Telotristat ethyl (

USAN 280px, "Samguk Sagi" Book 04. Silla's Records. In 512, Usan-guk（于山國）was Ulleungdo（鬱陵島） Usan-guk, or the State of Usan, occupied Ulleung-do and the adjacent islands during the Korean Three Kingdoms period. According to th ...

, brand name Xermelo) is a

prodrug A prodrug is a medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. Instead of administering a drug directly, a corresponding prodrug can be used to improve how the drug ...

of telotristat, which is an inhibitor of

tryptophan hydroxylase Tryptophan hydroxylase (TPH) is an enzyme () involved in the synthesis of the neurotransmitter serotonin. Tyrosine hydroxylase, phenylalanine hydroxylase, and tryptophan hydroxylase together constitute the family of biopterin-dependent aromat ...

. It is formulated as telotristat etiprate — a

hippurate Hippuric acid ( Gr. ''hippos'', horse, ''ouron'', urine) is a carboxylic acid and organic compound. It is found in urine and is formed from the combination of benzoic acid and glycine. Levels of hippuric acid rise with the consumption of phenolic ...

salt of telotristat ethyl. On February 28, 2017, the U.S.

Food and Drug Administration The United States Food and Drug Administration (FDA or US FDA) is a List of United States federal agencies, federal agency of the United States Department of Health and Human Services, Department of Health and Human Services. The FDA is respon ...

(FDA) approved telotristat ethyl in combination with

somatostatin Somatostatin, also known as growth hormone-inhibiting hormone (GHIH) or by several other names, is a peptide hormone that regulates the endocrine system and affects neurotransmission and cell proliferation via interaction with G protein-couple ...

analog (SSA) therapy for the treatment of adults with

diarrhea Diarrhea, also spelled diarrhoea, is the condition of having at least three loose, liquid, or watery bowel movements each day. It often lasts for a few days and can result in dehydration due to fluid loss. Signs of dehydration often begin wi ...

associated with

carcinoid syndrome Carcinoid syndrome is a paraneoplastic syndrome comprising the signs and symptoms that occur secondary to carcinoid tumors. The syndrome includes flushing and diarrhea, and less frequently, heart failure, vomiting and bronchoconstriction. It is ...

that SSA therapy alone has inadequately controlled. Telotristat ethyl was approved for use in the European Union in September 2017. The U.S.

(FDA) considers it to be a

first-in-class medication A first-in-class medication is a pharmaceutical that uses a "new and unique mechanism of action" to treat a particular medical condition. While the Food and Drug Administration's Center for Drug Evaluation and Research tracks first-in-class medicat ...

Pharmacology

Telotristat is an inhibitor of tryptophan hydroxylase, which mediates the

rate-limiting step In chemical kinetics, the overall rate of a reaction is often approximately determined by the slowest step, known as the rate-determining step (RDS or RD-step or r/d step) or rate-limiting step. For a given reaction mechanism, the prediction of the ...

serotonin biosynthesis Serotonin () or 5-hydroxytryptamine (5-HT) is a monoamine neurotransmitter. Its biological function is complex and multifaceted, modulating mood, cognition, reward, learning, memory, and numerous physiological processes such as vomiting and vas ...

Action of telotristat on tryptophan hydroxylase

Adverse effects

Common adverse effects noted in clinical trials include nausea, headache, elevated liver enzymes, depression, accumulation of fluid causing swelling (peripheral edema), flatulence, decreased appetite, and fever. Constipation is also common, and may be serious or life-threatening (especially in overdose).

Formulations

It is marketed by

Lexicon Pharmaceuticals Lexicon Pharmaceuticals, Inc. is a biotechnology, biopharmaceutical company developing treatments for human disease. The company was founded in 1995 in The Woodlands, Texas under the name Lexicon Genetics, Incorporated by co-founders Allan Bradley ...

(as telotristat etiprate). 328 mg telotristat etiprate is equivalent to 250 mg telotristate ethyl.

References

External links

* * {{Portal bar , Medicine Amines Ethyl esters Guanidines Chloroarenes CYP3A4 inducers Trifluoromethyl compounds Phenethylamines Prodrugs Pyrazoles Aminopyrimidines Tryptophan hydroxylase inhibitors

Pharmacology

Adverse effects

Formulations

References

Further reading

External links