Tesaglitazar Explained

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]

Notes and References

  1. Wilding JP, Gause-Nilsson I, Persson A . 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 . September 2007 . 17907109 . 10.3132/dvdr.2007.040 . 896195 . free .
  2. Web site: GALIDA (tesaglitazar) Clinical Trial Report Summaries . 2008-03-17 . AstraZeneca .
  3. Web site: AstraZeneca Discontinues Development of GALIDA (tesaglitazar) . 2012-07-23 . 2006-05-04 . AstraZeneca .
  4. Kalliora C, Kyriazis ID, Oka SI, Lieu MJ, Yue Y, Area-Gomez E, Pol CJ, Tian Y, Mizushima W, Chin A, Scerbo D, Schulze PC, Civelek M, Sadoshima J, Madesh M, Goldberg IJ, Drosatos K . 6 . Dual peroxisome-proliferator-activated-receptor-α/γ activation inhibits SIRT1-PGC1α axis and causes cardiac dysfunction . JCI Insight . 5 . 17 . August 2019 . 31393858 . 6777908 . 10.1172/jci.insight.129556 .

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