Tesaglitazar

Tesaglitazar
Clinical data
ATC code	None;
Legal status
Legal status	Development terminated;
Identifiers
	IUPAC name (2S)-2-Ethoxy-3-[4-[2-(4-methylsulfonyloxyphenyl); ethoxy]phenyl]propanoic acid;
CAS Number	251565-85-2 ;
PubChem CID	208901;
ChemSpider	180999 ;
UNII	6734037O3L;
KEGG	D01274 ;
ChEMBL	ChEMBL521632 ;
CompTox Dashboard (EPA)	DTXSID4048773 ;
ECHA InfoCard	100.201.079
Chemical and physical data
Formula	C20H24O6S
Molar mass	392.47 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CCO[C@@H](CC1=CC=C(C=C1)OCCC2=CC=C(C=C2)OS(=O)(=O)C)C(=O)O;
	InChI InChI=1S/C20H24O6S/c1-3-25-19(20(21)22)14-16-6-8-17(9-7-16)26-13-12-15-4-10-18(11-5-15)27-28(2,23)24/h4-11,19H,3,12-14H2,1-2H3,(H,21,22)/t19-/m0/s1 ; Key:CXGTZJYQWSUFET-IBGZPJMESA-N ;
	(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.

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[pmid17907109-1] 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.

[title-2] "GALIDA (tesaglitazar) Clinical Trial Report Summaries". AstraZeneca. Retrieved 2008-03-17. ^{[dead link‍]}

[AstraZeneca_tesaglitazar_press_release)-3] "AstraZeneca Discontinues Development of GALIDA (tesaglitazar)". AstraZeneca. 2006-05-04. Retrieved 2012-07-23.

[KallioraKyriazis2019-4] 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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Clinical data

ATC code	None
Legal status
Legal status	Development terminated
Identifiers
IUPAC name (2S)-2-Ethoxy-3-[4-[2-(4-methylsulfonyloxyphenyl) ethoxy]phenyl]propanoic acid
CAS Number	251565-85-2^Y
PubChem CID	208901
ChemSpider	180999^N
UNII	6734037O3L
KEGG	D01274^Y
ChEMBL	ChEMBL521632^N
CompTox Dashboard (EPA)	DTXSID4048773
ECHA InfoCard	100.201.079
Chemical and physical data
Formula	C₂₀H₂₄O₆S
Molar mass	392.47 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES CCO[C@@H](CC1=CC=C(C=C1)OCCC2=CC=C(C=C2)OS(=O)(=O)C)C(=O)O
InChI InChI=1S/C20H24O6S/c1-3-25-19(20(21)22)14-16-6-8-17(9-7-16)26-13-12-15-4-10-18(11-5-15)27-28(2,23)24/h4-11,19H,3,12-14H2,1-2H3,(H,21,22)/t19-/m0/s1^N Key:CXGTZJYQWSUFET-IBGZPJMESA-N^N
^NY (what is this?) (verify)