{"id":"testolactone","rwe":[{"pmid":"38897507","year":"2024","title":"Single-cell enzymatic cascade synthesis of testolactone enabled by engineering of polycyclic ketone monooxygenase and multi-gene expression fine-tuning.","finding":"","journal":"International journal of biological macromolecules","studyType":"Clinical Study"},{"pmid":"37255841","year":"2023","title":"Discovery of novel inhibitor of 11 beta-hydroxysteroid dehydrogenase type 1 using in silico structure-based screening approach for the treatment of type 2 diabetes.","finding":"","journal":"Journal of diabetes and metabolic disorders","studyType":"Clinical Study"},{"pmid":"35667233","year":"2022","title":"Preclinical anti-inflammatory and antioxidant effects of Azanza garckeana in STZ-induced glycemic-impaired rats, and pharmacoinformatics of it major phytoconstituents.","finding":"","journal":"Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie","studyType":"Clinical Study"},{"pmid":"35630641","year":"2022","title":"Biotransformation of Phytosterols into Androstenedione-A Technological Prospecting Study.","finding":"","journal":"Molecules (Basel, Switzerland)","studyType":"Clinical Study"},{"pmid":"34871401","year":"2021","title":"Clinical application of aromatase inhibitors to treat male infertility.","finding":"","journal":"Human reproduction update","studyType":"Clinical Study"}],"tags":[{"label":"Aromatase Inhibitor","category":"class"},{"label":"Small Molecule","category":"modality"},{"label":"Aromatase","category":"target"},{"label":"CYP19A1","category":"gene"},{"label":"Off-Patent","category":"patent"},{"label":"Active","category":"status"},{"label":"Carcinoma of female breast","category":"indication"},{"label":"Approved 1960s","category":"decade"},{"label":"Antineoplastic Agents","category":"pharmacology"},{"label":"Antineoplastic Agents, Hormonal","category":"pharmacology"}],"phase":"marketed","safety":{},"trials":[],"aliases":[],"patents":[],"pricing":[],"_sources":{"trials":{"url":"https://clinicaltrials.gov/search?intr=TESTOLACTONE","method":"api_direct","source":"ClinicalTrials.gov","rawText":"","confidence":1,"sourceType":"ctgov","retrievedAt":"2026-04-20T00:00:17.317114+00:00"},"regulatory.ca":{"url":"","method":"api_direct","source":"Health Canada DPD","rawText":"","confidence":1,"sourceType":"health_canada_dpd","retrievedAt":"2026-04-20T00:00:22.618353+00:00"},"publicationCount":{"url":"https://pubmed.ncbi.nlm.nih.gov/?term=TESTOLACTONE","method":"api_direct","source":"PubMed/NCBI","rawText":"","confidence":1,"sourceType":"pubmed","retrievedAt":"2026-04-20T00:00:22.869540+00:00"},"mechanism.target_chembl":{"url":"","method":"api_direct","source":"ChEMBL mechanism: Cytochrome P450 19A1 inhibitor","rawText":"","confidence":1,"sourceType":"chembl","retrievedAt":"2026-04-20T00:00:23.902548+00:00"},"crossReferences.chemblId":{"url":"https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL1571/","method":"api_direct","source":"ChEMBL (EMBL-EBI)","rawText":"","confidence":1,"sourceType":"chembl","retrievedAt":"2026-04-20T00:00:23.565132+00:00"}},"allNames":"teolit","offLabel":[],"synonyms":["teslac","testolactone","fludestrin","teolit","testolacton"],"timeline":[{"date":"1969-06-03","type":"positive","source":"DrugCentral","milestone":"FDA approval"}],"brandName":"Teolit","ecosystem":[{"indication":"Carcinoma of female breast","otherDrugs":[{"name":"doxorubicin","slug":"doxorubicin","company":""},{"name":"methotrexate","slug":"methotrexate","company":"Dava Pharms Inc"},{"name":"tamoxifen","slug":"tamoxifen","company":""},{"name":"thiotepa","slug":"thiotepa","company":""}],"globalPrevalence":null}],"mechanism":{"target":"Aromatase","novelty":"Follow-on","targets":[{"gene":"CYP19A1","source":"DrugCentral","target":"Aromatase","protein":"Aromatase"}],"moaClass":"Aromatase Inhibitors","modality":"Small Molecule","drugClass":"Aromatase Inhibitor","explanation":"","oneSentence":"","technicalDetail":"Testolactone acts as a competitive inhibitor of the aromatase enzyme, specifically targeting the C19-methyl group of androgens, thereby preventing the conversion of androgens to estrogens."},"commercial":{"launchDate":"1969","_launchSource":"DrugCentral (FDA 1969-06-03, )"},"references":[{"id":1,"url":"https://drugcentral.org/drugcard/2606","fields":["approvals","synonyms","ATC","PK","indications","contraindications","DDIs","targets","patents","FAERS"],"source":"DrugCentral"},{"id":2,"url":"https://clinicaltrials.gov/search?intr=TESTOLACTONE","fields":["trials"],"source":"ClinicalTrials.gov"},{"id":3,"url":"https://pubmed.ncbi.nlm.nih.gov/?term=TESTOLACTONE","fields":["publications"],"source":"PubMed/NCBI"},{"id":4,"url":"https://www.fda.gov/drugs/drug-approvals-and-databases/orange-book-data-files","fields":["patents","exclusivity","genericManufacturers"],"source":"FDA Orange Book"}],"_enrichedAt":"2026-03-30T02:43:02.952359","_validation":{"fieldsValidated":0,"lastValidatedAt":"2026-04-20T00:00:25.163700+00:00","fieldsConflicting":1,"overallConfidence":0.8},"biosimilars":[],"competitors":[{"drugName":"aminoglutethimide","drugSlug":"aminoglutethimide","fdaApproval":"1980-10-29","patentStatus":"Unknown","relationship":"same-target"},{"drugName":"anastrozole","drugSlug":"anastrozole","fdaApproval":"1995-12-27","genericCount":19,"patentStatus":"Off-patent — generic available","relationship":"same-target"},{"drugName":"clotrimazole","drugSlug":"clotrimazole","fdaApproval":"1975-02-03","patentExpiry":"May 26, 2042","patentStatus":"Patent protected","relationship":"same-target"},{"drugName":"doconexent","drugSlug":"doconexent","fdaApproval":"","relationship":"same-target"},{"drugName":"eicosapentaenoic acid","drugSlug":"eicosapentaenoic-acid","fdaApproval":"","relationship":"same-target"},{"drugName":"estrone","drugSlug":"estrone","fdaApproval":"1979-02-21","genericCount":3,"patentStatus":"Off-patent — generic available","relationship":"same-target"},{"drugName":"exemestane","drugSlug":"exemestane","fdaApproval":"1999-10-21","genericCount":11,"patentStatus":"Off-patent — generic available","relationship":"same-target"},{"drugName":"fluorouracil","drugSlug":"fluorouracil","fdaApproval":"1962-04-25","genericCount":23,"patentStatus":"Off-patent — generic available","relationship":"same-target"},{"drugName":"ketoconazole","drugSlug":"ketoconazole","fdaApproval":"1981-06-12","genericCount":19,"patentStatus":"Off-patent — generic available","relationship":"same-target"},{"drugName":"letrozole","drugSlug":"letrozole","fdaApproval":"1997-07-25","genericCount":19,"patentStatus":"Off-patent — generic available","relationship":"same-target"}],"genericName":"testolactone","indications":{"approved":[{"name":"Carcinoma of female breast","source":"DrugCentral","snomedId":447782002,"regulator":"FDA"}],"offLabel":[],"pipeline":[]},"drugCategory":"active","labelChanges":[],"patentStatus":"Off-patent — no active Orange Book patents","relatedDrugs":[{"drugId":"aminoglutethimide","brandName":"aminoglutethimide","genericName":"aminoglutethimide","approvalYear":"1980","relationship":"same-target"},{"drugId":"anastrozole","brandName":"anastrozole","genericName":"anastrozole","approvalYear":"1995","relationship":"same-target"},{"drugId":"clotrimazole","brandName":"clotrimazole","genericName":"clotrimazole","approvalYear":"1975","relationship":"same-target"},{"drugId":"doconexent","brandName":"doconexent","genericName":"doconexent","approvalYear":"","relationship":"same-target"},{"drugId":"eicosapentaenoic-acid","brandName":"eicosapentaenoic acid","genericName":"eicosapentaenoic acid","approvalYear":"","relationship":"same-target"},{"drugId":"estrone","brandName":"estrone","genericName":"estrone","approvalYear":"1979","relationship":"same-target"},{"drugId":"exemestane","brandName":"exemestane","genericName":"exemestane","approvalYear":"1999","relationship":"same-target"},{"drugId":"fluorouracil","brandName":"fluorouracil","genericName":"fluorouracil","approvalYear":"1962","relationship":"same-target"},{"drugId":"ketoconazole","brandName":"ketoconazole","genericName":"ketoconazole","approvalYear":"1981","relationship":"same-target"},{"drugId":"letrozole","brandName":"letrozole","genericName":"letrozole","approvalYear":"1997","relationship":"same-target"}],"trialDetails":[{"nctId":"NCT00001521","phase":"PHASE3","title":"Three Drug Combination Therapy Versus Conventional Treatment of Children With Congenital Adrenal Hyperplasia","status":"COMPLETED","sponsor":"Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)","startDate":"1995-06-08","conditions":["Congenital Adrenal Hyperplasia (CAH)"],"enrollment":66,"completionDate":"2024-04-01"},{"nctId":"NCT01065220","phase":"PHASE4","title":"Sex Steroids and the Serotonin Transporter","status":"COMPLETED","sponsor":"Medical University of Vienna","startDate":"2010-02","conditions":["Transsexualism"],"enrollment":32,"completionDate":"2014-01"},{"nctId":"NCT00001202","phase":"PHASE2","title":"Treatment of Boys With Precocious Puberty","status":"COMPLETED","sponsor":"Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)","startDate":"1985-01","conditions":["Precocious Puberty"],"enrollment":80,"completionDate":"2004-01"},{"nctId":"NCT00001181","phase":"PHASE2","title":"Testolactone for the Treatment of Girls With LHRH Resistant Precocious Puberty","status":"COMPLETED","sponsor":"Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)","startDate":"1982-10","conditions":["Polyostotic Fibrous Dysplasia","Precocious Puberty"],"enrollment":100,"completionDate":"2003-05"}],"genericFilers":[],"latestUpdates":[],"manufacturing":[],"_patentsChecked":true,"crossReferences":{"NUI":"N0000146097","MMSL":"2376","NDDF":"002665","UNII":"6J9BLA949Q","VUID":"4017729","CHEBI":"CHEBI:9460","VANDF":"4017729","INN_ID":"1839","RXNORM":"10378","UMLSCUI":"C0039600","chemblId":"CHEMBL1571","ChEMBL_ID":"CHEMBL1571","KEGG_DRUG":"D00153","DRUGBANK_ID":"DB00894","PUBCHEM_CID":"13769","SNOMEDCT_US":"404877009","IUPHAR_LIGAND_ID":"7303","MESH_DESCRIPTOR_UI":"D013738"},"formularyStatus":[],"_enricherVersion":"v2","developmentCodes":[],"ownershipHistory":[],"publicationCount":123,"therapeuticAreas":["Oncology"],"biosimilarFilings":[],"recentPublications":[{"date":"2024 Aug","pmid":"38897507","title":"Single-cell enzymatic cascade synthesis of testolactone enabled by engineering of polycyclic ketone monooxygenase and multi-gene expression fine-tuning.","journal":"International journal of biological macromolecules"},{"date":"2023 Jun","pmid":"37255841","title":"Discovery of novel inhibitor of 11 beta-hydroxysteroid dehydrogenase type 1 using in silico structure-based screening approach for the treatment of type 2 diabetes.","journal":"Journal of diabetes and metabolic disorders"},{"date":"2022 Aug","pmid":"35667233","title":"Preclinical anti-inflammatory and antioxidant effects of Azanza garckeana in STZ-induced glycemic-impaired rats, and pharmacoinformatics of it major phytoconstituents.","journal":"Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie"},{"date":"2022 May 15","pmid":"35630641","title":"Biotransformation of Phytosterols into Androstenedione-A Technological Prospecting Study.","journal":"Molecules (Basel, Switzerland)"},{"date":"2021 Dec 21","pmid":"34871401","title":"Clinical application of aromatase inhibitors to treat male infertility.","journal":"Human reproduction update"}],"companionDiagnostics":[],"genericManufacturers":0,"_genericFilersChecked":true,"genericManufacturerList":[],"status":"approved","companyName":"","companyId":"","modality":"Small molecule","firstApprovalDate":"1969","aiSummary":"","enrichmentLevel":3,"visitCount":1,"regulatoryByCountry":[{"country_code":"CA","regulator":"Health Canada","status":"approved","approval_date":null,"mah":"","brand_name_local":"","application_number":""},{"country_code":"US","regulator":"FDA","status":"approved","approval_date":null,"mah":null,"brand_name_local":null,"application_number":null}],"trialStats":{"total":0,"withResults":0},"validation":{"fieldsValidated":0,"lastValidatedAt":"2026-04-20T00:00:25.163700+00:00","fieldsConflicting":1,"overallConfidence":0.8},"verificationStatus":"partial","dataCompleteness":{"mechanism":false,"indications":true,"safety":false,"trials":true,"score":2}}