{"id":"casopitant","rwe":[{"pmid":"39708024","year":"2025","title":"Pharmacological Strategies for Postdischarge Nausea and Vomiting: Evidence-based Review Update.","finding":"","journal":"Journal of perianesthesia nursing : official journal of the American Society of PeriAnesthesia Nurses","studyType":"Clinical Study"},{"pmid":"37904319","year":"2024","title":"Homology modeling, virtual screening, molecular docking, and ADME approaches to identify a potent agent targeting NK2R protein.","finding":"","journal":"Biotechnology and applied biochemistry","studyType":"Clinical Study"},{"pmid":"35045580","year":"2022","title":"Novel Antidepressants in the Pipeline (Phase II and III): A Systematic Review of the US Clinical Trials Registry.","finding":"","journal":"Pharmacopsychiatry","studyType":"Clinical Study"},{"pmid":"34784425","year":"2021","title":"Antiemetics for adults for prevention of nausea and vomiting caused by moderately or highly emetogenic chemotherapy: a network meta-analysis.","finding":"","journal":"The Cochrane database of systematic reviews","studyType":"Clinical Study"},{"pmid":"33075160","year":"2020","title":"Drugs for preventing postoperative nausea and vomiting in adults after general anaesthesia: a network meta-analysis.","finding":"","journal":"The Cochrane database of systematic reviews","studyType":"Clinical Study"}],"tags":[{"label":"casopitant","category":"class"},{"label":"Small Molecule","category":"modality"},{"label":"Substance-P receptor","category":"target"},{"label":"TACR1","category":"gene"},{"label":"SIGMAR1","category":"gene"},{"label":"A04AD13","category":"atc"},{"label":"Active","category":"status"},{"label":"Antiemetics","category":"pharmacology"},{"label":"Central Nervous System Agents","category":"pharmacology"},{"label":"Gastrointestinal Agents","category":"pharmacology"},{"label":"Neurokinin-1 Receptor Antagonists","category":"pharmacology"},{"label":"Neurotransmitter Agents","category":"pharmacology"},{"label":"Peripheral Nervous System Agents","category":"pharmacology"}],"phase":"phase_3","safety":{},"trials":[],"aliases":[],"patents":[],"pricing":[],"allNames":"zunrisa","offLabel":[],"synonyms":["zunrisa","casopitant","casopitant mesilate","casopitant mesylate","GW679769","GW-679769"],"timeline":[],"aiSummary":"Zunrisa (casopitant) is a small molecule drug that targets the Substance-P receptor. It is a member of the drug class casopitant and works by blocking the action of Substance-P, a natural substance in the body that can cause nausea and vomiting. Zunrisa is not FDA-approved for any indications, and its commercial status is unknown. Key safety considerations include its half-life of 15.6 hours, although its bioavailability and off-patent status are unknown.","brandName":"Zunrisa","ecosystem":[],"mechanism":{"target":"Sigma non-opioid intracellular receptor 1, Substance-P receptor","targets":[{"gene":"TACR1","source":"DrugCentral","target":"Substance-P receptor","protein":"Substance-P receptor"},{"gene":"SIGMAR1","source":"DrugCentral","target":"Sigma non-opioid intracellular receptor 1","protein":"Sigma non-opioid intracellular receptor 1"}],"modality":"Small Molecule","drugClass":"casopitant","explanation":"Imagine your body has a natural 'message' system that helps you feel sick when you're about to vomit. Substance-P is one of these messages, and it's sent to your brain to make you feel nauseous. Zunrisa blocks this message, helping to prevent nausea and vomiting.","oneSentence":"Zunrisa works by blocking the action of Substance-P, a natural substance that can cause nausea and vomiting.","technicalDetail":"Zunrisa is a selective antagonist of the neurokinin 1 (NK1) receptor, which is the primary receptor for Substance-P. By blocking this receptor, Zunrisa prevents Substance-P from binding and triggering the nausea and vomiting response."},"commercial":{},"references":[{"id":1,"url":"https://drugcentral.org/drugcard/4401","fields":["approvals","synonyms","ATC","PK","indications","contraindications","DDIs","targets","patents","FAERS"],"source":"DrugCentral"},{"id":2,"url":"https://clinicaltrials.gov/search?intr=CASOPITANT","fields":["trials"],"source":"ClinicalTrials.gov"},{"id":3,"url":"https://pubmed.ncbi.nlm.nih.gov/?term=CASOPITANT","fields":["publications"],"source":"PubMed/NCBI"}],"_enrichedAt":"2026-03-30T09:16:00.618046","biosimilars":[],"competitors":[{"drugName":"scopolamine","drugSlug":"scopolamine","fdaApproval":"1979-12-31","genericCount":7,"patentStatus":"Off-patent — generic available","relationship":"same-class"},{"drugName":"chlorobutanol","drugSlug":"chlorobutanol","fdaApproval":"","relationship":"same-class"},{"drugName":"dronabinol","drugSlug":"dronabinol","fdaApproval":"1985-05-31","patentExpiry":"Aug 6, 2028","patentStatus":"Patent protected","relationship":"same-class"},{"drugName":"nabilone","drugSlug":"nabilone","fdaApproval":"1985-12-26","patentStatus":"Unknown","relationship":"same-class"},{"drugName":"aprepitant","drugSlug":"aprepitant","fdaApproval":"2003-03-27","patentExpiry":"Sep 26, 2027","patentStatus":"Patent protected","relationship":"same-class"},{"drugName":"rolapitant","drugSlug":"rolapitant","fdaApproval":"2015-09-01","patentExpiry":"Oct 9, 2029","patentStatus":"Patent protected","relationship":"same-class"}],"dataSources":[{"url":"https://drugcentral.org","name":"DrugCentral","fields":["indications","contraindications","safety","target","drugInteractions"],"retrievedDate":"2026-04-07"}],"genericName":"casopitant","indications":{"approved":[],"offLabel":[],"pipeline":[]},"drugCategory":"active","labelChanges":[],"relatedDrugs":[{"drugId":"scopolamine","brandName":"scopolamine","genericName":"scopolamine","approvalYear":"1979","relationship":"same-class"},{"drugId":"chlorobutanol","brandName":"chlorobutanol","genericName":"chlorobutanol","approvalYear":"","relationship":"same-class"},{"drugId":"dronabinol","brandName":"dronabinol","genericName":"dronabinol","approvalYear":"1985","relationship":"same-class"},{"drugId":"nabilone","brandName":"nabilone","genericName":"nabilone","approvalYear":"1985","relationship":"same-class"},{"drugId":"aprepitant","brandName":"aprepitant","genericName":"aprepitant","approvalYear":"2003","relationship":"same-class"},{"drugId":"rolapitant","brandName":"rolapitant","genericName":"rolapitant","approvalYear":"2015","relationship":"same-class"}],"trialDetails":[{"nctId":"NCT00601172","phase":"PHASE3","title":"A Study Of IV Casopitant For The Prevention Of Chemotherapy Induced Nausea And Vomiting.","status":"COMPLETED","sponsor":"GlaxoSmithKline","startDate":"2008-03-10","conditions":["Nausea and Vomiting, Chemotherapy-Induced"],"enrollment":710,"completionDate":"2009-04-13"},{"nctId":"NCT00334646","phase":"PHASE1","title":"Cyclophosphamide Drug Interaction Study In Cancer Patients","status":"TERMINATED","sponsor":"GlaxoSmithKline","startDate":"2005-08-10","conditions":["Nausea and Vomiting, Chemotherapy-Induced"],"enrollment":25,"completionDate":"2009-10-14"},{"nctId":"NCT00437229","phase":"PHASE1","title":"A Study to Assess the Safety & Interaction Between GW679769, Dexamethasone, & Ondansetron When Taken by Healthy Adults","status":"COMPLETED","sponsor":"GlaxoSmithKline","startDate":"2007-02-19","conditions":["Nausea and Vomiting, Chemotherapy-Induced"],"enrollment":37,"completionDate":"2007-05-15"},{"nctId":"NCT00359177","phase":"PHASE1","title":"Observational Study Evaluating The Processing Or Breakdown Of GW679769 In Subjects With Hepatic Impairment","status":"COMPLETED","sponsor":"GlaxoSmithKline","startDate":"2005-12-01","conditions":["Vomiting"],"enrollment":24,"completionDate":"2006-10-12"},{"nctId":"NCT00405080","phase":"PHASE1","title":"A Study in Healthy Subjects to Assess How Dosing of Rifampin Affects What the Body Does to a Dose of GW679769 (Casopitant).","status":"COMPLETED","sponsor":"GlaxoSmithKline","startDate":"2006-11-11","conditions":["Nausea and Vomiting, Chemotherapy-Induced"],"enrollment":12,"completionDate":"2007-01-05"},{"nctId":"NCT00404378","phase":"PHASE1","title":"Study Of Healthy Subjects To Assess The Effect Of Ketoconazole And The Way The Body Will React To Casopitant [GW679769]","status":"COMPLETED","sponsor":"GlaxoSmithKline","startDate":"2006-10-20","conditions":["Nausea and Vomiting, Chemotherapy-Induced"],"enrollment":15,"completionDate":"2007-01-05"},{"nctId":"NCT00431236","phase":"PHASE3","title":"A Study of the Drug Casopitant for the Prevention of Nausea Caused By Cisplatin-Based Highly Emetogenic Chemotherapy","status":"COMPLETED","sponsor":"GlaxoSmithKline","startDate":"2006-11-06","conditions":["Nausea and Vomiting, Chemotherapy-Induced"],"enrollment":810,"completionDate":"2007-10-09"},{"nctId":"NCT00404274","phase":"PHASE1","title":"A Study Testing the Effect and Safety of Casopitant (GW679769) While Taking Warfarin in Healthy Human Volunteers","status":"COMPLETED","sponsor":"GlaxoSmithKline","startDate":"2006-11-01","conditions":["Nausea and Vomiting, Chemotherapy-Induced"],"enrollment":97,"completionDate":"2007-03-18"},{"nctId":"NCT00650871","phase":"PHASE2","title":"A Study to Evaluate the Effects of GW679769 on Sleep and Cognitive Function in Subjects With Primary Insomnia","status":"COMPLETED","sponsor":"GlaxoSmithKline","startDate":"2004-07-30","conditions":["Sleep Initiation and Maintenance Disorders"],"enrollment":48,"completionDate":"2005-08-30"},{"nctId":"NCT00358813","phase":"PHASE1","title":"Observational Pharmacokinetic Study Of GW679769 In Subjects With Renal Impairment","status":"COMPLETED","sponsor":"GlaxoSmithKline","startDate":"2006-09-08","conditions":["Vomiting"],"enrollment":18,"completionDate":"2008-08-22"},{"nctId":"NCT00440128","phase":"PHASE1","title":"The Effects Of GW679769 (Casopitant) On The Pharmacokinetics Of Docetaxel In Subjects With Cancer","status":"COMPLETED","sponsor":"GlaxoSmithKline","startDate":"2007-05-04","conditions":["Nausea and Vomiting, Chemotherapy-Induced"],"enrollment":12,"completionDate":"2008-07-17"},{"nctId":"NCT00511823","phase":"PHASE1","title":"The Pharmacokinetic Interaction Between Oral Casopitant and Oral Dolasetron, Granisetron or Rosiglitazone in Subjects","status":"COMPLETED","sponsor":"GlaxoSmithKline","startDate":"2007-07-23","conditions":["Nausea and Vomiting, Chemotherapy-Induced"],"enrollment":16,"completionDate":"2007-09-21"},{"nctId":"NCT00460707","phase":"PHASE1","title":"A Study to Assess the Safety and Interaction Between Casopitant and Ketoconazole When Taken By Healthy Adults","status":"COMPLETED","sponsor":"GlaxoSmithKline","startDate":"2007-04-16","conditions":["Nausea and Vomiting, Chemotherapy-Induced"],"enrollment":85,"completionDate":"2007-08-27"},{"nctId":"NCT00334152","phase":"PHASE3","title":"Casopitant And ZOFRAN To Prevent Post Operative Nausea And Vomiting In Women","status":"COMPLETED","sponsor":"GlaxoSmithKline","startDate":"2006-03","conditions":["Nausea and Vomiting, Postoperative","Postoperative Nausea and Vomiting"],"enrollment":515,"completionDate":"2006-07"},{"nctId":"NCT00358410","phase":"PHASE2","title":"An Exploratory Study Examining The Effects Of Taking GW679769 Once-Daily For 4 Days In Patients With Functional Dyspepsia","status":"COMPLETED","sponsor":"GlaxoSmithKline","startDate":"2006-01","conditions":["Nonulcer Dyspepsia"],"enrollment":13,"completionDate":"2006-08"},{"nctId":"NCT00108095","phase":"PHASE2","title":"A Study To Evaluate An NK-1 Antiemetic For The Prevention Of Post Operative Nausea And Vomiting","status":"COMPLETED","sponsor":"GlaxoSmithKline","startDate":"2004-10","conditions":["Postoperative Nausea and Vomiting","Nausea and Vomiting, Postoperative"],"enrollment":701,"completionDate":"2005-08"},{"nctId":"NCT00321477","phase":"PHASE2","title":"A Study Of GW679769 Compared To Placebo In Women With Overactive Bladder","status":"COMPLETED","sponsor":"GlaxoSmithKline","startDate":"2005-12","conditions":["Incontinence, Urinary and Urinary Bladder, Overactive","Overactive Bladder"],"enrollment":160,"completionDate":"2007-02"},{"nctId":"NCT00274690","phase":"PHASE2","title":"Post-Operative Nausea And Vomiting Study In Female Patients","status":"COMPLETED","sponsor":"GlaxoSmithKline","startDate":"2005-02","conditions":["Postoperative Nausea and Vomiting","Nausea and Vomiting, Postoperative"],"enrollment":435,"completionDate":"2005-08"},{"nctId":"NCT00413023","phase":"PHASE2","title":"Study Of The Effects Of A New Antidepressant Therapy In Patients With Major Depressive Disorder (MDD)","status":"COMPLETED","sponsor":"GlaxoSmithKline","startDate":"2005-06","conditions":["Depressive Disorder, Major"],"enrollment":348,"completionDate":"2006-09"},{"nctId":"NCT00273039","phase":"PHASE2","title":"A Study Of A New Medicine (GW679769) For The Treatment Of Social Anxiety Disorder","status":"COMPLETED","sponsor":"GlaxoSmithKline","startDate":"2005-08","conditions":["Social Anxiety Disorder","Anxiety Disorders"],"enrollment":242,"completionDate":"2006-09"},{"nctId":"NCT00326248","phase":"PHASE3","title":"Casopitant (Oral) And ZOFRAN To Prevent Postoperative Nausea And Vomiting In Women","status":"COMPLETED","sponsor":"GlaxoSmithKline","startDate":"2006-03","conditions":["Nausea and Vomiting, Postoperative"],"enrollment":482,"completionDate":"2006-07"},{"nctId":"NCT00891761","phase":"PHASE3","title":"A Study of IV Casopitant for the Prevention of Nausea and Vomiting Caused By Cisplatin-Based Highly Emetogenic Chemotherapy","status":"WITHDRAWN","sponsor":"GlaxoSmithKline","startDate":"2009-09","conditions":["Cancer","Chemotherapy-Induced Nausea and Vomiting","Nausea and Vomiting","Solid Tumor Cancer"],"enrollment":0,"completionDate":"2010-07"},{"nctId":"NCT00332319","phase":"PHASE2","title":"Effects Of GW679769 On Bladder Nerve Function And Symptoms Of Overactive Bladder In Spinal Cord Injury Patients","status":"TERMINATED","sponsor":"GlaxoSmithKline","startDate":"2006-01","conditions":["Incontinence, Urinary and Urinary Bladder, Overactive","Overactive Bladder"],"enrollment":1,"completionDate":"2007-02"},{"nctId":"NCT00104403","phase":"PHASE2","title":"Study Of Prevention of Chemo-Induced Nausea and Vomiting Caused By Moderately Emetogenic Chemotherapy","status":"COMPLETED","sponsor":"GlaxoSmithKline","startDate":"2004-12","conditions":["Nausea and Vomiting, Chemotherapy-Induced","Chemotherapy-Induced Nausea and Vomiting"],"enrollment":722,"completionDate":"2006-01"},{"nctId":"NCT00280436","phase":"PHASE2","title":"Effects Of GW679769 On Sleep Onset And Maintenance,And Next Day Functioning In The Elderly And Non-elderly With Primary Insomnia","status":"COMPLETED","sponsor":"GlaxoSmithKline","startDate":"2006-01","conditions":["Sleep Initiation and Maintenance Disorders","Insomnia"],"enrollment":122,"completionDate":"2007-03"},{"nctId":"NCT00354809","phase":"PHASE2","title":"Evaluation of A Morning Dosing Of A New Medicine And Its Effects On Sleep At Bedtime In Subjects With Primary Insomnia","status":"COMPLETED","sponsor":"GlaxoSmithKline","startDate":"2006-05","conditions":["Sleep Initiation and Maintenance Disorders","Insomnia"],"enrollment":68,"completionDate":"2007-07"},{"nctId":"NCT00264628","phase":"","title":"GW679769 In Fibromyalgia","status":"COMPLETED","sponsor":"GlaxoSmithKline","startDate":"2005-10","conditions":["Depressive Disorder","Depression","Fibromyalgia"],"enrollment":8,"completionDate":"2006-09"},{"nctId":"NCT00102492","phase":"PHASE2","title":"Study Of GW679769 In Major Depressive Disorder","status":"COMPLETED","sponsor":"GlaxoSmithKline","startDate":"2004-10","conditions":["Depressive Disorder, Major","Major Depressive Disorder (MDD)"],"enrollment":356,"completionDate":"2006-09"},{"nctId":"NCT00280423","phase":"PHASE2","title":"Effects Of GW679769 On Sleep Onset And Maintenance And Next Day Functioning In Subjects With Primary Insomnia","status":"COMPLETED","sponsor":"GlaxoSmithKline","startDate":"2006-01","conditions":["Sleep Initiation and Maintenance Disorders","Insomnia"],"enrollment":342,"completionDate":"2007-02"},{"nctId":"NCT00366834","phase":"PHASE3","title":"Intravenous And Oral Casopitant (GW679769) For The Prevention Of Chemotherapy Induced Nausea And Vomiting","status":"COMPLETED","sponsor":"GlaxoSmithKline","startDate":"2006-07","conditions":["Vomiting","Nausea","Nausea and Vomiting, Chemotherapy-Induced"],"enrollment":1840,"completionDate":"2009-10"},{"nctId":"NCT00169572","phase":"PHASE2","title":"Study for The Prevention Of Nausea in Cancer Patients Receiving Highly Emetogenic Cisplatin Based Chemotherapy","status":"COMPLETED","sponsor":"GlaxoSmithKline","startDate":"2005-02","conditions":["Nausea and Vomiting","Chemotherapy-Induced"],"enrollment":492,"completionDate":""},{"nctId":"NCT00332046","phase":"PHASE1","title":"fMRI Study Comparing BOLD Activation Patterns Using GW679769 In Subjects With Social Anxiety Disorder","status":"COMPLETED","sponsor":"GlaxoSmithKline","startDate":"2006-01","conditions":["Social Anxiety Disorder"],"enrollment":57,"completionDate":""}],"genericFilers":[],"latestUpdates":[],"manufacturing":[],"administration":{},"crossReferences":{"UNII":"3B03KPM27L","CHEBI":"CHEBI:135967","INN_ID":"8701","UMLSCUI":"C2347566","ChEMBL_ID":"CHEMBL1672054","KEGG_DRUG":"D06574","DRUGBANK_ID":"DB06634","PUBCHEM_CID":"9917021","IUPHAR_LIGAND_ID":"5758","SECONDARY_CAS_RN":"414910-30-8","MESH_SUPPLEMENTAL_RECORD_UI":"C531951"},"formularyStatus":[],"_enricherVersion":"v2","developmentCodes":[],"ownershipHistory":[],"pharmacokinetics":{"source":"DrugCentral","halfLife":"15.6 hours","clearance":"3.07 mL/min/kg","fractionUnbound":"1.0%","volumeOfDistribution":"2.77 L/kg"},"publicationCount":58,"therapeuticAreas":["Neuroscience"],"atcClassification":{"source":"DrugCentral","atcCode":"A04AD13","allCodes":["A04AD13"]},"biosimilarFilings":[],"recentPublications":[{"date":"2025 Aug","pmid":"39708024","title":"Pharmacological Strategies for Postdischarge Nausea and Vomiting: Evidence-based Review Update.","journal":"Journal of perianesthesia nursing : official journal of the American Society of PeriAnesthesia Nurses"},{"date":"2024 Feb","pmid":"37904319","title":"Homology modeling, virtual screening, molecular docking, and ADME approaches to identify a potent agent targeting NK2R protein.","journal":"Biotechnology and applied biochemistry"},{"date":"2022 Jul","pmid":"35045580","title":"Novel Antidepressants in the Pipeline (Phase II and III): A Systematic Review of the US Clinical Trials Registry.","journal":"Pharmacopsychiatry"},{"date":"2021 Nov 16","pmid":"34784425","title":"Antiemetics for adults for prevention of nausea and vomiting caused by moderately or highly emetogenic chemotherapy: a network meta-analysis.","journal":"The Cochrane database of systematic reviews"},{"date":"2020 Oct 19","pmid":"33075160","title":"Drugs for preventing postoperative nausea and vomiting in adults after general anaesthesia: a network meta-analysis.","journal":"The Cochrane database of systematic reviews"}],"companionDiagnostics":[],"genericManufacturerList":[],"status":"active","companyName":"","companyId":"","modality":"Small molecule","firstApprovalDate":"","enrichmentLevel":3,"visitCount":0,"regulatoryByCountry":[{"country_code":"EU","regulator":"EMA","status":"withdrawn","approval_date":"2009-12-31T00:00:00.000Z","mah":"Glaxo Group Ltd","brand_name_local":"Zunrisa","application_number":"EMEA/H/C/001040"}],"trialStats":{"total":0,"withResults":0},"verificationStatus":"partial","dataCompleteness":{"mechanism":true,"indications":false,"safety":false,"trials":true,"score":2}}