{"id":"bisulepine","rwe":[],"tags":[{"label":"Small Molecule","category":"modality"},{"label":"Histamine H1 receptor","category":"target"},{"label":"HRH1","category":"gene"},{"label":"Active","category":"status"}],"phase":"unknown","safety":{"safetySignals":[{"llr":68.844,"date":"","count":20,"signal":"Cytokine release syndrome","source":"DrugCentral FAERS","actionTaken":"Reported 20 times (LLR=69)"},{"llr":54.001,"date":"","count":16,"signal":"COVID-19 pneumonia","source":"DrugCentral FAERS","actionTaken":"Reported 16 times (LLR=54)"},{"llr":53.044,"date":"","count":11,"signal":"Haemolytic uraemic syndrome","source":"DrugCentral FAERS","actionTaken":"Reported 11 times (LLR=53)"},{"llr":44.006,"date":"","count":10,"signal":"Oligohydramnios","source":"DrugCentral FAERS","actionTaken":"Reported 10 times (LLR=44)"}],"commonSideEffects":[{"effect":"Cytokine release syndrome","drugRate":"LLR 69","severity":"common"},{"effect":"COVID-19 pneumonia","drugRate":"LLR 54","severity":"common"},{"effect":"Haemolytic uraemic syndrome","drugRate":"LLR 53","severity":"common"},{"effect":"Oligohydramnios","drugRate":"LLR 44","severity":"common"}]},"trials":[],"aliases":[],"patents":[],"pricing":[],"_fixedAt":"2026-03-30T16:38:25.374709","allNames":"bisulepin","offLabel":[],"synonyms":["bisulepin","bisulepine","dithiaden"],"timeline":[],"brandName":"Bisulepin","ecosystem":[],"mechanism":{"target":"Histamine H1 receptor","targets":[{"gene":"HRH1","source":"DrugCentral","target":"Histamine H1 receptor","protein":"Histamine H1 receptor","isPrimary":true,"activityType":"","activityValue":null}],"modality":"Small Molecule","explanation":"Think of histamine like a messenger in your body that helps control things like sleep, appetite, and how your body reacts to allergens. Bisulepin blocks this messenger from doing its job, which can help with certain conditions. However, this can also have unintended effects, so it's essential to understand how bisulepin interacts with the body before using it.","oneSentence":"Bisulepin works by binding to the histamine H1 receptor, which is involved in regulating various physiological processes, including sleep, appetite, and immune responses.","technicalDetail":"Bisulepin acts as a competitive antagonist at the histamine H1 receptor, which is a G-protein coupled receptor involved in the regulation of smooth muscle contraction, vascular permeability, and immune responses."},"_wikipedia":{"url":"https://en.wikipedia.org/wiki/Bisulepin","title":"Bisulepin","extract":"Bisulepin is strong and relatively selective antihistamine (H1 antagonist) with hypnotic, antiadrenergic and very weak anticholinergic and antiserotonergic effects. Bisulepin is marketed in the Czech Republic and Slovakia under the trademark Dithiaden as tablets and injections."},"commercial":{},"references":[{"id":1,"url":"https://drugcentral.org/drugcard/383","fields":["approvals","synonyms","ATC","PK","indications","contraindications","DDIs","targets","patents","FAERS"],"source":"DrugCentral"},{"id":2,"url":"https://pubmed.ncbi.nlm.nih.gov/?term=bisulepine","fields":["publications"],"source":"PubMed/NCBI"},{"id":3,"url":"https://en.wikipedia.org/wiki/Bisulepin","fields":["history","overview"],"source":"Wikipedia"}],"_enrichedAt":"2026-03-30T09:01:33.597084","biosimilars":[],"competitors":[{"drugName":"acrivastine","drugSlug":"acrivastine","fdaApproval":"1994-03-25","relationship":"same-target"},{"drugName":"alcaftadine","drugSlug":"alcaftadine","fdaApproval":"2010-07-28","patentExpiry":"Mar 19, 2027","patentStatus":"Patent protected","relationship":"same-target"},{"drugName":"alimemazine","drugSlug":"alimemazine","fdaApproval":"","relationship":"same-target"},{"drugName":"amitriptyline","drugSlug":"amitriptyline","fdaApproval":"1961-04-07","genericCount":33,"patentStatus":"Off-patent — generic available","relationship":"same-target"},{"drugName":"amoxapine","drugSlug":"amoxapine","fdaApproval":"1980-09-22","genericCount":3,"patentStatus":"Off-patent — generic available","relationship":"same-target"},{"drugName":"antazoline","drugSlug":"antazoline","fdaApproval":"1990-04-30","relationship":"same-target"},{"drugName":"aripiprazole","drugSlug":"aripiprazole","fdaApproval":"2002-11-15","patentExpiry":"Sep 24, 2033","patentStatus":"Patent protected","relationship":"same-target"},{"drugName":"aripiprazole lauroxil","drugSlug":"aripiprazole-lauroxil","fdaApproval":"2015-10-05","patentExpiry":"Sep 8, 2035","patentStatus":"Patent protected","relationship":"same-target"},{"drugName":"asenapine","drugSlug":"asenapine","fdaApproval":"2009-08-13","patentExpiry":"Sep 22, 2033","patentStatus":"Patent protected","relationship":"same-target"},{"drugName":"astemizole","drugSlug":"astemizole","fdaApproval":"1988-12-31","relationship":"same-target"}],"dataSources":[{"url":"https://drugcentral.org","name":"DrugCentral","fields":["indications","contraindications","safety","target","drugInteractions"],"retrievedDate":"2026-04-07"}],"genericName":"bisulepine","indications":{"approved":[],"offLabel":[],"pipeline":[]},"_fixedFields":["primaryTarget"],"drugCategory":"active","labelChanges":[],"relatedDrugs":[{"drugId":"acrivastine","brandName":"acrivastine","genericName":"acrivastine","approvalYear":"1994","relationship":"same-target"},{"drugId":"alcaftadine","brandName":"alcaftadine","genericName":"alcaftadine","approvalYear":"2010","relationship":"same-target"},{"drugId":"alimemazine","brandName":"alimemazine","genericName":"alimemazine","approvalYear":"","relationship":"same-target"},{"drugId":"amitriptyline","brandName":"amitriptyline","genericName":"amitriptyline","approvalYear":"1961","relationship":"same-target"},{"drugId":"amoxapine","brandName":"amoxapine","genericName":"amoxapine","approvalYear":"1980","relationship":"same-target"},{"drugId":"antazoline","brandName":"antazoline","genericName":"antazoline","approvalYear":"1990","relationship":"same-target"},{"drugId":"aripiprazole","brandName":"aripiprazole","genericName":"aripiprazole","approvalYear":"2002","relationship":"same-target"},{"drugId":"aripiprazole-lauroxil","brandName":"aripiprazole lauroxil","genericName":"aripiprazole lauroxil","approvalYear":"2015","relationship":"same-target"},{"drugId":"asenapine","brandName":"asenapine","genericName":"asenapine","approvalYear":"2009","relationship":"same-target"},{"drugId":"astemizole","brandName":"astemizole","genericName":"astemizole","approvalYear":"1988","relationship":"same-target"}],"trialDetails":[],"genericFilers":[],"latestUpdates":[],"manufacturing":[],"administration":{},"crossReferences":{"UNII":"595726R32U","CHEBI":"CHEBI:135277","UMLSCUI":"C0058491","KEGG_DRUG":"D07532","PUBCHEM_CID":"6537425","SECONDARY_CAS_RN":"42504-83-6"},"formularyStatus":[],"_enricherVersion":"v2","developmentCodes":[],"ownershipHistory":[],"publicationCount":0,"therapeuticAreas":["Immunology"],"biosimilarFilings":[],"recentPublications":[],"companionDiagnostics":[],"genericManufacturerList":[],"status":"active","companyName":"","companyId":"unknown","modality":"Small Molecule","firstApprovalDate":"","aiSummary":"Bisulepin (bisulepine) is a small molecule modality targeting the histamine H1 receptor. Its exact drug class is unknown, and its commercial status is unclear. Bisulepin is not FDA-approved for any indications, and its pharmacokinetic properties, such as half-life and bioavailability, are also unknown. As a result, there is limited information available on its safety profile and potential side effects. Further research is needed to fully understand the properties and potential uses of bisulepin.","enrichmentLevel":3,"visitCount":0,"trialStats":{"total":0,"withResults":0},"verificationStatus":"partial","dataCompleteness":{"mechanism":true,"indications":false,"safety":true,"trials":false,"score":2}}