{"id":"intoplicine","rwe":[{"pmid":"12570767","year":"2003","title":"Dual topoisomerase I/II inhibitors in cancer therapy.","finding":"","journal":"Current topics in medicinal chemistry","studyType":"Clinical Study"},{"pmid":"10630356","year":"1999","title":"Phase I trial of intoplicine (RP 60475) administered as a 72 h infusion every 3 weeks in patients with solid tumors.","finding":"","journal":"Anti-cancer drugs","studyType":"Clinical Study"},{"pmid":"10194543","year":"1999","title":"Topoisomerase I/II inhibitor intoplicine administered as a 24 h infusion: phase I and pharmacologic study.","finding":"","journal":"Anti-cancer drugs","studyType":"Clinical Study"},{"pmid":"9140928","year":"1997","title":"Complementary advantages of fluorescence and SIMS microscopies in the study of cellular localization of two new antitumor drugs.","finding":"","journal":"Microscopy research and technique","studyType":"Clinical Study"},{"pmid":"8740721","year":"1996","title":"Phase I and pharmacology study of intoplicine (RP 60475; NSC 645008), novel topoisomerase I and II inhibitor, in cancer patients.","finding":"","journal":"Anti-cancer drugs","studyType":"Clinical Study"}],"tags":[{"label":"intoplicine","category":"class"},{"label":"Small Molecule","category":"modality"},{"label":"DNA topoisomerase 1","category":"target"},{"label":"TOP1","category":"gene"},{"label":"TOP1MT","category":"gene"},{"label":"TOP2A","category":"gene"},{"label":"Active","category":"status"}],"phase":"phase_2","safety":{},"trials":[],"aliases":[],"patents":[],"pricing":[],"allNames":["intoplicine","RP-60475"],"offLabel":[],"synonyms":["intoplicine","RP-60475"],"timeline":[],"approvals":[],"ecosystem":[],"mechanism":{"target":"DNA topoisomerase 1, DNA topoisomerase 2-alpha, DNA topoisomerase I, mitochondrial","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":"TOP2A","source":"DrugCentral","target":"DNA topoisomerase 2-alpha","protein":"DNA topoisomerase 2-alpha"}],"modality":"Small Molecule","drugClass":"intoplicine","explanation":"Think of DNA topoisomerase 1 like a pair of scissors that helps cut and repair DNA. INTOPLICINE blocks these scissors, making it harder for cancer cells to grow and divide. This can help slow or stop the growth of cancer.","oneSentence":"INTOPLICINE works by binding to and inhibiting DNA topoisomerase 1, an enzyme that helps cancer cells replicate and repair their DNA.","technicalDetail":"INTOPLICINE binds to the ATP-binding site of DNA topoisomerase 1, preventing the enzyme from interacting with DNA and thereby inhibiting its catalytic activity, which is essential for DNA replication and repair."},"commercial":{},"references":[{"id":1,"url":"https://drugcentral.org/drugcard/1446","fields":["approvals","synonyms","ATC","PK","indications","contraindications","DDIs","targets","patents","FAERS"],"source":"DrugCentral"},{"id":2,"url":"https://clinicaltrials.gov/search?intr=INTOPLICINE","fields":["trials"],"source":"ClinicalTrials.gov"},{"id":3,"url":"https://pubmed.ncbi.nlm.nih.gov/?term=INTOPLICINE","fields":["publications"],"source":"PubMed/NCBI"}],"_enrichedAt":"2026-03-30T13:58:49.072661","biosimilars":[],"competitors":[{"drugName":"daunorubicin","drugSlug":"daunorubicin","fdaApproval":"1979-12-19","patentStatus":"Unknown","relationship":"same-target"},{"drugName":"dexrazoxane","drugSlug":"dexrazoxane","fdaApproval":"1995-05-26","genericCount":4,"patentStatus":"Off-patent — generic available","relationship":"same-target"},{"drugName":"doxorubicin","drugSlug":"doxorubicin","fdaApproval":"1974-08-07","genericCount":24,"patentStatus":"Off-patent — generic available","relationship":"same-target"},{"drugName":"etoposide","drugSlug":"etoposide","fdaApproval":"1983-11-10","genericCount":14,"patentStatus":"Off-patent — generic available","relationship":"same-target"},{"drugName":"etoposide phosphate","drugSlug":"etoposide-phosphate","fdaApproval":"1996-05-17","patentStatus":"Unknown","relationship":"same-target"},{"drugName":"idarubicin","drugSlug":"idarubicin","fdaApproval":"1990-09-27","genericCount":6,"patentStatus":"Off-patent — generic available","relationship":"same-target"},{"drugName":"mitoxantrone","drugSlug":"mitoxantrone","fdaApproval":"1987-12-23","genericCount":6,"patentStatus":"Off-patent — generic available","relationship":"same-target"},{"drugName":"teniposide","drugSlug":"teniposide","fdaApproval":"1992-07-14","patentStatus":"Unknown","relationship":"same-target"},{"drugName":"valrubicin","drugSlug":"valrubicin","fdaApproval":"1998-09-25","genericCount":1,"patentStatus":"Off-patent — generic available","relationship":"same-target"}],"dataSources":[{"url":"https://drugcentral.org","name":"DrugCentral","fields":["indications","contraindications","safety","target","drugInteractions"],"retrievedDate":"2026-04-07"}],"genericName":"intoplicine","indications":{"approved":[],"offLabel":[],"pipeline":[]},"drugCategory":"active","labelChanges":[],"relatedDrugs":[{"drugId":"daunorubicin","brandName":"daunorubicin","genericName":"daunorubicin","approvalYear":"1979","relationship":"same-target"},{"drugId":"dexrazoxane","brandName":"dexrazoxane","genericName":"dexrazoxane","approvalYear":"1995","relationship":"same-target"},{"drugId":"doxorubicin","brandName":"doxorubicin","genericName":"doxorubicin","approvalYear":"1974","relationship":"same-target"},{"drugId":"etoposide","brandName":"etoposide","genericName":"etoposide","approvalYear":"1983","relationship":"same-target"},{"drugId":"etoposide-phosphate","brandName":"etoposide phosphate","genericName":"etoposide phosphate","approvalYear":"1996","relationship":"same-target"},{"drugId":"idarubicin","brandName":"idarubicin","genericName":"idarubicin","approvalYear":"1990","relationship":"same-target"},{"drugId":"mitoxantrone","brandName":"mitoxantrone","genericName":"mitoxantrone","approvalYear":"1987","relationship":"same-target"},{"drugId":"teniposide","brandName":"teniposide","genericName":"teniposide","approvalYear":"1992","relationship":"same-target"},{"drugId":"valrubicin","brandName":"valrubicin","genericName":"valrubicin","approvalYear":"1998","relationship":"same-target"}],"trialDetails":[{"nctId":"NCT00003713","phase":"PHASE1","title":"Chemotherapy in Treating Patients With Advanced or Metastatic Solid Tumors","status":"COMPLETED","sponsor":"Genzyme, a Sanofi Company","startDate":"1997-08","conditions":["Unspecified Adult Solid Tumor, Protocol Specific"],"enrollment":35,"completionDate":""}],"genericFilers":[],"latestUpdates":[],"manufacturing":[],"administration":{},"crossReferences":{"UNII":"FB2CIN6HMI","CHEBI":"CHEBI:135474","INN_ID":"6947","UMLSCUI":"C0217476","ChEMBL_ID":"CHEMBL1908351","DRUGBANK_ID":"DB12868","PUBCHEM_CID":"65954","MESH_SUPPLEMENTAL_RECORD_UI":"C081834"},"formularyStatus":[],"_enricherVersion":"v2","developmentCodes":[],"ownershipHistory":[],"pharmacokinetics":{"source":"DrugCentral","halfLife":"19.0 hours","clearance":"18.0 mL/min/kg","volumeOfDistribution":"11.0 L/kg"},"publicationCount":16,"therapeuticAreas":["Oncology"],"biosimilarFilings":[],"recentPublications":[{"date":"2003","pmid":"12570767","title":"Dual topoisomerase I/II inhibitors in cancer therapy.","journal":"Current topics in medicinal chemistry"},{"date":"1999 Nov","pmid":"10630356","title":"Phase I trial of intoplicine (RP 60475) administered as a 72 h infusion every 3 weeks in patients with solid tumors.","journal":"Anti-cancer drugs"},{"date":"1999 Jan","pmid":"10194543","title":"Topoisomerase I/II inhibitor intoplicine administered as a 24 h infusion: phase I and pharmacologic study.","journal":"Anti-cancer drugs"},{"date":"1997 Feb 15","pmid":"9140928","title":"Complementary advantages of fluorescence and SIMS microscopies in the study of cellular localization of two new antitumor drugs.","journal":"Microscopy research and technique"},{"date":"1996 Feb","pmid":"8740721","title":"Phase I and pharmacology study of intoplicine (RP 60475; NSC 645008), novel topoisomerase I and II inhibitor, in cancer patients.","journal":"Anti-cancer drugs"}],"companionDiagnostics":[],"genericManufacturerList":[],"status":"active","brandName":"INTOPLICINE","companyName":"","companyId":"","modality":"Small molecule","firstApprovalDate":"","aiSummary":"INTOPLICINE is a small molecule drug that targets DNA topoisomerase 1, a key enzyme involved in DNA replication and repair. It is classified as an intoplicine, a class of drugs that inhibit this enzyme, thereby preventing cancer cell growth. However, its commercial status and approved indications are unknown. As a result, its availability and use are not established. Further research is needed to determine its potential as a cancer treatment.","enrichmentLevel":3,"visitCount":1,"trialStats":{"total":0,"withResults":0},"verificationStatus":"partial","dataCompleteness":{"mechanism":true,"indications":false,"safety":false,"trials":true,"score":2}}