{"id":"troglitazone","rwe":[{"pmid":"41865900","year":"2026","title":"The role of ferroptosis in epilepsy: mechanisms and targeted therapies.","finding":"","journal":"Biochemical pharmacology","studyType":"Clinical Study"},{"pmid":"41833074","year":"2026","title":"High concentrations of GW9508 enhance sperm velocity in mice via peroxisome proliferator-activated receptor γ.","finding":"","journal":"Biochemical and biophysical research communications","studyType":"Clinical Study"},{"pmid":"41709726","year":"2026","title":"Retrieval Augmented Generation (RAG) for Evaluating Regulatory Compliance of Drug Information and Clinical Trial Protocols.","finding":"","journal":"CPT: pharmacometrics & systems pharmacology","studyType":"Clinical Study"},{"pmid":"41664335","year":"2026","title":"Gene Expression Profiling to Unveil Novel Biomarkers for Early Diagnosis and Therapies for Breast Cancer.","finding":"","journal":"Current topics in medicinal chemistry","studyType":"Clinical Study"},{"pmid":"41613149","year":"2025","title":"Integrative causal inference and predictive modeling reveal the iron-related gene SLC17A4 as a key biomarker in chronic rhinosinusitis.","finding":"","journal":"Frontiers in immunology","studyType":"Clinical Study"}],"tags":[{"label":"troglitazone","category":"class"},{"label":"Small Molecule","category":"modality"},{"label":"Forkhead box protein M1","category":"target"},{"label":"FOXM1","category":"gene"},{"label":"PPARG","category":"gene"},{"label":"HTR2B","category":"gene"},{"label":"A10BG01","category":"atc"},{"label":"Off-Patent","category":"patent"},{"label":"Active","category":"status"},{"label":"Diabetes mellitus type 2","category":"indication"},{"label":"Pfizer Pharms","category":"company"},{"label":"Approved 1990s","category":"decade"},{"label":"Hypoglycemic Agents","category":"pharmacology"}],"phase":"marketed","safety":{"drugInteractions":[{"url":"/drug/ciprofloxacin","drug":"ciprofloxacin","action":"Monitor closely","effect":"May interact with Ciprofloxacin","source":"DrugCentral","drugSlug":"ciprofloxacin"},{"url":"/drug/gatifloxacin","drug":"gatifloxacin","action":"Monitor closely","effect":"May interact with Gatifloxacin","source":"DrugCentral","drugSlug":"gatifloxacin"},{"url":"/drug/levofloxacin","drug":"levofloxacin","action":"Monitor closely","effect":"May interact with Levofloxacin","source":"DrugCentral","drugSlug":"levofloxacin"},{"url":"/drug/norfloxacin","drug":"norfloxacin","action":"Monitor closely","effect":"May interact with Norfloxacin","source":"DrugCentral","drugSlug":"norfloxacin"},{"url":"/drug/ofloxacin","drug":"ofloxacin","action":"Monitor closely","effect":"May interact with Ofloxacin","source":"DrugCentral","drugSlug":"ofloxacin"}]},"trials":[],"aliases":[],"company":"Pfizer","patents":[],"pricing":[],"_sources":{"trials":{"url":"https://clinicaltrials.gov/search?intr=TROGLITAZONE","method":"api_direct","source":"ClinicalTrials.gov","rawText":"","confidence":1,"sourceType":"ctgov","retrievedAt":"2026-04-20T03:42:11.932040+00:00"},"timeline":{"url":"https://en.wikipedia.org/wiki/Troglitazone","method":"deterministic","source":"Wikipedia","rawText":"","confidence":0.8,"sourceType":"wikipedia","retrievedAt":"2026-04-20T03:42:19.092138+00:00"},"regulatory.ca":{"url":"","method":"api_direct","source":"Health Canada DPD","rawText":"","confidence":1,"sourceType":"health_canada_dpd","retrievedAt":"2026-04-20T03:42:17.709428+00:00"},"publicationCount":{"url":"https://pubmed.ncbi.nlm.nih.gov/?term=TROGLITAZONE","method":"api_direct","source":"PubMed/NCBI","rawText":"","confidence":1,"sourceType":"pubmed","retrievedAt":"2026-04-20T03:42:18.043532+00:00"},"mechanism.target_chembl":{"url":"","method":"api_direct","source":"ChEMBL mechanism: Peroxisome proliferator-activated receptor gamma agonist","rawText":"","confidence":1,"sourceType":"chembl","retrievedAt":"2026-04-20T03:42:19.092068+00:00"},"crossReferences.chemblId":{"url":"https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL408/","method":"api_direct","source":"ChEMBL (EMBL-EBI)","rawText":"","confidence":1,"sourceType":"chembl","retrievedAt":"2026-04-20T03:42:18.749102+00:00"}},"allNames":"rezulin","offLabel":[],"synonyms":["CS-045","rezulin","troglitazone","romglizone"],"timeline":[{"date":"1997-01-29","type":"positive","source":"DrugCentral","milestone":"FDA approval (Pfizer Pharms)"},{"date":"1997-08-04","type":"positive","source":"FDA Orange Book","milestone":"Rezulin approved — 300MG"}],"aiSummary":"Rezulin (TROGLITAZONE) is a small molecule drug developed by Pfizer Pharmaceuticals that targets the Forkhead box protein M1. It belongs to the troglitazone class and was approved by the FDA in 1997 for the treatment of type 2 diabetes mellitus. Although it is off-patent, it is still owned by Pfizer Pharmaceuticals. Rezulin works by activating the peroxisome proliferator-activated receptor gamma (PPAR-γ), which regulates glucose and lipid metabolism. However, due to safety concerns, its use has been limited.","approvals":[{"date":"1997-01-29","orphan":false,"company":"PFIZER PHARMS","regulator":"FDA"}],"brandName":"Rezulin","ecosystem":[{"indication":"Diabetes mellitus type 2","otherDrugs":[{"name":"acarbose","slug":"acarbose","company":"Bayer Hlthcare"},{"name":"acetohexamide","slug":"acetohexamide","company":"Lilly"},{"name":"albiglutide","slug":"albiglutide","company":"Glaxosmithkline Llc"},{"name":"alogliptin","slug":"alogliptin","company":"Takeda Pharms Usa"}],"globalPrevalence":537000000}],"mechanism":{"target":"Forkhead box protein M1","novelty":"Follow-on","targets":[{"gene":"FOXM1","source":"DrugCentral","target":"Forkhead box protein M1","protein":"Forkhead box protein M1"},{"gene":"PPARG","source":"DrugCentral","target":"Peroxisome proliferator-activated receptor gamma","protein":"Peroxisome proliferator-activated receptor gamma"},{"gene":"HTR2B","source":"DrugCentral","target":"5-hydroxytryptamine receptor 2B","protein":"5-hydroxytryptamine receptor 2B"},{"gene":"CA2","source":"DrugCentral","target":"Carbonic anhydrase 2","protein":"Carbonic anhydrase 2"},{"gene":"MAPK1","source":"DrugCentral","target":"Mitogen-activated protein kinase 1","protein":"Mitogen-activated protein kinase 1"},{"gene":"ABCB11","source":"DrugCentral","target":"Bile salt export pump","protein":"Bile salt export pump"},{"gene":"ADORA3","source":"DrugCentral","target":"Adenosine receptor A3","protein":"Adenosine receptor A3"},{"gene":"TBXAS1","source":"DrugCentral","target":"Thromboxane-A synthase","protein":"Thromboxane-A synthase"},{"gene":"CYP2C9","source":"DrugCentral","target":"Cytochrome P450 2C9","protein":"Cytochrome P450 2C9"},{"gene":"MAOB","source":"DrugCentral","target":"Amine oxidase [flavin-containing] B","protein":"Amine oxidase [flavin-containing] B"}],"modality":"Small Molecule","drugClass":"troglitazone","explanation":"","oneSentence":"","technicalDetail":"Rezulin acts as a PPAR-γ agonist, binding to the receptor and activating its transcriptional activity, which leads to the regulation of genes involved in glucose and lipid metabolism, including insulin sensitivity and glucose uptake in adipose tissue."},"_wikipedia":{"url":"https://en.wikipedia.org/wiki/Troglitazone","title":"Troglitazone","extract":"Troglitazone is an antidiabetic and anti-inflammatory drug, and a member of the drug class of the thiazolidinediones. It was prescribed for people with diabetes mellitus type 2.","wiki_history":"==History==\nthumb|A 30-tablet pharmacy stock bottle of Rezulin (troglitazone) (400 mg) from Parke-Davis. Manufactured 1997. Shown also is one broken tablet. Tablet branding is PD353.\nTroglitazone was developed by Daiichi Sankyo (Japan). In the United States, it was introduced and manufactured by Parke-Davis in the late 1990s but turned out to be associated with an idiosyncratic reaction leading to drug-induced hepatitis. The Food and Drug Administration (FDA) medical officer assigned to evaluate troglitazone, John Gueriguian, did not recommend its approval due to potentially high liver toxicity; Parke-Davis complained to the FDA, and Gueriguian was subsequently removed from his post. A panel of experts approved it in January 1997.  Once the prevalence of adverse liver effects became known, troglitazone was withdrawn from the British market in December 1997, from the United States market in 2000, and from the Japanese market soon afterwards. It did not get approval in the rest of Europe.\n\nTroglitazone was developed as the first anti-diabetic drug having a mechanism of action involving the enhancement of insulin resistance.  At the time, it was widely believed that such drugs, by addressing the primary metabolic defect associated with Type 2 diabetes, would have numerous benefits including avoiding the risk of hypoglycemia associated with insulin and earlier oral antidiabetic drugs.  It was further believed that reducing insulin resistance would potentially reduce the very high rate of cardiovascular disease that is associated with diabetes.\n\nParke-Davis/Warner Lambert submitted the diabetes drug Rezulin for FDA review on July 31, 1996. The medical officer assigned to the review, Dr. John L. Gueriguian, cited Rezulin's potential to harm the liver and the heart, and he questioned its viability in lowering blood sugar for patients with adult-onset diabetes, recommending against the drug's approval. After complaints from the drugmaker, Gueriguian was removed on November "},"commercial":{"launchDate":"1997","_launchSource":"DrugCentral (FDA 1997-01-29, PFIZER PHARMS)"},"references":[{"id":1,"url":"https://drugcentral.org/drugcard/2767","fields":["approvals","synonyms","ATC","PK","indications","contraindications","DDIs","targets","patents","FAERS"],"source":"DrugCentral"},{"id":2,"url":"https://clinicaltrials.gov/search?intr=TROGLITAZONE","fields":["trials"],"source":"ClinicalTrials.gov"},{"id":3,"url":"https://pubmed.ncbi.nlm.nih.gov/?term=TROGLITAZONE","fields":["publications"],"source":"PubMed/NCBI"},{"id":4,"url":"https://en.wikipedia.org/wiki/Troglitazone","fields":["history","overview"],"source":"Wikipedia"},{"id":5,"url":"https://www.fda.gov/drugs/drug-approvals-and-databases/orange-book-data-files","fields":["patents","exclusivity","genericManufacturers"],"source":"FDA Orange Book"}],"_enrichedAt":"2026-03-30T16:04:48.544582","_validation":{"fieldsValidated":0,"lastValidatedAt":"2026-04-20T03:42:20.311602+00:00","fieldsConflicting":1,"overallConfidence":0.8},"biosimilars":[],"competitors":[{"drugName":"rosiglitazone","drugSlug":"rosiglitazone","fdaApproval":"1999-05-25","genericCount":1,"patentStatus":"Off-patent — generic available","relationship":"same-class"},{"drugName":"pioglitazone","drugSlug":"pioglitazone","fdaApproval":"1999-07-15","genericCount":13,"patentStatus":"Off-patent — generic available","relationship":"same-class"}],"genericName":"troglitazone","indications":{"approved":[{"name":"Diabetes mellitus type 2","source":"DrugCentral","snomedId":44054006,"regulator":"FDA","usPrevalence":37300000,"globalPrevalence":537000000,"prevalenceMethod":"curated","prevalenceSource":"IDF Diabetes Atlas, 2024"}],"offLabel":[],"pipeline":[]},"drugCategory":"active","labelChanges":[],"patentStatus":"Off-patent — no active Orange Book patents","relatedDrugs":[{"drugId":"rosiglitazone","brandName":"rosiglitazone","genericName":"rosiglitazone","approvalYear":"1999","relationship":"same-class"},{"drugId":"pioglitazone","brandName":"pioglitazone","genericName":"pioglitazone","approvalYear":"1999","relationship":"same-class"}],"trialDetails":[{"nctId":"NCT03492580","phase":"","title":"A Study for Comparison of Canagliflozin Versus Alternative Antihyperglycemic Treatments on Risk of Heart Failure Hospitalization and Amputation for Participants With Type 2 Diabetes Mellitus and the Subpopulation With Established Cardiovascular Disease","status":"COMPLETED","sponsor":"Janssen Research & Development, LLC","startDate":"2018-02-22","conditions":["Diabetes Mellitus, Type 2","Cardiovascular Diseases"],"enrollment":714582,"completionDate":"2018-06-25"},{"nctId":"NCT01055223","phase":"","title":"Fracture Risk With Thiazolidinediones","status":"COMPLETED","sponsor":"GlaxoSmithKline","startDate":"2009-05","conditions":["Fractures, Bone","Type II Diabetes"],"enrollment":98483,"completionDate":"2010-03"},{"nctId":"NCT00003058","phase":"PHASE2","title":"Troglitazone in Treating Patients With Liposarcoma","status":"COMPLETED","sponsor":"Dana-Farber Cancer Institute","startDate":"1997-06","conditions":["Sarcoma"],"enrollment":85,"completionDate":"2000-01"},{"nctId":"NCT02476760","phase":"","title":"Incretin-based Drugs and Acute Pancreatitis","status":"COMPLETED","sponsor":"Canadian Network for Observational Drug Effect Studies, CNODES","startDate":"2014-03","conditions":["Diabetes Mellitus, Type 2"],"enrollment":1417914,"completionDate":"2015-04"},{"nctId":"NCT02456428","phase":"","title":"Incretin-based Drugs and the Risk of Heart Failure","status":"COMPLETED","sponsor":"Canadian Network for Observational Drug Effect Studies, CNODES","startDate":"2014-03","conditions":["Type 2 Diabetes Mellitus"],"enrollment":1499650,"completionDate":"2015-05"},{"nctId":"NCT02475499","phase":"","title":"Incretin-based Drugs and Pancreatic Cancer","status":"COMPLETED","sponsor":"Canadian Network for Observational Drug Effect Studies, CNODES","startDate":"2014-03","conditions":["Diabetes Mellitus, Type 2"],"enrollment":886172,"completionDate":"2015-04"},{"nctId":"NCT01068860","phase":"PHASE2","title":"To Compare the Effect of a Subcutaneous Canakinumab Administration to Placebo in Patients With Impaired Glucose Tolerance or Patients With Type 2 Diabetes With Differing Baseline Diabetes Therapies","status":"COMPLETED","sponsor":"Novartis","startDate":"2010-02","conditions":["Type 2 Diabetes Mellitus","Impaired Glucose Tolerance"],"enrollment":246,"completionDate":"2010-08"},{"nctId":"NCT00116545","phase":"PHASE2,PHASE3","title":"TART - Troglitazone Atherosclerosis Regression Trial","status":"COMPLETED","sponsor":"Parke-Davis","startDate":"1997-01","conditions":["Atherosclerosis","Diabetes Mellitus"],"enrollment":288,"completionDate":"2000-04"}],"genericFilers":[],"latestUpdates":[],"manufacturing":[],"_patentsChecked":true,"crossReferences":{"NUI":"N0000148466","MMSL":"5640","NDDF":"006355","UNII":"I66ZZ0ZN0E","VUID":"4020997","CHEBI":"CHEBI:9753","VANDF":"4020997","INN_ID":"6851","RXNORM":"203715","UMLSCUI":"C0245514","chemblId":"CHEMBL408","ChEMBL_ID":"CHEMBL408","KEGG_DRUG":"D00395","DRUGBANK_ID":"DB00197","PDB_CHEM_ID":" TDZ","PUBCHEM_CID":"5591","SNOMEDCT_US":"109085002","IUPHAR_LIGAND_ID":"2693","MESH_DESCRIPTOR_UI":"D000077288"},"formularyStatus":[],"_enricherVersion":"v2","developmentCodes":[],"ownershipHistory":[{"period":"1997-","companyName":"Pfizer Pharms","relationship":"Original Developer"}],"pharmacokinetics":{"source":"DrugCentral","bioavailability":"45%"},"publicationCount":2348,"therapeuticAreas":["Metabolic"],"atcClassification":{"source":"DrugCentral","atcCode":"A10BG01","allCodes":["A10BG01"]},"biosimilarFilings":[],"originalDeveloper":"Pfizer Pharms","recentPublications":[{"date":"2026 Mar 20","pmid":"41865900","title":"The role of ferroptosis in epilepsy: mechanisms and targeted therapies.","journal":"Biochemical pharmacology"},{"date":"2026 Mar 11","pmid":"41833074","title":"High concentrations of GW9508 enhance sperm velocity in mice via peroxisome proliferator-activated receptor γ.","journal":"Biochemical and biophysical research communications"},{"date":"2026 Mar","pmid":"41709726","title":"Retrieval Augmented Generation (RAG) for Evaluating Regulatory Compliance of Drug Information and Clinical Trial Protocols.","journal":"CPT: pharmacometrics & systems pharmacology"},{"date":"2026 Feb 3","pmid":"41664335","title":"Gene Expression Profiling to Unveil Novel Biomarkers for Early Diagnosis and Therapies for Breast Cancer.","journal":"Current topics in medicinal chemistry"},{"date":"2025","pmid":"41613149","title":"Integrative causal inference and predictive modeling reveal the iron-related gene SLC17A4 as a key biomarker in chronic rhinosinusitis.","journal":"Frontiers in immunology"}],"companionDiagnostics":[],"genericManufacturers":0,"_genericFilersChecked":true,"genericManufacturerList":[],"status":"withdrawn","companyName":"Pfizer","companyId":"pfizer","modality":"Small molecule","firstApprovalDate":"1997","enrichmentLevel":3,"visitCount":1,"regulatoryByCountry":[{"country_code":"US","regulator":"FDA","status":"approved","approval_date":"1997-01-29T00:00:00.000Z","mah":"PFIZER PHARMS","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":"2026-04-20T03:42:20.311602+00:00","fieldsConflicting":1,"overallConfidence":0.8},"verificationStatus":"partial","dataCompleteness":{"mechanism":false,"indications":true,"safety":false,"trials":true,"score":2}}