Saroglitazar

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.

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

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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