Drug reference

telotristat ethyl

Tryptophan hydroxylase inhibitor · Antidiarrheal

Tryptophan hydroxylase inhibitorAntidiarrhealATC A07XA05

CDSCO approvedATC A07XA05

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

—

not curated

Top interactionssee all 12 →

BenzhydrocodoneSevereDatabaseDDInter
BrigatinibSevereDatabaseDDInter
ButorphanolSevereDatabaseDDInter
CobimetinibSevereDatabaseDDInter

Mechanism

Telotristat ethyl reduces diarrhea by inhibiting tryptophan hydroxylase, the rate-limiting enzyme of 5HT biosynthesis. Reduced 5HT secretion decreases fluid secretion and motility in the GI tract.

Indications

Diarrhea associated with carcinoid tumors (in combination with somatostatin analogue therapy)

Dosing

Adult: 250 mg three times per day (in combination with somatostatin analogue therapy for diarrhea associated with carcinoid tumors).

Pharmacokinetics

Peak effect

1 to 3 h (for active agent telotristat)

Half-life

5 h (for active agent telotristat)

Metabolism

Converted to active agent telotristat by carboxylesterases

Excretion

Via the feces

Side effects

Common

ConstipationNauseaHeadacheDepressionPeripheral edemaFlatulenceReduced appetitePyrexia

Serious

Increased gamma glutamyl transferase levels

Drug interactions

Benzhydrocodone

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Brigatinib

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Butorphanol

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Cobimetinib

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Doravirine

Severe

Database

Clinical effect not specified

Source: DDInter

Erdafitinib

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Fentanyl

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Glasdegib

Severe

Database

Clinical effect not specified

Source: DDInter

Hydrocodone

Severe

Database

Clinical effect not specified

Source: DDInter

Levacetylmethadol

Severe

Database

Clinical effect not specified

Source: DDInter

Lonafarnib

Severe

Database

Clinical effect not specified

Source: DDInter

Lorlatinib

Severe

Database

Clinical effect not specified

Source: DDInter

Related guidelines

Heart failure in diabetes

RSSDI · Cardiology · 2023

Extrapulmonary tuberculosis

ICMR · Infectious Diseases · 2022

Childhood pneumonia and respiratory infection

MOHFW · Paediatrics · 2021

Hypertension in adults

ICMR · Cardiology · 2019

Hypertrophic cardiomyopathy

ESC · Cardiology · 2026

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Sources: Goodman & Gilman 14e·Verified: 2026-05-10 · House clinical team