{"id":"melperone","rwe":[],"tags":[{"label":"melperone","category":"class"},{"label":"Small Molecule","category":"modality"},{"label":"D(3) dopamine receptor","category":"target"},{"label":"DRD3","category":"gene"},{"label":"DRD2","category":"gene"},{"label":"ADRA2A","category":"gene"},{"label":"N05AD03","category":"atc"},{"label":"Active","category":"status"}],"phase":"discontinued","safety":{"safetySignals":[{"llr":179.868,"date":"","count":124,"signal":"General physical health deterioration","source":"DrugCentral FAERS","actionTaken":"Reported 124 times (LLR=180)"},{"llr":120.386,"date":"","count":34,"signal":"Systemic infection","source":"DrugCentral FAERS","actionTaken":"Reported 34 times (LLR=120)"},{"llr":104.473,"date":"","count":117,"signal":"Fall","source":"DrugCentral FAERS","actionTaken":"Reported 117 times (LLR=104)"},{"llr":97.129,"date":"","count":22,"signal":"Pleurothotonus","source":"DrugCentral FAERS","actionTaken":"Reported 22 times (LLR=97)"},{"llr":90.646,"date":"","count":97,"signal":"Drug interaction","source":"DrugCentral FAERS","actionTaken":"Reported 97 times (LLR=91)"},{"llr":80.173,"date":"","count":38,"signal":"Epilepsy","source":"DrugCentral FAERS","actionTaken":"Reported 38 times (LLR=80)"},{"llr":77.685,"date":"","count":40,"signal":"Haematemesis","source":"DrugCentral FAERS","actionTaken":"Reported 40 times (LLR=78)"},{"llr":72.602,"date":"","count":15,"signal":"Sleep-related eating disorder","source":"DrugCentral FAERS","actionTaken":"Reported 15 times (LLR=73)"},{"llr":61.546,"date":"","count":36,"signal":"Disorientation","source":"DrugCentral FAERS","actionTaken":"Reported 36 times (LLR=62)"},{"llr":58.403,"date":"","count":26,"signal":"Labelled drug-drug interaction medication error","source":"DrugCentral FAERS","actionTaken":"Reported 26 times (LLR=58)"},{"llr":56.411,"date":"","count":36,"signal":"Medication error","source":"DrugCentral FAERS","actionTaken":"Reported 36 times (LLR=56)"},{"llr":55.042,"date":"","count":12,"signal":"Peripheral circulatory failure","source":"DrugCentral FAERS","actionTaken":"Reported 12 times (LLR=55)"},{"llr":53.563,"date":"","count":38,"signal":"Depressed level of consciousness","source":"DrugCentral FAERS","actionTaken":"Reported 38 times (LLR=54)"},{"llr":51.81,"date":"","count":50,"signal":"Syncope","source":"DrugCentral FAERS","actionTaken":"Reported 50 times (LLR=52)"},{"llr":50.397,"date":"","count":75,"signal":"Hypotension","source":"DrugCentral FAERS","actionTaken":"Reported 75 times (LLR=50)"}],"commonSideEffects":[{"effect":"General physical health deterioration","drugRate":"LLR 180","severity":"common"},{"effect":"Systemic infection","drugRate":"LLR 120","severity":"common"},{"effect":"Fall","drugRate":"LLR 104","severity":"common"},{"effect":"Pleurothotonus","drugRate":"LLR 97","severity":"common"},{"effect":"Drug interaction","drugRate":"LLR 91","severity":"common"},{"effect":"Epilepsy","drugRate":"LLR 80","severity":"common"},{"effect":"Haematemesis","drugRate":"LLR 78","severity":"common"},{"effect":"Sleep-related eating disorder","drugRate":"LLR 73","severity":"common"},{"effect":"Disorientation","drugRate":"LLR 62","severity":"common"},{"effect":"Medication error","drugRate":"LLR 56","severity":"common"},{"effect":"Peripheral circulatory failure","drugRate":"LLR 55","severity":"common"},{"effect":"Depressed level of consciousness","drugRate":"LLR 54","severity":"common"},{"effect":"Syncope","drugRate":"LLR 52","severity":"common"},{"effect":"Hypotension","drugRate":"LLR 50","severity":"common"}]},"trials":[],"aliases":[],"patents":[],"pricing":[],"allNames":"flubuperone","offLabel":[],"synonyms":["melperone","flubuperone","methylperone"],"timeline":[{"date":"1972-01-01","type":"positive","source":"DrugCentral","milestone":"YEAR INTRODUCED approval"}],"aiSummary":"Flubuperone, also known as Melperone, is a small molecule targeting the D(3) dopamine receptor. It belongs to the melperone drug class and is used to treat various psychiatric conditions. However, its commercial status and approved indications are unknown. The half-life of Flubuperone is approximately 3.9 hours, but its bioavailability and off-patent status are not available. As a result, its availability and usage are limited.","approvals":[{"date":"1972-01-01","orphan":false,"company":"","regulator":"YEAR INTRODUCED"}],"brandName":"Flubuperone","ecosystem":[],"mechanism":{"target":"D(4) dopamine receptor, 5-hydroxytryptamine receptor 1A, 5-hydroxytryptamine receptor 1D","targets":[{"gene":"DRD3","source":"DrugCentral","target":"D(3) dopamine receptor","protein":"D(3) dopamine receptor"},{"gene":"DRD2","source":"DrugCentral","target":"D(2) dopamine receptor","protein":"D(2) dopamine receptor"},{"gene":"ADRA2A","source":"DrugCentral","target":"Alpha-2A adrenergic receptor","protein":"Alpha-2A adrenergic receptor"},{"gene":"ADRA1A","source":"DrugCentral","target":"Alpha-1A adrenergic receptor","protein":"Alpha-1A adrenergic receptor"},{"gene":"HTR2A","source":"DrugCentral","target":"5-hydroxytryptamine receptor 2A","protein":"5-hydroxytryptamine receptor 2A"},{"gene":"DRD4","source":"DrugCentral","target":"D(4) dopamine receptor","protein":"D(4) dopamine receptor"},{"gene":"HRH1","source":"DrugCentral","target":"Histamine H1 receptor","protein":"Histamine H1 receptor"},{"gene":"HTR2C","source":"DrugCentral","target":"5-hydroxytryptamine receptor 2C","protein":"5-hydroxytryptamine receptor 2C"},{"gene":"HTR1A","source":"DrugCentral","target":"5-hydroxytryptamine receptor 1A","protein":"5-hydroxytryptamine receptor 1A"},{"gene":"CHRM2","source":"DrugCentral","target":"Muscarinic acetylcholine receptor M2","protein":"Muscarinic acetylcholine receptor M2"}],"modality":"Small Molecule","drugClass":"melperone","explanation":"Imagine your brain has a system to control emotions and mood. Flubuperone helps by blocking a specific part of this system, called the D(3) dopamine receptor, which can become overactive in certain conditions. This helps to calm down excessive emotional responses and stabilize mood.","oneSentence":"Flubuperone works by selectively blocking the D(3) dopamine receptor, which helps regulate mood and emotional responses.","technicalDetail":"Flubuperone acts as a selective antagonist at the D(3) dopamine receptor, which is a subtype of dopamine receptor involved in the regulation of mood, motivation, and reward processing."},"commercial":{},"references":[{"id":1,"url":"https://drugcentral.org/drugcard/1677","fields":["approvals","synonyms","ATC","PK","indications","contraindications","DDIs","targets","patents","FAERS"],"source":"DrugCentral"},{"id":2,"url":"https://clinicaltrials.gov/search?intr=MELPERONE","fields":["trials"],"source":"ClinicalTrials.gov"},{"id":3,"url":"https://pubmed.ncbi.nlm.nih.gov/?term=MELPERONE","fields":["publications"],"source":"PubMed/NCBI"}],"_enrichedAt":"2026-03-30T15:01:35.276179","biosimilars":[],"competitors":[{"drugName":"haloperidol","drugSlug":"haloperidol","fdaApproval":"1967-04-12","genericCount":20,"patentStatus":"Off-patent — generic available","relationship":"same-class"},{"drugName":"droperidol","drugSlug":"droperidol","fdaApproval":"1970-06-11","genericCount":10,"patentStatus":"Off-patent — generic available","relationship":"same-class"},{"drugName":"lumateperone","drugSlug":"lumateperone","fdaApproval":"2019-12-20","patentExpiry":"Oct 27, 2039","patentStatus":"Patent protected","relationship":"same-class"}],"dataSources":[{"url":"https://drugcentral.org","name":"DrugCentral","fields":["indications","contraindications","safety","target","drugInteractions"],"retrievedDate":"2026-04-07"}],"genericName":"melperone","indications":{"approved":[],"offLabel":[],"pipeline":[]},"drugCategory":"active","labelChanges":[],"relatedDrugs":[{"drugId":"haloperidol","brandName":"haloperidol","genericName":"haloperidol","approvalYear":"1967","relationship":"same-class"},{"drugId":"droperidol","brandName":"droperidol","genericName":"droperidol","approvalYear":"1970","relationship":"same-class"},{"drugId":"lumateperone","brandName":"lumateperone","genericName":"lumateperone","approvalYear":"2019","relationship":"same-class"}],"trialDetails":[{"nctId":"NCT02435095","phase":"PHASE4","title":"Antipsychotic Induced Structural and Functional Brain Changes","status":"TERMINATED","sponsor":"RWTH Aachen University","startDate":"2015-05","conditions":["Schizophrenia"],"enrollment":174,"completionDate":"2020-08"},{"nctId":"NCT02374567","phase":"PHASE3","title":"Pharmacovigilance in Gerontopsychiatric Patients","status":"TERMINATED","sponsor":"Hannover Medical School","startDate":"2015-01","conditions":["Dementia","Depression","Schizophrenia","Psychosomatic Disorders","Anxiety Disorders"],"enrollment":407,"completionDate":"2017-06-28"},{"nctId":"NCT01323205","phase":"PHASE2","title":"Investigation of the Safety, Tolerability and Potential Therapeutic Effects of JNJ-40411813 in Patients With Schizophrenia","status":"COMPLETED","sponsor":"Janssen Research & Development, LLC","startDate":"2011-05","conditions":["Schizophrenia"],"enrollment":100,"completionDate":"2012-12"},{"nctId":"NCT00125138","phase":"PHASE2","title":"Melperone (an Anti-Psychotic) in Patients With Psychosis Associated With Parkinson's Disease","status":"COMPLETED","sponsor":"Lundbeck LLC","startDate":"2005-07","conditions":["Parkinson's Disease","Psychotic Disorders"],"enrollment":90,"completionDate":"2008-04"}],"genericFilers":[],"latestUpdates":[],"manufacturing":[],"administration":{},"crossReferences":{"NDDF":"006742","UNII":"J8WA3K39B7","CHEBI":"CHEBI:93626","INN_ID":"2070","RXNORM":"29961","UMLSCUI":"C0066477","ChEMBL_ID":"CHEMBL1531134","KEGG_DRUG":"D07309","DRUGBANK_ID":"DB09224","PUBCHEM_CID":"15387","SNOMEDCT_US":"441821005"},"formularyStatus":[],"_enricherVersion":"v2","developmentCodes":[],"ownershipHistory":[],"pharmacokinetics":{"source":"DrugCentral","halfLife":"3.9 hours","clearance":"46.0 mL/min/kg","volumeOfDistribution":"14.0 L/kg"},"publicationCount":161,"therapeuticAreas":["Other"],"atcClassification":{"source":"DrugCentral","atcCode":"N05AD03","allCodes":["N05AD03"]},"biosimilarFilings":[],"recentPublications":[],"companionDiagnostics":[],"genericManufacturerList":[],"status":"discontinued","companyName":"","companyId":"","modality":"Small molecule","firstApprovalDate":"","enrichmentLevel":3,"visitCount":0,"regulatoryByCountry":[{"country_code":"OTHER","regulator":"YEAR INTRODUCED","status":"approved","approval_date":"1972-01-01T00:00:00.000Z","mah":"","brand_name_local":null,"application_number":""}],"trialStats":{"total":0,"withResults":0},"verificationStatus":"verified","dataCompleteness":{"mechanism":true,"indications":false,"safety":true,"trials":true,"score":3}}