{"id":"telotristat-etiprate","rwe":[],"tags":[],"safety":{"boxedWarnings":[],"drugInteractions":[],"commonSideEffects":[{"effect":"Nausea","drugRate":"24%","severity":"Moderate"},{"effect":"Fatigue","drugRate":"20%","severity":"Mild to Moderate"},{"effect":"Headache","drugRate":"18%","severity":"Mild"},{"effect":"Dizziness","drugRate":"16%","severity":"Mild"},{"effect":"Decreased Appetite","drugRate":"14%","severity":"Mild"},{"effect":"Constipation","drugRate":"12%","severity":"Mild"},{"effect":"Abdominal Pain","drugRate":"10%","severity":"Mild to Moderate"}],"contraindications":[],"specialPopulations":{}},"trials":[],"_chembl":null,"aliases":[],"patents":[{"number":"US9295701B2","expiration":"2032"},{"number":"US9603879B2","expiration":"2033"},{"type":"Compound","number":"7709493","applicant":"TERSERA THERAPEUTICS LLC","territory":"US","tradeName":"XERMELO","expiryDate":"2031-02-28"},{"type":"Method of Use","number":"7968559","applicant":"TERSERA THERAPEUTICS LLC","territory":"US","tradeName":"XERMELO","expiryDate":"2027-12-11"},{"type":"Method of Use","number":"8653094","applicant":"TERSERA THERAPEUTICS LLC","territory":"US","tradeName":"XERMELO","expiryDate":"2028-12-19"},{"type":"Compound","number":"8193204","applicant":"TERSERA THERAPEUTICS LLC","territory":"US","tradeName":"XERMELO","expiryDate":"2031-02-27"},{"type":"Compound","number":"7553840","applicant":"TERSERA THERAPEUTICS LLC","territory":"US","tradeName":"XERMELO","expiryDate":"2027-12-11"}],"pricing":[],"offLabel":[],"timeline":[{"date":"March 30, 2017","type":"Approval","milestone":"FDA Approval","regulator":"FDA"},{"date":"April 2017","type":"Approval","milestone":"EU Approval","regulator":"EMA"}],"_dailymed":null,"aiSummary":"Telotristat etiprate is a serotonin synthesis inhibitor developed by Lexicon Pharmaceuticals for the treatment of carcinoid syndrome. It works by reducing the production of serotonin in the body, which can help manage symptoms such as flushing and diarrhea. The drug is approved for use in combination with somatostatin analogs in adults with carcinoid syndrome who have inadequately controlled symptoms. Despite its efficacy, telotristat etiprate has several side effects, including nausea, fatigue, and headache. The drug is not currently available as a generic, and it faces competition from other treatments for carcinoid syndrome.","ecosystem":[],"mechanism":{"target":"Tryptophan Hydroxylase-1 (TPH1)","novelty":"First-in-class serotonin synthesis inhibitor","modality":"Small Molecule","drugClass":"Serotonin Synthesis Inhibitor","explanation":"By inhibiting tryptophan hydroxylase, telotristat etiprate decreases the production of serotonin, which is often elevated in patients with carcinoid syndrome.","oneSentence":"Telotristat etiprate inhibits tryptophan hydroxylase, the rate-limiting enzyme in serotonin synthesis, thereby reducing serotonin levels in the body.","technicalDetail":"Telotristat etiprate specifically targets tryptophan hydroxylase-1 (TPH1), the isoform primarily responsible for serotonin production in peripheral tissues."},"_scrapedAt":"2026-03-28T00:37:04.950Z","_scrapedBy":"cloudflare-swarm","_wikipedia":null,"commercial":{"yoyGrowth":"Not Available","launchDate":"March 30, 2017","annualCostUS":"$34,500","currentRevenue":"Not Available","patientPopulation":"Approximately 10,000 patients in the US","peakSalesEstimate":"$200 million"},"references":[],"biosimilars":[],"competitors":["Lanreotide (Somatuline)","Octreotide (Sandostatin)","Pasireotide (Signifor)"],"indications":{"approved":["Carcinoid Syndrome"],"offLabel":[],"pipeline":[]},"labelChanges":[],"relatedDrugs":[],"trialDetails":[{"nctId":"NCT04810091","phase":"PHASE3","title":"Telotristat Ethyl for the Treatment of Carcinoid Heart Disease in Patients With Metastatic Neuroendocrine Tumor","status":"ACTIVE_NOT_RECRUITING","sponsor":"M.D. Anderson Cancer Center","startDate":"2021-05-18","conditions":"Locally Advanced Neuroendocrine Neoplasm, Metastatic Neuroendocrine Neoplasm","enrollment":79},{"nctId":"NCT03910387","phase":"PHASE2","title":"Telotristat Ethyl to Promote Weight Stability in Patients With Advanced Stage Pancreatic Cancer","status":"COMPLETED","sponsor":"Emory University","startDate":"2019-04-17","conditions":"Locally Advanced Unresectable Pancreatic Adenocarcinoma, Metastatic Pancreatic Adenocarcinoma, Recurrent Pancreatic Adenocarcinoma","enrollment":23},{"nctId":"NCT03453489","phase":"PHASE2","title":"AMT-PET in Monitoring Telotristat Etiprate Treatment in Participants With MetastaticNeuroendocrine Neoplasm","status":"COMPLETED","sponsor":"Barbara Ann Karmanos Cancer Institute","startDate":"2018-06-20","conditions":"Carcinoid Syndrome, Metastatic Nonfunctional Well Differentiated Neuroendocrine Neoplasm","enrollment":4},{"nctId":"NCT03223428","phase":"","title":"Real-world Evidence Study EvaLuating PAtient-Reported Outcomes With XERMELO","status":"COMPLETED","sponsor":"TerSera Therapeutics LLC","startDate":"2017-06-22","conditions":"Carcinoid Syndrome","enrollment":223},{"nctId":"NCT04543955","phase":"PHASE2","title":"Telotristat With Lutathera in Neuroendocrine Tumors","status":"TERMINATED","sponsor":"Lowell Anthony, MD","startDate":"2021-09-13","conditions":"Neuroendocrine Tumors","enrollment":1},{"nctId":"NCT03790111","phase":"PHASE2","title":"A Safety and Efficacy Study of XERMELO® + First-line Chemotherapy in Patients With Advanced Biliary Tract Cancer","status":"TERMINATED","sponsor":"TerSera Therapeutics LLC","startDate":"2019-03-13","conditions":"Biliary Tract Cancer (BTC)","enrollment":53},{"nctId":"NCT04713202","phase":"PHASE2","title":"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","status":"WITHDRAWN","sponsor":"Chandrikha Chandrasekhara","startDate":"2021-03-03","conditions":"Neuroendocrine Tumors, Carcinoid Syndrome, Diarrhea","enrollment":""},{"nctId":"NCT04672876","phase":"PHASE2","title":"Telotristat Ethyl for Reducing Intraoperative Carcinoid Crisis in Patients With Neuroendocrine Tumors","status":"WITHDRAWN","sponsor":"University of Chicago","startDate":"2022-01","conditions":"Neuroendocrine Tumors","enrollment":""},{"nctId":"NCT04776876","phase":"PHASE2","title":"Retifanlimab (INCMGA00012) and Telotristat Ethyl for the Treatment of Advanced Neuroendocrine Tumors and Carcinoid Syndrome","status":"WITHDRAWN","sponsor":"M.D. Anderson Cancer Center","startDate":"2021-03-01","conditions":"Advanced Neuroendocrine Neoplasm, Carcinoid Syndrome","enrollment":""},{"nctId":"NCT04034745","phase":"","title":"Open Label Study to Analyze the Effect of Telotristat Ethyl on Weight Regulation/Gain","status":"WITHDRAWN","sponsor":"Andrew Hendifar, MD","startDate":"2020-10","conditions":"Pancreatic Cancer, Neuroendocrine Tumors, Cachexia; Cancer","enrollment":""},{"nctId":"NCT03442725","phase":"PHASE1","title":"Study to Compare a Dose of Telotristat Etiprate in Subjects With Renal Impairment With Matched Subjects With Normal Renal Function","status":"COMPLETED","sponsor":"Ipsen","startDate":"2018-02-09","conditions":"Renal Impairment","enrollment":16},{"nctId":"NCT04065165","phase":"PHASE3","title":"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","status":"WITHDRAWN","sponsor":"European Organisation for Research and Treatment of Cancer - EORTC","startDate":"2020-04","conditions":"Small Intestinal NET, Carcinoid Heart Disease","enrollment":""},{"nctId":"NCT02026063","phase":"PHASE3","title":"Telotristat Etiprate - Expanded Treatment for Patients With Carcinoid Syndrome Symptoms","status":"COMPLETED","sponsor":"Lexicon Pharmaceuticals","startDate":"2014-01-14","conditions":"Carcinoid Syndrome","enrollment":124},{"nctId":"NCT01456052","phase":"PHASE2","title":"A Study to Evaluate Safety and Efficacy of Telotristat Etiprate (LX1606) in Participants With Acute, Mild to Moderate Ulcerative Colitis","status":"COMPLETED","sponsor":"Lexicon Pharmaceuticals","startDate":"2012-01-30","conditions":"Ulcerative Colitis","enrollment":59},{"nctId":"NCT01104415","phase":"PHASE2","title":"Study of Telotristat Etiprate (LX1606) in Participants With Symptomatic Carcinoid Syndrome","status":"COMPLETED","sponsor":"Lexicon Pharmaceuticals","startDate":"2010-06-15","conditions":"Carcinoid Syndrome","enrollment":15},{"nctId":"NCT02683577","phase":"PHASE1","title":"Study to Evaluate a Dose of Telotristat Etiprate in Male and Female With Mild, Moderate and Severe Hepatic Insufficiency and Matched Healthy Subjects","status":"COMPLETED","sponsor":"Ipsen","startDate":"2016-02","conditions":"Hepatic Impairment","enrollment":24},{"nctId":"NCT00853047","phase":"PHASE2","title":"Study of Telotristat Etiprate (LX1606) in Participants With Symptomatic Carcinoid Syndrome Not Managed by Stable-Dose Octreotide Therapy","status":"COMPLETED","sponsor":"Lexicon Pharmaceuticals","startDate":"2009-03","conditions":"Carcinoid Syndrome","enrollment":23},{"nctId":"NCT03423446","phase":"PHASE1","title":"Study to Evaluate the Pharmacokinetics of Telotristat Ethyl in Subjects With Severe Hepatic Impairment","status":"COMPLETED","sponsor":"Lexicon Pharmaceuticals","startDate":"2017-11-28","conditions":"Hepatic Impairment","enrollment":16},{"nctId":"NCT03302845","phase":"PHASE1","title":"A Phase 1 Study to Evaluate the Effects of Omeprazole and Famotidine on the Absorption of Telotristat Ethyl in Healthy Subjects","status":"COMPLETED","sponsor":"Lexicon Pharmaceuticals","startDate":"2017-09-21","conditions":"Drug-drug Interaction","enrollment":32},{"nctId":"NCT01677910","phase":"PHASE3","title":"TELESTAR (Telotristat Etiprate for Somatostatin Analogue Not Adequately Controlled Carcinoid Syndrome)","status":"COMPLETED","sponsor":"Lexicon Pharmaceuticals","startDate":"2013-01-08","conditions":"Carcinoid Syndrome","enrollment":135},{"nctId":"NCT02063659","phase":"PHASE3","title":"Telotristat Etiprate for Carcinoid Syndrome Therapy","status":"COMPLETED","sponsor":"Lexicon Pharmaceuticals","startDate":"2014-03-11","conditions":"Carcinoid Syndrome","enrollment":76},{"nctId":"NCT02195635","phase":"PHASE1","title":"Phase 1, Open-label, Drug-drug Interaction Study With Octreotide Acetate Injection and Telotristat Etiprate in Healthy Subjects","status":"COMPLETED","sponsor":"Lexicon Pharmaceuticals","startDate":"2014-07","conditions":"Drug Interactions","enrollment":24},{"nctId":"NCT02147808","phase":"PHASE1","title":"A Open-Label Drug-Drug Interaction Study of Telotristat Etiprate and Midazolam in Healthy Subjects","status":"COMPLETED","sponsor":"Lexicon Pharmaceuticals","startDate":"2014-05","conditions":"Drug Interactions","enrollment":24},{"nctId":"NCT02155205","phase":"PHASE1","title":"A Thorough QT Study of Telotristat Etiprate","status":"COMPLETED","sponsor":"Lexicon Pharmaceuticals","startDate":"2014-05","conditions":"QT Interval","enrollment":48},{"nctId":"NCT02157584","phase":"PHASE1","title":"An Open-Label Food Effect Study of Telotristat Etiprate","status":"COMPLETED","sponsor":"Lexicon Pharmaceuticals","startDate":"2014-06","conditions":"Healthy","enrollment":22},{"nctId":"NCT02157558","phase":"PHASE1","title":"An Open-Label Drug-Drug Interaction Study of Telotristat Etiprate and Fexofenadine in Healthy Subjects","status":"COMPLETED","sponsor":"Lexicon Pharmaceuticals","startDate":"2014-07","conditions":"Drug Interactions","enrollment":24},{"nctId":"NCT01932528","phase":"PHASE1","title":"An Open-label Study to Evaluate the Absorption, Metabolism, and Excretion of [14C]-Telotristat Etiprate in Males","status":"COMPLETED","sponsor":"Lexicon Pharmaceuticals","startDate":"2013-08","conditions":"Carcinoid Syndrome","enrollment":8}],"_emaApprovals":[],"_faersSignals":[],"genericFilers":[],"latestUpdates":[],"manufacturing":[],"formularyStatus":[],"_approvalHistory":[],"developmentCodes":[],"ownershipHistory":[],"publicationCount":0,"therapeuticAreas":["Oncology"],"biosimilarFilings":[],"companionDiagnostics":[],"genericManufacturerList":[],"phase":"marketed","status":"approved","brandName":"TELOTRISTAT ETIPRATE","genericName":"TELOTRISTAT ETIPRATE","companyName":"","companyId":"","modality":"Small molecule","firstApprovalDate":"2017","enrichmentLevel":3,"visitCount":0,"regulatoryByCountry":[{"country_code":"CA","regulator":"Health Canada","status":"approved","approval_date":null,"mah":"","brand_name_local":"","application_number":""},{"country_code":"US","regulator":"FDA","status":"approved","approval_date":null,"mah":null,"brand_name_local":null,"application_number":null}],"patentsNormalised":[{"patent_number":"7968559","territory":"US","patent_type":"Method of 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