 | |
| Clinical data | |
|---|---|
| Trade names | Xermelo |
| Other names | Telotristat ethyl, LX1032, LX1606 |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a617029 |
| License data | |
| Pregnancy category |
|
| Routes of administration | By mouth (tablets) |
| Legal status | |
| Legal status | |
| Pharmacokinetic data | |
| Protein binding | >99% (both telotristat ethyl and telotristat) |
| Metabolism | Hydrolysis via carboxylesterases |
| Metabolites | Telotristat |
| Elimination half-life | 0.6 hours (telotristat ethyl), 5 hours (telotristat) |
| Excretion | Feces (92.8%), urine (less than 0.4%)[1] |
| Identifiers | |
| |
| Chemical and physical data | |
| Formula | C27H26ClF3N6O3 |
| Molar mass | 574.99 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
Telotristat, sold under the brand name Xermelo, is a medication used to treat diarrhea due to carcinoid syndrome.[3] It is taken by mouth, three times per day.[3] It is used together with a somatostatin like agent.[3]
Common side effects include abdominal pain, liver problems, and tiredness.[2] Other side effects may include constipation.[3] Smaller doses may be required in those with liver problems.[2] Use during pregnancy is not recommended.[4] It works by blocking tryptophan hydroxylase, thereby decreasing the production of serotonin.[3][2]
Telotristat was approved for medical use in the United States and Europe in 2017.[3][2] In the United States it costs about 8,000 USD per month as of 2021.[5] This amount in the United Kingdom costs the NHS about £1,100.[4]
References
edit- ^ a b "Xermelo- telotristat ethyl tablet". DailyMed. 30 October 2020. Archived from the original on 12 November 2020. Retrieved 11 November 2020.
- ^ a b c d e f "Xermelo EPAR". European Medicines Agency (EMA). Archived from the original on 29 December 2019. Retrieved 17 April 2020.
- ^ a b c d e f g h "Telotristat Monograph for Professionals". Drugs.com. Archived from the original on 5 March 2021. Retrieved 25 September 2021.
- ^ a b BNF (80 ed.). BMJ Group and the Pharmaceutical Press. September 2020 – March 2021. p. 938. ISBN 978-0-85711-369-6.
{{cite book}}: CS1 maint: date format (link) - ^ "Xermelo Prices, Coupons & Patient Assistance Programs". Drugs.com. Archived from the original on 11 July 2021. Retrieved 25 September 2021.