troglitazone (Rezulin) Report issue

Small molecule Withdrawn Priority Review FDA
AACT ChEMBL DrugBank Drug Central Drugs@FDA KEGG MeSH PubChem

Active Ingredient History

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Troglitazone (TGZ, brand name: Rezulin and Prelay) is a peroxisome proliferator-activated receptor gamma (PPAR gamma) ligand, which was developed by Daiichi Sankyo and approved for the US market for the treatment of Type II diabetes mellitus. The drug is used alone or in combination with a sulfonylurea, metformin, or insulin as an adjunct to diet and exercise, and was not indicated as initial therapy in patients with type 2 diabetes. This drug was withdrawn from the UK market due to liver toxicity. It was removed from the US market in 2000, only 3 years after its introduction and from Japan, shortly afterward. In addition, was conducted a clinical trial for the treatment of patients with advanced liposarcoma by using troglitazone, but the positive result wasn’t obtained. It was shown, that in case of cancer cells troglitazone acted independently of PPAR gamma, by up-regulation of early growth response-1 (Egr-1). Egr-1 transcription factor has been linked to apoptosis and shown to be activated by extracellular signal-regulated kinase (ERK).   NCATS

Chemistry

  • SMILES: Cc1c(C)c2OC(C)(COc3ccc(CC4SC(=O)NC4=O)cc3)CCc2c(C)c1O
  • InChIKey: GXPHKUHSUJUWKP-UHFFFAOYSA-N
  • Mol. Mass: 441.55
  • ALogP: 4.37
  • ChEMBL Molecule:
    troglitazone  
More Chemistry

Pharmacology

Alternative names

2,4-thiazolidinedione, 5-((4-((3,4-dihydro-6-hydroxy-2,5,7,8-tetramethyl-2h-1-benzopyran-2-yl)methoxy)phenyl)methyl)- | 5-(4-((6-hydroxy-2,5,7,8-tetramethylchroman-2-yl-methoxy)benzyl)-2,4-thiazolidinedione) | ci-991 | cs 045 | cs-045 | gr92132x | gr-92132x | parke davis brand of troglitazone | prelay | rezulin | romglizone | romozin | troglitazone | warner-lambert brand of troglitazone

Organizations (6)

Research & Development (4)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Marketing (2)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Indications (6)

Approved Indications (1)


 

Diabetes Mellitus, Type 2 (approved 1997)

Experimental Indications - Clinical Trial Phases 1-4 (5)


 

Atherosclerosis (Phase 2/Phase 3)

Diabetes Mellitus (Phase 2/Phase 3)

Liposarcoma (Phase 2)

Polycystic Ovary Syndrome (Phase 3)

Sarcoma (Phase 2)

Overview

  • Highest Phase: Phase 3
  • # of Trials: 2
  • # of Trial Organizations: 4

Trials by Phase

Trial Phase Start Date Organizations Indications

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