method of Use |
| 8653094 | 2028-12-19 | Method of Use |
| 8193204 | 2031-02-27 | Compound |
| 7553840 | 2027-12-11 | Compound |
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- TELOTRISTAT ETIPRATE CI brief — competitive landscape report
- TELOTRISTAT ETIPRATE updates RSS · CI watch RSS