Saroglitazar

Saroglitazar
Clinical data
Trade namesLipaglyn
Pregnancy
category
  • C
Routes of
administration		Oral
ATC code
  • None
Legal status
Legal status
  • Approved in India
Identifiers
IUPAC name
  • (2S)-2-Ethoxy-3-[4-(2-{2-methyl-5-[4-(methylsulfanyl)phenyl]-1H-pyrrol-1-yl}ethoxy)phenyl]propanoic acid
CAS Number
PubChem CID
ChemSpider
UNII
ChEBI
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC25H29NO4S
Molar mass439.57 g·mol−1
3D model (JSmol)
SMILES
  • CSc3ccc(cc3)-c(ccc1C)n1CCOc(cc2)ccc2CC(C(=O)O)OCC
InChI
  • InChI=1S/C25H29NO4S/c1-4-29-24(25(27)28)17-19-6-10-21(11-7-19)30-16-15-26-18(2)5-14-23(26)20-8-12-22(31-3)13-9-20/h5-14,24H,4,15-17H2,1-3H3,(H,27,28)/t24-/m0/s1
  • Key:MRWFZSLZNUJVQW-DEOSSOPVSA-N

Saroglitazar (INN, trade name Lipaglyn) is a drug for the treatment of type 2 diabetes mellitus and dyslipidemia. It is approved for use in India by the Drug Controller General of India.[1] Saroglitazar is indicated for the treatment of diabetic dyslipidemia and hypertriglyceridemia with type 2 diabetes mellitus not controlled by statin therapy. In clinical studies, saroglitazar has demonstrated reduction of triglycerides (TG), LDL cholesterol, VLDL cholesterol, non-HDL cholesterol and an increase in HDL cholesterol a characteristic hallmark of atherogenic diabetic dyslipidemia (ADD). It has also shown anti-diabetic medication properties by reducing the fasting plasma glucose and HBA1c in diabetes patients.

Mechanism of action

Saroglitazar is an insulin sensitizer. It is a first in class drug which acts as a dual PPAR agonist at the subtypes α (alpha) and γ (gamma) of the peroxisome proliferator-activated receptor (PPAR). Agonist action on PPARα lowers high blood triglycerides, and agonist action on PPARγ improves insulin resistance and consequently lowers blood sugar.[2]

Efficacy

Being a dual PPAR agonist, saroglitazar helps in controlling blood glucose and lipid parameters, especially high triglycerides and high non-HDL cholesterol.[3][4][5] A study done in rats concluded that saroglitazar has the potential to prevent the progression of retinopathy in diabetes patients.[6] Using preclinical models, it has also been shown to be useful in diabetic nephropathy.[7]

Safety

No major serious adverse events have been reported; however, long-term cardiovascular safety has not been established.[8]

References

  1. ↑ "Zydus Group launches new diabetic drug". The Times of India. Jun 6, 2013.
  2. ↑ "Lipaglyn (Saroglitazar) for Treating Hypertriglycerdemia in Type II Diabetes, India". Drug Development and Technology.
  3. ↑ Manoria PC, Chopra HK, Parashar SK, Dutta AL, Pinto B, Mullasari A, Prajapati S (December 2013). "The nuances of atherogenic dyslipidemia in diabetes: focus on triglycerides and current management strategies". Indian Heart Journal. 65 (6): 683–90. doi:10.1016/j.ihj.2013.10.015. PMC 3905264. PMID 24407538.
  4. ↑ Chatterjee S, Majumder A, Ray S (January 2015). "Observational study of effects of Saroglitazar on glycaemic and lipid parameters on Indian patients with type 2 diabetes". Scientific Reports. 5: 7706. Bibcode:2015NatSR...5E7706C. doi:10.1038/srep07706. PMC 4287720. PMID 25573251.
  5. ↑ Ramakrishnan S (2015). "From 'Make in India' to 'Made in India': the saroglitazar story". Indian Heart Journal. 67 (1): 8–10. doi:10.1016/j.ihj.2015.02.014. PMC 4382552. PMID 25820041.
  6. ↑ Joharapurkar A, Patel V, Kshirsagar S, Patel M, Savsani H, and Jain M (March 2021). "Effect of dual PPAR-α/γ agonist saroglitazar on diabetic retinopathy and oxygen-induced retinopathy". European Journal of Pharmacology. 899: 174032. doi:10.1016/j.ejphar.2021.174032. PMID 33753107.
  7. ↑ Jain, Mukul; Joharapurkar, Amit; Kshirsagar, Samadhan. "WO2017089979-Dual PPAR modulators for the treatment of diabetic nephropathy and related diseases". WIPO IP portal. WIPO. Retrieved 2 April 2021.
  8. ↑ Munigoti SP, Harinarayan CV (May 2014). "Role of Glitazars in atherogenic dyslipidemia and diabetes: Two birds with one stone?". Indian Journal of Endocrinology and Metabolism. 18 (3): 283–7. doi:10.4103/2230-8210.131134. PMC 4056123. PMID 24944919.
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