Saroglitazar (INN, trade name Lipaglyn) is a drug for the treatment of type 2 diabetes mellitus, dyslipidemia, NASH and NAFLD 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.
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]
Concerns have been raised regarding increase in serum creatinine with the use of saroglitazar, initially noted in a meta-analysis published by Dutta et. al. [9]
In another randomized controlled trial published by Gawrieh et. al., a mild but significant increase in serum creatinine was noted with 16 weeks use of saroglitazar at 4mg/day dose. [10]
Controversies
In December 2016, Zydus Discovery DMCC, a research subsidiary Zydus Lifesciences, was cited by the US FDA for deliberately misbranding saroglitazar. In a December 21, 2016, letter to the company, the US FDA asked it to stop using broad statements, such as the "world's first" and to stop suggesting that the drug is approved throughout the world, including in the United States, when that is not true. [11]
^Joharapurkar A, Patel V, Kshirsagar S, Patel MS, Savsani H, Jain M (May 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. PMID33753107. S2CID232326306.
^WO 2017089979, Jain M, Joharapurkar A, Kshirsagar S, "Dual PPAR modulators for the treatment of diabetic nephropathy and related diseases", published 1 June 2017, assigned to Cadila Healthcare Limited
^Dutta D, Bhattacharya S, Surana V, Aggarwal S, Singla R, Khandelwal D, Sharma M (Nov–Dec 2020). "Efficacy and safety of saroglitazar in managing hypertriglyceridemia in type-2 diabetes: A meta-analysis". Diabetes & Metabolic Syndrome. 14 (6): 1759–1768. doi:10.1016/j.dsx.2020.08.039. PMID32937280. S2CID221767590.
^Gawrieh S, Noureddin M, Loo N, Mohseni R, Awasty V, Cusi K, et al. (October 2021). "Saroglitazar, a PPAR-α/γ Agonist, for Treatment of NAFLD: A Randomized Controlled Double-Blind Phase 2 Trial". Hepatology. 74 (4): 1809–1824. doi:10.1002/hep.31843. hdl:1805/26913. PMID33811367. S2CID232772287.
