TheraRadar
Data updated: May 26, 2026

XERMELO (telotristat etiprate)

Trial Activity: Declining 1 active trials
First-in-Class Orphan Drug Priority Review Fast Track
Gastrointestinal Approved 2017-02-28

Xermelo helps patients with carcinoid syndrome diarrhea when their symptoms are not fully managed by somatostatin analog therapy alone. It is used in combination with these standard treatments to provide better control over gastrointestinal symptoms in adults. This medication is specifically for those who continue to experience frequent diarrhea despite being on a stable regimen of other therapies.

Source: FDA Label • TERSERA

How XERMELO Works

This drug works by inhibiting tryptophan hydroxylase, the enzyme responsible for the rate-limiting step in serotonin production. By blocking this enzyme, the medication reduces the over-production of peripheral serotonin that typically occurs in carcinoid syndrome. Lowering these serotonin levels helps decrease the frequency of diarrhea.

Development Insights

Lexicon Pharmaceuticals conducting 13 trials (59%)
21 indications explored (Broad Platform)
carcinoid syndrome (8 trials)
drug interactions (3 trials)
hepatic impairment (2 trials)
1
Indication
--
Phase 3 Trials
1
Priority Reviews
9
Years on Market

Details

Status
Prescription
First Approved
2017-02-28
Patent Cliff
2031

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Patent cliff and revenue data

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Routes
ORAL
Dosage Forms
TABLET

Companies

Active Ingredient: TELOTRISTAT ETIPRATE

XERMELO Approval History

2018
2019
2020
2021
2022
2023
2024
2025
2026
Original
New Indication
New Form
Label Update
3 FDA actions from 2017 to 2022
Sep 2022 SUPPL
Label · Labeling
Oct 2020 SUPPL
Label · Labeling
Feb 2017 ORIGINAL Priority
New Drug · Type 1 - New Molecular Entity

What XERMELO Treats

1 indications

XERMELO is approved for 1 conditions since its original approval in 2017. These indications span multiple therapeutic areas including oncology, immunology, and more.

  • Carcinoid Syndrome Diarrhea
Source: FDA Label
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Clinical Trial Registry

21 trials
Trial Sponsor ID Phase Status Title
NCT04810091 results posted 2019-1205 NCI-2021-00852, 2019-1205 Ph 3 active not recruiting Telotristat Ethyl for the Treatment of Carcinoid Heart Disease in Patients With Metastatic Neuroendocrine Tumor
NCT03910387 results posted IRB00105292 NCI-2018-01977, Winship4441-18 Ph 2 completed Telotristat Ethyl to Promote Weight Stability in Patients With Advanced Stage Pancreatic Cancer
NCT03453489 results posted 2017-144 NCI-2018-00294, 2017-144 Ph 2 completed AMT-PET in Monitoring Telotristat Etiprate Treatment in Participants With MetastaticNeuroendocrine Neoplasm
NCT03790111 TELE-ABC results posted LX1606.1-207-BTC LX1606.207, LX1606.207 Ph 2 terminated A Safety and Efficacy Study of XERMELO® + First-line Chemotherapy in Patients With Advanced Biliary Tract Cancer
NCT04713202 NET-PACS BTCRC-GI19-400 Ph 2 withdrawn Prospective Assessment of Patients With Neuroendocrine Tumors and Current or Prior History of Carcinoid Syndrome or Diarrhea Undergoing Peptide Receptor Radionuclide Therapy With or Without Telotristat Ethyl
NCT04776876 2020-0083 NCI-2021-00021, 2020-0083 Ph 2 withdrawn Retifanlimab (INCMGA00012) and Telotristat Ethyl for the Treatment of Advanced Neuroendocrine Tumors and Carcinoid Syndrome
NCT03442725 results posted D-FR-01017-002 2017-003948-20 Ph 1 completed Study to Compare a Dose of Telotristat Etiprate in Subjects With Renal Impairment With Matched Subjects With Normal Renal Function
NCT04065165 TELEFIRST EORTC-1715-GITCG Ph 3 withdrawn Lanreotide Combined With Telotristat Ethyl or Placebo for the First-line Treatment in Patients With Advanced Well Differentiated Small Intestinal Neuroendocrine Tumours (siNET) With Highly-functioning Carcinoid Syndrome
NCT02026063 TELEPATH results posted LX1606.1-302-CS LX1606.302, 2013-002596-18 Ph 3 completed Telotristat Etiprate - Expanded Treatment for Patients With Carcinoid Syndrome Symptoms
NCT01456052 results posted LX1606.1-204-UC LX1606.204, LX1032 Ph 2 completed A Study to Evaluate Safety and Efficacy of Telotristat Etiprate (LX1606) in Participants With Acute, Mild to Moderate Ulcerative Colitis
NCT01104415 results posted LX1606.1-203-CS LX1606.203, LX1032, 2009-016973-13 Ph 2 completed Study of Telotristat Etiprate (LX1606) in Participants With Symptomatic Carcinoid Syndrome
NCT02683577 results posted D-FR-01017-001 2015-004120-64 Ph 1 completed Study to Evaluate a Dose of Telotristat Etiprate in Male and Female With Mild, Moderate and Severe Hepatic Insufficiency and Matched Healthy Subjects
NCT00853047 results posted LX1606.1-202-CS LX1606.202 Ph 2 completed Study of Telotristat Etiprate (LX1606) in Participants With Symptomatic Carcinoid Syndrome Not Managed by Stable-Dose Octreotide Therapy
NCT03423446 LX1606.1-111-HEP LX1606.111 Ph 1 completed Study to Evaluate the Pharmacokinetics of Telotristat Ethyl in Subjects With Severe Hepatic Impairment
NCT01677910 results posted LX1606.1-301-CS LX1606.301, 2012-003460-47 Ph 3 completed TELESTAR (Telotristat Etiprate for Somatostatin Analogue Not Adequately Controlled Carcinoid Syndrome)
NCT02063659 TELECAST results posted LX1606.1-303-CS LX1606.303, 2013-001543-31 Ph 3 completed Telotristat Etiprate for Carcinoid Syndrome Therapy
NCT02195635 LX1606.1-109-NRM LX1606.109 Ph 1 completed Phase 1, Open-label, Drug-drug Interaction Study With Octreotide Acetate Injection and Telotristat Etiprate in Healthy Subjects
NCT02157558 LX1606.1-106-NRM LX1606.106 Ph 1 completed An Open-Label Drug-Drug Interaction Study of Telotristat Etiprate and Fexofenadine in Healthy Subjects
NCT02155205 LX1606.1-105-NRM LX1606.105 Ph 1 completed A Thorough QT Study of Telotristat Etiprate
NCT02157584 LX1606.1-107-NRM LX1606.107 Ph 1 completed An Open-Label Food Effect Study of Telotristat Etiprate
NCT02147808 LX1606.1-108-NRM LX1606.108 Ph 1 completed A Open-Label Drug-Drug Interaction Study of Telotristat Etiprate and Midazolam in Healthy Subjects
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Active Pipeline

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Ongoing clinical trials by development phase

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Key Completed Trials

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Completed studies with published results, ranked by significance

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Trial Timeline

Full development history with FDA approval milestones

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Understanding FDA Approval Types
Count Type What it means
- ORIG Original approval - drug first enters market
- SUPPL - Efficacy New indication (new disease/condition approved)
- SUPPL - Labeling Label text changes (warnings, dosing updates)
- SUPPL - Manufacturing Production changes (new facility)
- SUPPL - Chemistry Formulation changes (new dosage strength)

Green lines in the timeline show ORIG and Efficacy approvals - the clinically meaningful milestones.

XERMELO FDA Label Details

Indications & Usage

FDA Label (PDF)

XERMELO is indicated for the treatment of Carcinoid Syndrome Diarrhea.

View full patent landscape →
5 OB patents · 2 families · 100 international docs across 30 countries

XERMELO Patents & Exclusivity

Latest Patent: Feb 2031

Patents (5 active)

US7709493 Expires Feb 28, 2031
US8193204 Expires Feb 27, 2031
US8653094 Expires Dec 19, 2028
US7968559 Expires Dec 11, 2027
US7553840 Expires Dec 11, 2027
Source: FDA Orange Book

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Deep insights for XERMELO

Revenue Insights

  • Quarterly revenue tracking
  • Historical trend analysis

Patent Timeline

  • Cliff: 2031
  • 5 active patents

Trial Analysis

  • 22 total trials
  • Stage: Declining

Competitive Landscape

  • Competitor tracking
  • Same target/indication analysis
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Data Sources

Data sourced from official FDA and NIH databases. Click links to verify on original sources.

How We Calculate These Metrics

Trial Activity Stage

Measures the current development activity pattern based on trial phases, status, and trends. Important: This measures R&D activity, not commercial lifecycle.

Trial statuses: "Active" means recruiting or ongoing. "Completed" means reached planned endpoint. "Terminated" means stopped early—often due to safety, efficacy, or business reasons.

  • Growth: High proportion of early-phase trials (Phase 1/2), active development
  • Expansion: Significant Phase 3 activity, approaching or pursuing approvals
  • Mature: Substantial Phase 4 post-marketing studies
  • Stable: Mixed phase distribution, steady development
  • Declining: Low active trial ratio, reduced R&D investment