{"id":"cyclomethycaine","rwe":[{"pmid":"6138200","year":"1983","title":"A comparison in rat and mouse heart of the ability of several local anesthetics to inhibit monoamine oxidase.","finding":"","journal":"Comparative biochemistry and physiology. C, Comparative pharmacology and toxicology","studyType":"Clinical Study"},{"pmid":"978414","year":"1976","title":"In vitro release of therapeutically active ingredients from polymer matrixes.","finding":"","journal":"Journal of pharmaceutical sciences","studyType":"Clinical Study"},{"pmid":"235555","year":"1975","title":"Cell to substrate adhesion and spreading: inhibition by cationic anesthetics.","finding":"","journal":"Journal of cellular physiology","studyType":"Clinical Study"},{"pmid":"13415978","year":"1957","title":"CYCLOMETHYCAINE sulfate.","finding":"","journal":"Journal of the American Medical Association","studyType":"Clinical Study"}],"tags":[{"label":"cyclomethycaine","category":"class"},{"label":"Small Molecule","category":"modality"},{"label":"Sodium channel alpha subunits; brain (Types I, II, III)","category":"target"},{"label":"SCN1A","category":"gene"},{"label":"SCN2A","category":"gene"},{"label":"SCN3A","category":"gene"},{"label":"Active","category":"status"}],"phase":"phase_2","safety":{"contraindications":["Conduction disorder of the heart","Decreased respiratory function","Denuded skin","Open wound","Seizure disorder"]},"trials":[],"aliases":[],"patents":[],"pricing":[],"allNames":"topocaine","offLabel":[],"synonyms":["cyclomethycaine sulfate","cyclomethycaine","topocaine"],"timeline":[],"approvals":[],"brandName":"Topocaine","ecosystem":[],"mechanism":{"target":"Sodium channel alpha subunits; brain (Types I, II, III)","targets":[{"gene":"SCN1A","source":"DrugCentral","target":"Sodium channel alpha subunits; brain (Types I, II, III)","protein":"Sodium channel protein type 1 subunit alpha"},{"gene":"SCN2A","source":"DrugCentral","target":"Sodium channel alpha subunits; brain (Types I, II, III)","protein":"Sodium channel protein type 2 subunit alpha"},{"gene":"SCN3A","source":"DrugCentral","target":"Sodium channel alpha subunits; brain (Types I, II, III)","protein":"Sodium channel protein type 3 subunit alpha"}],"modality":"Small Molecule","drugClass":"cyclomethycaine","explanation":"Imagine your nerves are like electrical wires that send signals to your brain. Sodium channels are like the switches that turn these signals on and off. Topocaine works by flipping these switches to the 'off' position, which can help relieve pain.","oneSentence":"Topocaine blocks sodium channels in the brain to prevent pain signals from being transmitted.","technicalDetail":"Topocaine specifically targets the sodium channel alpha subunits (Types I, II, III) in the brain, blocking the influx of sodium ions and preventing the depolarization of neurons, which is responsible for the transmission of pain signals."},"commercial":{},"references":[{"id":1,"url":"https://drugcentral.org/drugcard/3123","fields":["approvals","synonyms","ATC","PK","indications","contraindications","DDIs","targets","patents","FAERS"],"source":"DrugCentral"},{"id":2,"url":"https://pubmed.ncbi.nlm.nih.gov/?term=CYCLOMETHYCAINE","fields":["publications"],"source":"PubMed/NCBI"}],"_enrichedAt":"2026-03-30T10:24:54.408260","biosimilars":[],"competitors":[{"drugName":"articaine","drugSlug":"articaine","fdaApproval":"2000-04-03","patentExpiry":"Mar 27, 2039","patentStatus":"Patent protected","relationship":"same-target"},{"drugName":"bepridil","drugSlug":"bepridil","fdaApproval":"1990-12-28","patentStatus":"Unknown","relationship":"same-target"},{"drugName":"brompheniramine","drugSlug":"brompheniramine","fdaApproval":"1957-08-23","genericCount":13,"patentStatus":"Off-patent — generic available","relationship":"same-target"},{"drugName":"butacaine","drugSlug":"butacaine","fdaApproval":"","relationship":"same-target"},{"drugName":"chlorphenamine","drugSlug":"chlorphenamine","fdaApproval":"1950-08-15","relationship":"same-target"},{"drugName":"chlorpromazine","drugSlug":"chlorpromazine","fdaApproval":"1957-09-18","patentStatus":"Unknown","relationship":"same-target"},{"drugName":"cinchocaine","drugSlug":"cinchocaine","fdaApproval":"","relationship":"same-target"},{"drugName":"cyproheptadine","drugSlug":"cyproheptadine","fdaApproval":"1961-10-17","genericCount":31,"patentStatus":"Off-patent — generic available","relationship":"same-target"},{"drugName":"desipramine","drugSlug":"desipramine","fdaApproval":"1964-11-20","genericCount":8,"patentStatus":"Off-patent — generic available","relationship":"same-target"},{"drugName":"dicycloverine","drugSlug":"dicycloverine","fdaApproval":"1950-05-11","relationship":"same-target"}],"dataSources":[{"url":"https://drugcentral.org","name":"DrugCentral","fields":["indications","contraindications","safety","target","drugInteractions"],"retrievedDate":"2026-04-07"}],"genericName":"cyclomethycaine","indications":{"approved":[],"offLabel":[],"pipeline":[]},"drugCategory":"active","labelChanges":[],"relatedDrugs":[{"drugId":"articaine","brandName":"articaine","genericName":"articaine","approvalYear":"2000","relationship":"same-target"},{"drugId":"bepridil","brandName":"bepridil","genericName":"bepridil","approvalYear":"1990","relationship":"same-target"},{"drugId":"brompheniramine","brandName":"brompheniramine","genericName":"brompheniramine","approvalYear":"1957","relationship":"same-target"},{"drugId":"butacaine","brandName":"butacaine","genericName":"butacaine","approvalYear":"","relationship":"same-target"},{"drugId":"chlorphenamine","brandName":"chlorphenamine","genericName":"chlorphenamine","approvalYear":"1950","relationship":"same-target"},{"drugId":"chlorpromazine","brandName":"chlorpromazine","genericName":"chlorpromazine","approvalYear":"1957","relationship":"same-target"},{"drugId":"cinchocaine","brandName":"cinchocaine","genericName":"cinchocaine","approvalYear":"","relationship":"same-target"},{"drugId":"cyproheptadine","brandName":"cyproheptadine","genericName":"cyproheptadine","approvalYear":"1961","relationship":"same-target"},{"drugId":"desipramine","brandName":"desipramine","genericName":"desipramine","approvalYear":"1964","relationship":"same-target"},{"drugId":"dicycloverine","brandName":"dicycloverine","genericName":"dicycloverine","approvalYear":"1950","relationship":"same-target"}],"trialDetails":[],"genericFilers":[],"latestUpdates":[],"manufacturing":[],"administration":{},"crossReferences":{"NDDF":"001365","UNII":"15E9I74NZ8","CHEBI":"CHEBI:135520","INN_ID":"659","RXNORM":"21990","UMLSCUI":"C0056780","ChEMBL_ID":"CHEMBL127487","PUBCHEM_CID":"10839","SNOMEDCT_US":"54197005","SECONDARY_CAS_RN":"6202-05-7","MESH_SUPPLEMENTAL_RECORD_UI":"C013463"},"formularyStatus":[],"_enricherVersion":"v2","developmentCodes":[],"ownershipHistory":[],"publicationCount":4,"therapeuticAreas":["Neuroscience"],"biosimilarFilings":[],"recentPublications":[{"date":"1983","pmid":"6138200","title":"A comparison in rat and mouse heart of the ability of several local anesthetics to inhibit monoamine oxidase.","journal":"Comparative biochemistry and physiology. C, Comparative pharmacology and toxicology"},{"date":"1976 Oct","pmid":"978414","title":"In vitro release of therapeutically active ingredients from polymer matrixes.","journal":"Journal of pharmaceutical sciences"},{"date":"1975 Apr","pmid":"235555","title":"Cell to substrate adhesion and spreading: inhibition by cationic anesthetics.","journal":"Journal of cellular physiology"},{"date":"1957 May 18","pmid":"13415978","title":"CYCLOMETHYCAINE sulfate.","journal":"Journal of the American Medical Association"}],"companionDiagnostics":[],"genericManufacturerList":[],"status":"active","companyName":"","companyId":"","modality":"Small molecule","firstApprovalDate":"","aiSummary":"Topocaine (CYCLOMETHYCAINE) is a cyclomethycaine, a small molecule that targets sodium channel alpha subunits in the brain. It is believed to work by blocking these channels, which are responsible for transmitting pain signals. However, due to a lack of FDA approval information, its approved indications and commercial status are unknown. As a result, key safety considerations and pharmacokinetic properties, such as half-life and bioavailability, are also unclear. Further research is needed to fully understand this medication.","enrichmentLevel":3,"visitCount":0,"trialStats":{"total":0,"withResults":0},"verificationStatus":"partial","dataCompleteness":{"mechanism":true,"indications":false,"safety":false,"trials":false,"score":1}}