Telotristat Ethyl API is a synthetic small-molecule pharmaceutical active ingredient and an orally administered prodrug of telotristat. It is a tryptophan hydroxylase (TPH) inhibitor that reduces peripheral serotonin production. Telotristat Ethyl is used in pharmaceutical formulations for the management of carcinoid syndrome diarrhea in adults whose symptoms are inadequately controlled with short-acting somatostatin analog therapy.
Swapnroop provides Telotristat Ethyl API for pharmaceutical development and manufacturing applications, supported by quality-focused manufacturing, analytical testing and documentation practices.
Telotristat Ethyl is also associated with the development code LX1606 and is the free-base form associated with the active pharmaceutical ingredient used in Xermelo. The marketed product contains telotristat ethyl as the hippurate salt, known as telotristat etiprate.
Telotristat Ethyl works as a prodrug that is hydrolyzed to its active metabolite, telotristat. Telotristat inhibits tryptophan hydroxylase, the rate-limiting enzyme involved in serotonin biosynthesis. By reducing peripheral serotonin production, telotristat can help reduce the frequency of carcinoid syndrome diarrhea.
The API is relevant to pharmaceutical research and manufacturing focused on gastrointestinal disorders associated with neuroendocrine tumors and carcinoid syndrome.
Telotristat Ethyl is a chiral synthetic molecule containing a substituted pyrimidine structure, trifluoroethoxy group, chlorophenyl group, pyrazole moiety and an ethyl ester of an L-phenylalanine derivative.
According to PubChem, Telotristat Ethyl has the molecular formula C₂₇H₂₆ClF₃N₆O₃ and molecular weight 575.0 g/mol. Its exact mass is approximately 574.1707 Da.
Telotristat Ethyl is primarily associated with pharmaceutical treatment of carcinoid syndrome diarrhea in adults with neuroendocrine tumors when short-acting somatostatin analog therapy does not provide adequate control.
Its pharmaceutical relevance is based on inhibition of peripheral serotonin synthesis. Serotonin contributes to gastrointestinal secretion, motility and other gastrointestinal effects associated with carcinoid syndrome. Telotristat, the active metabolite of Telotristat Ethyl, inhibits tryptophan hydroxylase and consequently reduces peripheral serotonin production.
Telotristat Ethyl API can be evaluated using validated analytical procedures appropriate for the material and intended pharmaceutical application.
Typical quality-control testing may include:
FDA regulatory documentation for Xermelo indicates that assay is determined using a validated HPLC method and that related substances and degradants are characterized and controlled using validated analytical methods.
Swapnroop offers Telotristat Ethyl API for pharmaceutical development, formulation and manufacturing requirements. Our API manufacturing approach emphasizes controlled production processes, analytical characterization and documentation designed to support pharmaceutical customers.
Telotristat Ethyl can be supplied according to mutually agreed technical requirements and applicable quality specifications. Documentation and analytical support can be provided according to the product grade and customer requirements.
Telotristat Ethyl API should be packaged in suitable pharmaceutical-grade, well-closed containers that protect the material from environmental exposure.
Recommended storage conditions should be established according to the validated stability data and the applicable product specification. Customers should follow the storage conditions stated on the batch-specific Certificate of Analysis and product documentation.
Depending on the applicable product grade and customer requirements, documentation may include:
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.2% |
| Heavy Metals | NMT 10 ppm |
| Individual Impurity | NMT 0.5% |
| Total Impurities | ≤ 1.5% |
| Water Content | NMT 1.0% |