{"id":"masoprocol","rwe":[],"tags":[{"label":"masoprocol","category":"class"},{"label":"Small Molecule","category":"modality"},{"label":"Aromatase","category":"target"},{"label":"CYP19A1","category":"gene"},{"label":"ALOX5","category":"gene"},{"label":"LTB4R","category":"gene"},{"label":"L01XX10","category":"atc"},{"label":"Off-Patent","category":"patent"},{"label":"Active","category":"status"},{"label":"Actinic keratosis","category":"indication"},{"label":"Approved 1990s","category":"decade"},{"label":"Analgesics","category":"pharmacology"},{"label":"Analgesics, Non-Narcotic","category":"pharmacology"},{"label":"Anti-Inflammatory Agents","category":"pharmacology"},{"label":"Anti-Inflammatory Agents, Non-Steroidal","category":"pharmacology"},{"label":"Antioxidants","category":"pharmacology"},{"label":"Antirheumatic Agents","category":"pharmacology"},{"label":"Cyclooxygenase Inhibitors","category":"pharmacology"},{"label":"Enzyme Inhibitors","category":"pharmacology"},{"label":"Lipoxygenase Inhibitors","category":"pharmacology"},{"label":"Peripheral Nervous System Agents","category":"pharmacology"},{"label":"Protective Agents","category":"pharmacology"},{"label":"Sensory System Agents","category":"pharmacology"}],"phase":"marketed","safety":{},"trials":[],"aliases":[],"patents":[],"pricing":[],"_sources":{"trials":{"url":"https://clinicaltrials.gov/search?intr=MASOPROCOL","method":"api_direct","source":"ClinicalTrials.gov","rawText":"","confidence":1,"sourceType":"ctgov","retrievedAt":"2026-04-20T03:33:25.842269+00:00"},"regulatory.ca":{"url":"","method":"api_direct","source":"Health Canada DPD","rawText":"","confidence":1,"sourceType":"health_canada_dpd","retrievedAt":"2026-04-20T03:33:32.202597+00:00"},"publicationCount":{"url":"https://pubmed.ncbi.nlm.nih.gov/?term=MASOPROCOL","method":"api_direct","source":"PubMed/NCBI","rawText":"","confidence":1,"sourceType":"pubmed","retrievedAt":"2026-04-20T03:33:32.962856+00:00"},"mechanism.target_chembl":{"url":"","method":"api_direct","source":"ChEMBL mechanism: Insulin-like growth factor I receptor inhibitor","rawText":"","confidence":1,"sourceType":"chembl","retrievedAt":"2026-04-20T03:33:33.531298+00:00"},"crossReferences.chemblId":{"url":"https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL313972/","method":"api_direct","source":"ChEMBL (EMBL-EBI)","rawText":"","confidence":1,"sourceType":"chembl","retrievedAt":"2026-04-20T03:33:33.435305+00:00"}},"allNames":"actinex","offLabel":[],"synonyms":["nordihydroguaiaretic acid","masoprocol","actinex","mesonordihydroguaiaretic acid"],"timeline":[{"date":"1992-09-04","type":"positive","source":"DrugCentral","milestone":"FDA approval"}],"aiSummary":"Actinex (MASOPROCOL) is a small molecule drug that targets aromatase, a key enzyme involved in the production of estrogen. It was originally developed and is currently owned by a pharmaceutical company. Actinex is FDA-approved for the treatment of actinic keratosis, a skin condition caused by prolonged sun exposure. The drug is off-patent, meaning it is no longer protected by patents, and there are no generic manufacturers. As a result, its commercial status is uncertain.","approvals":[{"date":"1992-09-04","orphan":false,"company":"","regulator":"FDA"}],"brandName":"Actinex","ecosystem":[{"indication":"Actinic keratosis","otherDrugs":[{"name":"aminolevulinic acid","slug":"aminolevulinic-acid","company":"Dusa"},{"name":"diclofenac","slug":"diclofenac","company":""},{"name":"fluorouracil","slug":"fluorouracil","company":"Spectrum Pharms"},{"name":"imiquimod","slug":"imiquimod","company":"Medicis"}],"globalPrevalence":null}],"mechanism":{"target":"Aromatase","novelty":"Follow-on","targets":[{"gene":"CYP19A1","source":"DrugCentral","target":"Aromatase","protein":"Aromatase"},{"gene":"ALOX5","source":"DrugCentral","target":"Arachidonate 5-lipoxygenase","protein":"Arachidonate 5-lipoxygenase"},{"gene":"LTB4R","source":"DrugCentral","target":"Leukotriene B4 receptor 1","protein":"Leukotriene B4 receptor 1"},{"gene":"ALOX12","source":"DrugCentral","target":"Arachidonate 12-lipoxygenase, 12S-type","protein":"Arachidonate 12-lipoxygenase, 12S-type"},{"gene":"ALOX15","source":"DrugCentral","target":"Arachidonate 15-lipoxygenase","protein":"Arachidonate 15-lipoxygenase"},{"gene":"SNCA","source":"DrugCentral","target":"Alpha-synuclein","protein":"Alpha-synuclein"},{"gene":"HSD17B2","source":"DrugCentral","target":"Estradiol 17-beta-dehydrogenase 2","protein":"Estradiol 17-beta-dehydrogenase 2"},{"gene":"IGF1R","source":"DrugCentral","target":"Insulin-like growth factor 1 receptor","protein":"Insulin-like growth factor 1 receptor"},{"gene":"TRPA1","source":"DrugCentral","target":"Transient receptor potential cation channel subfamily A member 1","protein":"Transient receptor potential cation channel subfamily A member 1"},{"gene":"HSD17B1","source":"DrugCentral","target":"Estradiol 17-beta-dehydrogenase 1","protein":"Estradiol 17-beta-dehydrogenase 1"}],"modality":"Small Molecule","drugClass":"masoprocol","explanation":"","oneSentence":"","technicalDetail":"Actinex (masoprocol) is a competitive inhibitor of the aromatase enzyme, specifically targeting the heme-containing active site and preventing the conversion of androgen precursors to estrogen."},"commercial":{"launchDate":"1992","_launchSource":"DrugCentral (FDA 1992-09-04, )"},"references":[{"id":1,"url":"https://drugcentral.org/drugcard/1637","fields":["approvals","synonyms","ATC","PK","indications","contraindications","DDIs","targets","patents","FAERS"],"source":"DrugCentral"},{"id":2,"url":"https://clinicaltrials.gov/search?intr=MASOPROCOL","fields":["trials"],"source":"ClinicalTrials.gov"},{"id":3,"url":"https://pubmed.ncbi.nlm.nih.gov/?term=MASOPROCOL","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":"2026-03-30T12:30:37.575027","_validation":{"fieldsValidated":0,"lastValidatedAt":"2026-04-20T03:33:35.327518+00:00","fieldsConflicting":1,"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 — generic available","relationship":"same-class"},{"drugName":"mitotane","drugSlug":"mitotane","fdaApproval":"1970-07-08","patentStatus":"Unknown","relationship":"same-class"},{"drugName":"pegaspargase","drugSlug":"pegaspargase","fdaApproval":"1994-02-01","relationship":"same-class"},{"drugName":"arsenic trioxide","drugSlug":"arsenic-trioxide","fdaApproval":"2000-09-25","genericCount":11,"patentStatus":"Off-patent — generic available","relationship":"same-class"},{"drugName":"denileukin diftitox","drugSlug":"denileukin-diftitox","fdaApproval":"1999-02-05","relationship":"same-class"},{"drugName":"celecoxib","drugSlug":"celecoxib","fdaApproval":"1998-12-31","patentExpiry":"May 27, 2036","patentStatus":"Patent protected","relationship":"same-class"},{"drugName":"anagrelide","drugSlug":"anagrelide","fdaApproval":"1997-03-14","genericCount":9,"patentStatus":"Off-patent — generic available","relationship":"same-class"},{"drugName":"omacetaxine mepesuccinate","drugSlug":"omacetaxine-mepesuccinate","fdaApproval":"2012-10-26","patentExpiry":"Oct 26, 2026","patentStatus":"Patent protected","relationship":"same-class"},{"drugName":"eribulin","drugSlug":"eribulin","fdaApproval":"2010-11-15","patentExpiry":"Jul 8, 2027","patentStatus":"Patent protected","relationship":"same-class"},{"drugName":"aflibercept","drugSlug":"aflibercept","fdaApproval":"2011-11-18","relationship":"same-class"},{"drugName":"venetoclax","drugSlug":"venetoclax","fdaApproval":"2016-04-11","patentExpiry":"Sep 6, 2033","patentStatus":"Patent protected","relationship":"same-class"},{"drugName":"enasidenib","drugSlug":"enasidenib","fdaApproval":"2017-08-01","patentExpiry":"Sep 16, 2034","patentStatus":"Patent protected","relationship":"same-class"},{"drugName":"ivosidenib","drugSlug":"ivosidenib","fdaApproval":"2018-07-20","patentExpiry":"Oct 18, 2036","patentStatus":"Patent protected","relationship":"same-class"},{"drugName":"selinexor","drugSlug":"selinexor","fdaApproval":"2019-07-03","patentExpiry":"Jul 3, 2033","patentStatus":"Patent protected","relationship":"same-class"},{"drugName":"tagraxofusp","drugSlug":"tagraxofusp","fdaApproval":"2018-12-21","relationship":"same-class"},{"drugName":"lurbinectedin","drugSlug":"lurbinectedin","fdaApproval":"2020-06-15","patentExpiry":"May 29, 2040","patentStatus":"Patent protected","relationship":"same-class"},{"drugName":"tazemetostat","drugSlug":"tazemetostat","fdaApproval":"2020-01-23","patentExpiry":"Sep 12, 2031","patentStatus":"Patent protected","relationship":"same-class"}],"genericName":"masoprocol","indications":{"approved":[{"name":"Actinic keratosis","source":"DrugCentral","snomedId":201101007,"regulator":"FDA"}],"offLabel":[],"pipeline":[]},"drugCategory":"active","labelChanges":[],"patentStatus":"Off-patent — no active Orange Book patents","relatedDrugs":[{"drugId":"asparaginase","brandName":"asparaginase","genericName":"asparaginase","approvalYear":"1994","relationship":"same-class"},{"drugId":"altretamine","brandName":"altretamine","genericName":"altretamine","approvalYear":"1990","relationship":"same-class"},{"drugId":"hydroxycarbamide","brandName":"hydroxycarbamide","genericName":"hydroxycarbamide","approvalYear":"1967","relationship":"same-class"},{"drugId":"pentostatin","brandName":"pentostatin","genericName":"pentostatin","approvalYear":"1991","relationship":"same-class"},{"drugId":"mitotane","brandName":"mitotane","genericName":"mitotane","approvalYear":"1970","relationship":"same-class"},{"drugId":"pegaspargase","brandName":"pegaspargase","genericName":"pegaspargase","approvalYear":"1994","relationship":"same-class"},{"drugId":"arsenic-trioxide","brandName":"arsenic trioxide","genericName":"arsenic trioxide","approvalYear":"2000","relationship":"same-class"},{"drugId":"denileukin-diftitox","brandName":"denileukin diftitox","genericName":"denileukin diftitox","approvalYear":"1999","relationship":"same-class"},{"drugId":"celecoxib","brandName":"celecoxib","genericName":"celecoxib","approvalYear":"1998","relationship":"same-class"},{"drugId":"anagrelide","brandName":"anagrelide","genericName":"anagrelide","approvalYear":"1997","relationship":"same-class"}],"trialDetails":[{"nctId":"NCT02575794","phase":"PHASE1","title":"Terameprocol in Treating Patients With Recurrent High Grade Glioma","status":"COMPLETED","sponsor":"Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins","startDate":"2018-05-03","conditions":["High Grade Glioma (III or IV)"],"enrollment":20,"completionDate":"2023-10-04"},{"nctId":"NCT00404248","phase":"PHASE1,PHASE2","title":"Tetra-O-Methyl Nordihydroguaiaretic Acid in Treating Patients With Recurrent High-Grade Glioma","status":"COMPLETED","sponsor":"Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins","startDate":"2007-01","conditions":["Brain and Central Nervous System Tumors"],"enrollment":35,"completionDate":"2012-02"},{"nctId":"NCT00154089","phase":"PHASE1,PHASE2","title":"A Pilot Study of EM-1421 for the Treatment of Cervical Intraepithelial Neoplasia","status":"COMPLETED","sponsor":"Erimos Pharmaceuticals","startDate":"2004-11","conditions":["Cervical Intraepithelial Neoplasia"],"enrollment":8,"completionDate":"2006-12"},{"nctId":"NCT00057512","phase":"PHASE1","title":"Study of Intralesional Injection of M4N in Patients With Refractory Malignant Tumors of the Head and Neck","status":"COMPLETED","sponsor":"Erimos Pharmaceuticals","startDate":"2003-01","conditions":["Head and Neck Neoplasms"],"enrollment":9,"completionDate":"2003-12"},{"nctId":"NCT00664586","phase":"PHASE1","title":"A Phase 1 Continuous Intravenous Infusion Study of Terameprocol (EM-1421) in Subjects With Refractory Solid Tumors","status":"TERMINATED","sponsor":"Erimos Pharmaceuticals","startDate":"2007-05","conditions":["Refractory Solid Tumors","Lymphoma"],"enrollment":21,"completionDate":"2009-06"},{"nctId":"NCT00664677","phase":"PHASE1","title":"Phase 1 Study of Terameprocol (EM-1421) in Patients With Leukemia","status":"TERMINATED","sponsor":"Erimos Pharmaceuticals","startDate":"2007-08","conditions":["Leukemias","Acute Myeloid Leukemia (AML)","Acute Lymphocytic Leukemia (ALL)","Adult T Cell Leukemia (ATL)","Chronic Myeloid Leukemia (CML-BP)","Chronic Lymphocytic Leukemia (CLL)","Myelodysplastic Syndrome (MDS)","Chronic Myelomonocytic Leukemia (CMML)"],"enrollment":16,"completionDate":"2009-06"},{"nctId":"NCT00678015","phase":"PHASE2","title":"Pharmacokinetic and Efficacy Study of Nordihydroguaiaretic Acid (NDGA) in Non Metastatic Recurrent Prostate Cancer","status":"TERMINATED","sponsor":"University of California, San Francisco","startDate":"2008-05","conditions":["Prostate Cancer"],"enrollment":12,"completionDate":"2011-06"},{"nctId":"NCT00313534","phase":"PHASE1","title":"Nordihydroguaiaretic Acid in Treating Patients With Nonmetastatic Relapsed Prostate Cancer","status":"TERMINATED","sponsor":"University of California, San Francisco","startDate":"2005-06","conditions":["Prostate Cancer"],"enrollment":15,"completionDate":"2006-10"},{"nctId":"NCT00259818","phase":"PHASE1","title":"Dose Escalation Study of EM-1421 for the Treatment of Recurrent or Refractory Solid Tumors","status":"COMPLETED","sponsor":"Erimos Pharmaceuticals","startDate":"2005-12","conditions":["Cancer"],"enrollment":30,"completionDate":"2008-01"}],"genericFilers":[],"latestUpdates":[],"manufacturing":[],"_patentsChecked":true,"crossReferences":{"NUI":"N0000179680","MMSL":"5024","NDDF":"004081","UNII":"7BO8G1BYQU","VUID":"4020556","CHEBI":"CHEBI:73468","VANDF":"4020556","INN_ID":"6615","RXNORM":"227238","UMLSCUI":"C0733397","chemblId":"CHEMBL313972","ChEMBL_ID":"CHEMBL313972","KEGG_DRUG":"D04862","DRUGBANK_ID":"DB00179","PUBCHEM_CID":"71398","SNOMEDCT_US":"108933006","MESH_DESCRIPTOR_UI":"D009637"},"formularyStatus":[],"_enricherVersion":"v2","developmentCodes":[],"ownershipHistory":[],"publicationCount":21,"therapeuticAreas":["Metabolic"],"atcClassification":{"source":"DrugCentral","atcCode":"L01XX10","allCodes":["L01XX10"]},"biosimilarFilings":[],"recentPublications":[],"companionDiagnostics":[],"genericManufacturers":0,"_genericFilersChecked":true,"genericManufacturerList":[],"status":"approved","companyName":"","companyId":"","modality":"Small molecule","firstApprovalDate":"1992","enrichmentLevel":3,"visitCount":0,"regulatoryByCountry":[{"country_code":"US","regulator":"FDA","status":"approved","approval_date":"1992-09-04T00:00:00.000Z","mah":"","brand_name_local":null,"application_number":""},{"country_code":"CA","regulator":"Health Canada","status":"approved","approval_date":null,"mah":"","brand_name_local":"","application_number":""},{"country_code":"IL","regulator":"MOH","status":"likely_approved","approval_date":null,"mah":null,"brand_name_local":null,"application_number":null},{"country_code":"SG","regulator":"HSA","status":"likely_approved","approval_date":null,"mah":null,"brand_name_local":null,"application_number":null},{"country_code":"AE","regulator":"MOH","status":"likely_approved","approval_date":null,"mah":null,"brand_name_local":null,"application_number":null},{"country_code":"KR","regulator":"MFDS","status":"likely_approved","approval_date":null,"mah":null,"brand_name_local":null,"application_number":null},{"country_code":"AU","regulator":"TGA","status":"likely_approved","approval_date":null,"mah":null,"brand_name_local":null,"application_number":null},{"country_code":"GB","regulator":"MHRA","status":"likely_approved","approval_date":null,"mah":null,"brand_name_local":null,"application_number":null}],"trialStats":{"total":0,"withResults":0},"validation":{"fieldsValidated":0,"lastValidatedAt":"2026-04-20T03:33:35.327518+00:00","fieldsConflicting":1,"overallConfidence":0.8},"verificationStatus":"partial","dataCompleteness":{"mechanism":false,"indications":true,"safety":false,"trials":true,"score":2}}