Saroglitazar Explained

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.

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] 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]

Notes and References

  1. News: Zydus Group launches new diabetic drug . Ramalingam A . The Times of India . 6 June 2013 .
  2. News: Lipaglyn (Saroglitazar) for Treating Hypertriglycerdemia in Type II Diabetes, India . https://web.archive.org/web/20140512225804/http://www.drugdevelopment-technology.com/projects/-lipaglyn-saroglitazar-treating-type-ii-diabetes/ . 12 May 2014. Drug Development and Technology.
  3. Manoria PC, Chopra HK, Parashar SK, Dutta AL, Pinto B, Mullasari A, Prajapati S . The nuances of atherogenic dyslipidemia in diabetes: focus on triglycerides and current management strategies . Indian Heart Journal . 65 . 6 . 683–690 . December 2013 . 24407538 . 3905264 . 10.1016/j.ihj.2013.10.015 .
  4. Chatterjee S, Majumder A, Ray S . Observational study of effects of Saroglitazar on glycaemic and lipid parameters on Indian patients with type 2 diabetes . Scientific Reports . 5 . 7706 . January 2015 . 25573251 . 4287720 . 10.1038/srep07706 . 2015NatSR...5E7706C .
  5. Ramakrishnan S . From 'Make in India' to 'Made in India': the saroglitazar story . Indian Heart Journal . 67 . 1 . 8–10 . 2015 . 25820041 . 4382552 . 10.1016/j.ihj.2015.02.014 .
  6. Joharapurkar A, Patel V, Kshirsagar S, Patel MS, Savsani H, Jain M . Effect of dual PPAR-α/γ agonist saroglitazar on diabetic retinopathy and oxygen-induced retinopathy . European Journal of Pharmacology . 899 . 174032 . May 2021 . 33753107 . 10.1016/j.ejphar.2021.174032 . 232326306 .
  7. Jain M, Joharapurkar A, Kshirsagar S . WO . 2017089979 . Dual PPAR modulators for the treatment of diabetic nephropathy and related diseases . Cadila Healthcare Limited . 1 June 2017 .
  8. Munigoti SP, Harinarayan CV . Role of Glitazars in atherogenic dyslipidemia and diabetes: Two birds with one stone? . Indian Journal of Endocrinology and Metabolism . 18 . 3 . 283–287 . May 2014 . 24944919 . 4056123 . 10.4103/2230-8210.131134 . free .
  9. Dutta D, Bhattacharya S, Surana V, Aggarwal S, Singla R, Khandelwal D, Sharma M . Efficacy and safety of saroglitazar in managing hypertriglyceridemia in type-2 diabetes: A meta-analysis . Diabetes & Metabolic Syndrome . 14 . 6 . 1759–1768 . Nov–Dec 2020 . 32937280 . 10.1016/j.dsx.2020.08.039 . 221767590 .
  10. Gawrieh S, Noureddin M, Loo N, Mohseni R, Awasty V, Cusi K, Kowdley KV, Lai M, Schiff E, Parmar D, Patel P, Chalasani N . 6 . Saroglitazar, a PPAR-α/γ Agonist, for Treatment of NAFLD: A Randomized Controlled Double-Blind Phase 2 Trial . Hepatology . 74 . 4 . 1809–1824 . October 2021 . 33811367 . 10.1002/hep.31843 . free . 232772287 . 1805/26913 .
  11. Web site: Dandekar V . 28 December 2016 . The Economic Times . Cadila Healthcare misbranded Saroglitazar, says US FDA .

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