telotristat ethyl

Action and Spectrum

Actions and Spectrum 

Tryptophan hydroxylase, an enzyme necessary for the body’s conversion of tryptophan to serotonin, is specifically inhibited by the drug telotristat ethyl. It helps to regulate the diarrhea brought on by carcinoid syndrome by blocking this enzyme, which in turn lowers the amount of serotonin produced in the gastrointestinal system. 

Diarrhea caused by the carcinoid syndrome in adults can be treated with telotristat ethyl. People with neuroendocrine tumors, especially those originating from the gastrointestinal tract, are at risk of developing the illness known as carcinoid syndrome.   

Drug Interaction

Adverse Reaction

Frequency defined  

1-10% 

Decreased appetite (7%) 

Increased ALT and AST (<5%) 

Pyrexia (7%) 

Increased alkaline phosphatase (<5%) 

Increased GGT (9%) 

Flatulence (7%) 

Abdominal pain (5%) 

Constipation (5%) 

Depression (9%) 

Peripheral edema (7%) 

>10% 

Headache (11%) 

Nausea (13%) 

Post marketing reports 

Angioedema  

Pruritus   

Intestinal obstruction 

Rash 

Black Box Warning

Black Box Warning 

None

Contraindication / Caution

Contraindication/Caution: 

Contraindication:  

• telotristat ethyl should not be used in individuals with history of hypersensitivity or allergic reaction to the medication or its components. 

Caution: 

• Individuals with mild to severe hepatic impairment should not be given telotristat ethyl, therefore caution should be taken. 
• telotristat ethyl has not been proven to be safe for use while nursing or when pregnant. Should it be used during pregnancy or breast-feeding only if the potential advantages outweigh the possible risks. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: N/A 

Lactation: Excretion into human milk is unknown  

Pregnancy Categories:         

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.  

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women. 

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 

Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology  

Tryptophan is converted to 5-hydroxytryptophan (5-HTP), the precursor of serotonin, by the TPH enzyme, specifically TPH1 and TPH2 and thus telotristat ethyl blocks this enzyme. Serotonin regulates several physiological functions, including gastrointestinal secretion and motility. 

Pharmacodynamics 

The tryptophan hydroxylase (TPH) activity of telotristat ethyl is affected by the drug’s pharmacodynamics, which in turn affects serotonin levels.  

A decrease in serotonin synthesis results from telotristat ethyl’s suppression of TPH. It further assists in reducing the symptoms of carcinoid syndrome by reducing the synthesis of serotonin. 

Pharmacokinetics 

Absorption   

When telotristat ethyl is taken orally, the digestive tract quickly absorbs it. Esterases in the blood transform telotristat ethyl, which has been ingested, into telotristat, its active metabolite. 

Distribution 

telotristat, the active metabolite, is extensively bound to plasma proteins, primarily albumin. 

Metabolism 

The UDP-glucuronosyltransferase (UGT) enzymes play a key role in the liver’s metabolism of telotristat ethyl, which mostly involves glucuronidation.  

Elimination and excretion 

telotristat ethyl and its byproducts are mainly excreted via feces (around 91%) and to a minor extent in urine (about 2%). 

Adminstartion

Administration 

telotristat ethyl is available in the form of oral tablets. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: telotristat ethyl 

Why do we use telotristat ethyl? 

Adults suffering from diarrhoea related to carcinoid syndrome are typically treated with telotristat ethyl.   

By reducing serotonin levels, telotristat ethyl can improve the quality of life for individuals with carcinoid syndrome.   

telotristat ethyl works by lowering serotonin synthesis to reduce the diarrhoea brought on by carcinoid syndrome.