Tesaglitazar
Jump to navigation
Jump to search
Clinical data | |
---|---|
ATC code |
|
Legal status | |
Legal status |
|
Identifiers | |
| |
CAS Number | |
PubChem CID | |
ChemSpider | |
UNII | |
KEGG | |
ChEMBL | |
CompTox Dashboard (EPA) | |
ECHA InfoCard | 100.201.079 |
Chemical and physical data | |
Formula | C20H24O6S |
Molar mass | 392.47 g·mol−1 |
3D model (JSmol) | |
| |
| |
(what is this?) (verify) |
Tesaglitazar (also known as AZ 242) is a dual peroxisome proliferator-activated receptor agonist with affinity to PPARα and PPARγ, proposed for the management of type 2 diabetes.[1]
The drug had completed several phase III clinical trials,[2] however in May, 2006 AstraZeneca announced that it had discontinued further development.[3]
Cardiac toxicity of tesaglitazar is related to mitochondrial toxicity caused by decrease in PPARγ coactivator 1-α (PPARGC1A, PGC1α) and sirtuin 1 (SIRT1).[4]
References
- ^ Wilding JP, Gause-Nilsson I, Persson A (September 2007). "Tesaglitazar, as add-on therapy to sulphonylurea, dose-dependently improves glucose and lipid abnormalities in patients with type 2 diabetes". Diabetes & Vascular Disease Research. 4 (3): 194–203. doi:10.3132/dvdr.2007.040. PMID 17907109. S2CID 896195.
- ^ "GALIDA (tesaglitazar) Clinical Trial Report Summaries". AstraZeneca. Retrieved 2008-03-17.[dead link]
- ^ "AstraZeneca Discontinues Development of GALIDA (tesaglitazar)". AstraZeneca. 2006-05-04. Retrieved 2012-07-23.
- ^ Kalliora C, Kyriazis ID, Oka SI, Lieu MJ, Yue Y, Area-Gomez E, et al. (August 2019). "Dual peroxisome-proliferator-activated-receptor-α/γ activation inhibits SIRT1-PGC1α axis and causes cardiac dysfunction". JCI Insight. 5 (17). doi:10.1172/jci.insight.129556. PMC 6777908. PMID 31393858.
Categories:
- All articles with dead external links
- Articles with dead external links from October 2010
- Articles with short description
- Short description matches Wikidata
- Drugs not assigned an ATC code
- Drugs with non-standard legal status
- Articles with changed ChemSpider identifier
- Articles with changed EBI identifier
- ECHA InfoCard ID from Wikidata
- Articles with changed InChI identifier
- Chemical pages without DrugBank identifier
- Drugboxes which contain changes to verified fields
- Drugboxes which contain changes to watched fields
- Abandoned drugs
- Carboxylic acids
- Phenol ethers
- PPAR agonists
- Benzosulfones
- Ethoxy compounds
- All stub articles
- Gastrointestinal system drug stubs