{"id":"amsacrine","rwe":[],"tags":[{"label":"amsacrine","category":"class"},{"label":"Small Molecule","category":"modality"},{"label":"DNA topoisomerase 1","category":"target"},{"label":"TOP1","category":"gene"},{"label":"TOP1MT","category":"gene"},{"label":"KCNH2","category":"gene"},{"label":"L01XX01","category":"atc"},{"label":"Active","category":"status"},{"label":"Antineoplastic Agents","category":"pharmacology"},{"label":"Indicators and Reagents","category":"pharmacology"},{"label":"Intercalating Agents","category":"pharmacology"}],"phase":"marketed","safety":{"safetySignals":[{"llr":194.883,"date":"","count":35,"signal":"Acute myeloid leukaemia recurrent","source":"DrugCentral FAERS","actionTaken":"Reported 35 times (LLR=195)"},{"llr":151.929,"date":"","count":35,"signal":"Venoocclusive liver disease","source":"DrugCentral FAERS","actionTaken":"Reported 35 times (LLR=152)"},{"llr":99.049,"date":"","count":33,"signal":"Drug resistance","source":"DrugCentral FAERS","actionTaken":"Reported 33 times (LLR=99)"},{"llr":98.531,"date":"","count":26,"signal":"Graft versus host disease","source":"DrugCentral FAERS","actionTaken":"Reported 26 times (LLR=99)"},{"llr":77.373,"date":"","count":15,"signal":"Cerebral toxoplasmosis","source":"DrugCentral FAERS","actionTaken":"Reported 15 times (LLR=77)"}],"commonSideEffects":[]},"trials":[],"aliases":[],"patents":[],"pricing":[],"_sources":{"trials":{"url":"https://clinicaltrials.gov/search?intr=AMSACRINE","method":"api_direct","source":"ClinicalTrials.gov","rawText":"","confidence":1,"sourceType":"ctgov","retrievedAt":"2026-04-19T23:31:21.345362+00:00"},"regulatory.ca":{"url":"","method":"api_direct","source":"Health Canada DPD","rawText":"","confidence":1,"sourceType":"health_canada_dpd","retrievedAt":"2026-04-19T23:31:27.063644+00:00"},"publicationCount":{"url":"https://pubmed.ncbi.nlm.nih.gov/?term=AMSACRINE","method":"api_direct","source":"PubMed/NCBI","rawText":"","confidence":1,"sourceType":"pubmed","retrievedAt":"2026-04-19T23:31:27.435263+00:00"},"crossReferences.chemblId":{"url":"https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL1256655/","method":"api_direct","source":"ChEMBL (EMBL-EBI)","rawText":"","confidence":1,"sourceType":"chembl","retrievedAt":"2026-04-19T23:31:28.138662+00:00"}},"allNames":"amekrin","offLabel":[],"synonyms":["amsacrine","acridinylanisidide","amekrin","amsidil","amsidine","amsidyl","lamasine"],"timeline":[{"date":"1987-01-01","type":"positive","source":"DrugCentral","milestone":"YEAR INTRODUCED approval"}],"aiSummary":"Amekrin (AMSACRINE) is a small molecule drug that targets DNA topoisomerase 1, a critical enzyme involved in DNA replication and repair. It is classified as an amsacrine drug and works by intercalating into DNA, thereby inhibiting the enzyme's activity and inducing DNA damage. Amekrin is used to treat certain types of cancer, although its commercial status and approved indications are unclear. The drug has a half-life of approximately 4.7 hours, but its bioavailability and generic manufacturing status are unknown. Further research is needed to determine its safety and efficacy profile.","brandName":"Amekrin","ecosystem":[],"mechanism":{"target":"DNA topoisomerase 2-beta, Solute carrier family 22 member 1, DNA topoisomerase II","targets":[{"gene":"TOP1","source":"DrugCentral","target":"DNA topoisomerase 1","protein":"DNA topoisomerase 1"},{"gene":"TOP1MT","source":"DrugCentral","target":"DNA topoisomerase I, mitochondrial","protein":"DNA topoisomerase I, mitochondrial"},{"gene":"KCNH2","source":"DrugCentral","target":"Potassium voltage-gated channel subfamily H member 2","protein":"Potassium voltage-gated channel subfamily H member 2"},{"gene":"TOP2A","source":"DrugCentral","target":"DNA topoisomerase II","protein":"DNA topoisomerase 2-alpha"},{"gene":"TOP2B","source":"DrugCentral","target":"DNA topoisomerase II","protein":"DNA topoisomerase 2-beta"},{"gene":"SLC22A1","source":"DrugCentral","target":"Solute carrier family 22 member 1","protein":"Solute carrier family 22 member 1"},{"gene":"CYP2D6","source":"DrugCentral","target":"Cytochrome P450 2D6","protein":"Cytochrome P450 2D6"}],"modality":"Small Molecule","drugClass":"amsacrine","explanation":"","oneSentence":"","technicalDetail":"Amekrin intercalates into DNA by inserting its planar aromatic ring system between adjacent base pairs, thereby stabilizing a cleavage complex and inhibiting the religation step of the topoisomerase 1 reaction."},"commercial":{},"references":[{"id":1,"url":"https://drugcentral.org/drugcard/203","fields":["approvals","synonyms","ATC","PK","indications","contraindications","DDIs","targets","patents","FAERS"],"source":"DrugCentral"},{"id":2,"url":"https://clinicaltrials.gov/search?intr=AMSACRINE","fields":["trials"],"source":"ClinicalTrials.gov"},{"id":3,"url":"https://pubmed.ncbi.nlm.nih.gov/?term=AMSACRINE","fields":["publications"],"source":"PubMed/NCBI"}],"_enrichedAt":"2026-03-30T08:43:26.518831","_validation":{"fieldsValidated":0,"lastValidatedAt":"2026-04-19T23:31:29.787227+00:00","fieldsConflicting":2,"overallConfidence":0.8},"biosimilars":[],"competitors":[{"drugName":"asparaginase","drugSlug":"asparaginase","fdaApproval":"1994-02-01","relationship":"same-class"},{"drugName":"altretamine","drugSlug":"altretamine","fdaApproval":"1990-12-26","patentStatus":"Unknown","relationship":"same-class"},{"drugName":"hydroxycarbamide","drugSlug":"hydroxycarbamide","fdaApproval":"1967-12-07","relationship":"same-class"},{"drugName":"pentostatin","drugSlug":"pentostatin","fdaApproval":"1991-10-11","genericCount":2,"patentStatus":"Off-patent 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