Viburnum

by | Mar 16, 2018 | Viburnum

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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

  1. ^ 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.
  2. ^ "GALIDA (tesaglitazar) Clinical Trial Report Summaries". AstraZeneca. Retrieved 2008-03-17. [dead link]
  3. ^ "AstraZeneca Discontinues Development of GALIDA (tesaglitazar)". AstraZeneca. 2006-05-04. Retrieved 2012-07-23.
  4. ^ 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.
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