Telotristat (telotristat ethyl)

Para qué se usa Telotristat

Cita de la sección «Indications and Usage» (indicaciones y uso) de la etiqueta aprobada por la FDA. Se muestra en inglés, tal como la publica la FDA.

Xermelo is indicated for the treatment of carcinoid syndrome diarrhea in combination with somatostatin analog (SSA) therapy in adults inadequately controlled by SSA therapy. Xermelo is a tryptophan hydroxylase inhibitor indicated for the treatment of carcinoid syndrome diarrhea in combination with somatostatin analog (SSA) therapy in adults inadequately controlled by SSA therapy.

— Etiqueta de la FDA: Xermelo, TerSera Therapeutics LLC, vigente desde el 6 de agosto de 2026. Leer la etiqueta completa en DailyMed →

Etiqueta citada: la de la presentación más común (tablet, oral), Xermelo, TerSera Therapeutics LLC; abarca 1 producto del directorio NDC de la FDA. Las citas sobre efectos secundarios, interacciones, dosis y embarazo de abajo vienen de esta misma etiqueta.

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Efectos secundarios de Telotristat

Cita de la sección «Adverse Reactions» (reacciones adversas) de la etiqueta aprobada por la FDA. Se muestra en inglés. Avise a su médico de cualquier efecto secundario que le preocupe.

Most common adverse reactions (≥5%) are nausea, headache, increased GGT, depression, flatulence, decreased appetite, peripheral edema, and pyrexia.

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(6.1) To report SUSPECTED ADVERSE REACTIONS, contact TerSera Therapeutics LLC at 1-844-334-4035 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Xermelo was studied in a double-blind, placebo-controlled clinical trial of 90 patients with metastatic neuroendocrine tumors and carcinoid syndrome diarrhea. Patients reported between 4 to 12 bowel movements daily despite the use of SSA therapy at a stable dose for at least 3 months [see Clinical Studies (14)]. Placebo or Xermelo 250 mg was administered three times daily for 12 weeks. Concomitant anti-diarrheal medications (e.g., loperamide) were used by 43% (36% and 51% in the placebo and Xermelo group, respectively), pancreatic enzyme replacement medications by 39% (36% and 42% in the placebo and Xermelo group, respectively), and opioid analgesics by 29% (24% and 33% in the placebo and Xermelo group, respectively) of patients during the 12-week double-blind period of the trial. Table 1 below lists adverse reactions occurring at an incidence of at least 5% in the Xermelo group (N=45) and at an incidence greater than placebo (N=45) during the 12-week placebo-controlled period of the trial. Table 1: Percent Common Adverse Reactions a by Treatment Group at 12-Weeks in a Double-Blind Placebo-Controlled Clinical Trial of Patients with Carcinoid Syndrome Diarrhea a incidence of at least 5% in the Xermelo group and at an incidence greater than placebo b including depression, depressed mood and decreased interest Adverse Reaction Xermelo 250 mg Three Times Daily, N=45 (%) Placebo, N=45 (%) Nausea 13 11 Headache 11 4 Increased gamma-glutamyl-transferase (GGT) 9 0 Depression b 9 7 Peripheral edema 7 2 Flatulence 7 2 Decreased appetite 7 4 Pyrexia 7 4 In another placebo-controlled clinical trial of patients with carcinoid syndrome diarrhea and less than 4 bowel movements per day, the following additional adverse reactions, not listed in Table 1, of abdominal pain (including upper and lower abdominal pain, abdominal distention and gastrointestinal pain) and constipation were reported in at least 5% of patients in the Xermelo treated group and at an incidence greater than placebo [see Warnings and Precautions (5.1)].

— Etiqueta de la FDA: Xermelo, TerSera Therapeutics LLC, vigente desde el 6 de agosto de 2026. Esto es solo una parte de la sección. Leer la etiqueta completa en DailyMed →

Interacciones de Telotristat

Cita de la sección «Drug Interactions» (interacciones) de la etiqueta aprobada por la FDA. Se muestra en inglés. Dígale a su farmacéutico todos los medicamentos, vitaminas y productos herbales que toma.

CYP3A4 Substrates (e.g., midazolam) and CYP2B6 Substrates (e.g., bupropion, efavirenz): Efficacy of concomitant drugs may be decreased; monitor patients’ response and consider increasing the dosage of the concomitant drug, if necessary. (7.1) 7.1 CYP3A4 Substrates Concomitant use of Xermelo may decrease the efficacy of drugs that are CYP3A4 substrates (e.g., midazolam) by decreasing their systemic exposure.

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Monitor patients’ response to CYP3A4 substrates when co-administered with Xermelo and consider increasing the dosage of the interacting drug, if necessary [see Clinical Pharmacology (12.3)]. 7.2 CYP2B6 Substrates Concomitant use of Xermelo may decrease the efficacy of drugs that are CYP2B6 substrates (e.g., bupropion, efavirenz) by decreasing their systemic exposure. Monitor patients’ response to CYP2B6 substrates when co-administered with Xermelo and consider increasing the dosage of the interacting drug, if necessary [see Clinical Pharmacology (12.3)]. 7.3 Short-Acting Octreotide Concurrent administration of short-acting octreotide with Xermelo significantly decreased the systemic exposure of telotristat ethyl and telotristat, the active metabolite. If treatment with short-acting octreotide is needed in combination with Xermelo, administer short-acting octreotide at least 30 minutes after administration of Xermelo [see Clinical Pharmacology (12.3)].

— Etiqueta de la FDA: Xermelo, TerSera Therapeutics LLC, vigente desde el 6 de agosto de 2026. Leer la etiqueta completa en DailyMed →

Dosis de Telotristat

Cita de la sección «Dosage and Administration» (dosis y administración) de la etiqueta aprobada por la FDA. Se muestra en inglés. Su dosis es la que le receta su médico: no la cambie por su cuenta.

The recommended dosage of Xermelo in adult patients is 250 mg three times daily for patients whose diarrhea is inadequately controlled by SSA therapy. Administration Take Xermelo with food [see Clinical Pharmacology (12.3), Clinical Studies (14)]. When short-acting octreotide is used in combination with Xermelo, administer short-acting octreotide at least 30 minutes after administering Xermelo [see Drug Interactions (7.3)].

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If a dose is missed, take the next dose at the regular time. Do not take 2 doses at the same time to make up for a missed dose. Discontinue Xermelo if severe constipation develops [see Warnings and Precautions (5.1)]. The recommended dosage of Xermelo in adult patients is 250 mg three times daily for patients whose diarrhea is inadequately controlled by a SSA therapy. (2) Take Xermelo with food. (2) When short-acting octreotide is used in combination with Xermelo, administer short-acting octreotide at least 30 minutes after administering Xermelo. (2, 7.3) Discontinue Xermelo if severe constipation develops. (2, 5.1)

— Etiqueta de la FDA: Xermelo, TerSera Therapeutics LLC, vigente desde el 6 de agosto de 2026. Leer la etiqueta completa en DailyMed →

Telotristat en el embarazo

Cita de la parte sobre embarazo (Pregnancy) de la etiqueta aprobada por la FDA. Se muestra en inglés. Pregunte a su médico antes de tomar cualquier medicamento si está embarazada o planea estarlo.

Risk Summary There are no human data with Xermelo use in pregnant women to inform a drug-associated risk. In animal reproduction studies, no effects on embryo-fetal development were observed with the administration of oral telotristat ethyl to rats during organogenesis at doses up to 750 mg/kg/day (approximately 9 times the exposure at the RHD [recommended human dose]).

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Treatment of pregnant rabbits with oral telotristat ethyl during organogenesis produced maternal toxicity and post-implantation loss at doses of 250 mg/kg/day or higher (approximately 15 times the exposure at the RHD), and reduced fetal weight at 500 mg/kg/day (approximately 33 times the exposure at the RHD). In a pre-/postnatal development study, an increased incidence of mortality in rat offspring was observed during postnatal days 0 to 4 at the maternal oral dose of 500 mg/kg/day (approximately 5 times the exposure at the RHD), given during organogenesis through lactation (see Data). The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal data An embryo-fetal development study performed in rats with oral telotristat ethyl at doses up to 750 mg/kg/day (approximately 9 times the AUC [area under the plasma concentration-time curve] for the active metabolite at the RHD) during organogenesis produced no harm to embryo-fetal development. In pregnant rabbits treated orally with telotristat ethyl during organogenesis, an increased incidence of post-implantation loss at doses of 250 and 500 mg/kg/day (approximately 15 times the AUC for the active metabolite at RHD) and a decrease in fetal weight at 500 mg/kg/day (approximately 33 times the AUC for the active metabolite at the RHD) was observed. The adverse effects on embryo-fetal development were associated with maternal toxicity (impaired weight gain and/or mortality) at 250 and 500 mg/kg/day. No adverse effects on embryo-fetal development were observed at 125 mg/kg/day (approximately 5 times the AUC for the active metabolite at the RHD). A pre-/postnatal development study was conducted in rats using oral administration of 100, 200, and 500 mg/kg/day telotristat ethyl during organogenesis through lactation. An increased incidence of pup mortality was observed during postnatal days 0 to 4 at the maternal dose of 500 mg/kg/day (approximately 5 times the AUC for the active metabolite at the RHD). No developmental abnormalities or effects on growth, learning and memory, or reproductive performance were observed through maturation of offspring at maternal doses of up to 500 mg/kg/day in surviving offspring.

— Etiqueta de la FDA: Xermelo, TerSera Therapeutics LLC, vigente desde el 6 de agosto de 2026. Leer la etiqueta completa en DailyMed →

Cuándo no se debe usar Telotristat

Cita de la sección «Contraindications» (contraindicaciones) de la etiqueta aprobada por la FDA. Se muestra en inglés.

Xermelo is contraindicated in patients with a history of a hypersensitivity reaction to telotristat. Reactions have included angioedema, rash and pruritus. History of hypersensitivity to telotristat. (4)

— Etiqueta de la FDA: Xermelo, TerSera Therapeutics LLC, vigente desde el 6 de agosto de 2026. Leer la etiqueta completa en DailyMed →

Presentaciones y vía de administración

Empresas que tienen este medicamento

Empresas en el directorio NDC de la FDA: la empresa que aparece en el envase (fabricante o distribuidor), con su número de productos con receta.

• Lexicon Pharmaceuticals, Inc.2 productos
• TerSera Therapeutics LLC1 producto

Historial de aprobación de la FDA

• NDA: Solicitud de nuevo medicamento (NDA): así se aprueba un medicamento nuevo, normalmente de marca.

Escasez

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Retiros del mercado

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• Lexicon Pharmaceuticals, Inc.Fabricante o distribuidor
• TerSera Therapeutics LLCFabricante o distribuidor
• Todos los medicamentos con receta de la A a la ZBusque por nombre genérico, de marca o en español

Fuentes

1. Etiqueta aprobada por la FDA en DailyMed (Biblioteca Nacional de Medicina) — Xermelo, TerSera Therapeutics LLC, vigente desde el 6 de agosto de 2026; vía openFDA, datos de la FDA exportados el 30 de octubre de 2026, consultados el 31 de octubre de 2026
2. NDC Directory (openFDA) — Administración de Alimentos y Medicamentos de los EE. UU. (FDA), datos de la FDA exportados el 30 de octubre de 2026, consultados el 31 de octubre de 2026
3. Drugs@FDA (openFDA) — Administración de Alimentos y Medicamentos de los EE. UU. (FDA), datos de la FDA exportados el 30 de octubre de 2026, consultados el 31 de octubre de 2026
4. Drug recall enforcement reports (openFDA) — Administración de Alimentos y Medicamentos de los EE. UU. (FDA), datos de la FDA exportados el 27 de octubre de 2026, consultados el 31 de octubre de 2026
5. Drug shortages (openFDA) — Administración de Alimentos y Medicamentos de los EE. UU. (FDA), datos de la FDA exportados el 30 de octubre de 2026, consultados el 31 de octubre de 2026
6. Nombre en español: RxNorm (Biblioteca Nacional de Medicina de EE. UU.) y Wikidata, vinculados por el identificador RxNorm (RxCUI) del principio activo, sin coincidencias aproximadas.

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