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| Trade names | Lipaglyn, Bilypsa |
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| Routes of administration | Oral |
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| Protein binding | 99% |
| Metabolism | Liver (CYP2C8, CYP3A4) |
| Eliminationhalf-life | 5.6 hours |
| Excretion | Bile duct |
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| Formula | C25H29NO4S |
| Molar mass | 439.57 g·mol−1 |
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Saroglitazar (INN, trade namesLipaglyn,Bilypsa) is a drug for the treatment oftype 2 diabetes mellitus,dyslipidemia,NASH andNAFLD It is approved for use in India by theDrug Controller General of India.[1][2] Saroglitazar is indicated for the treatment of diabetic dyslipidemia andhypertriglyceridemia with type 2 diabetes mellitus not controlled bystatin therapy. In clinical studies, saroglitazar has demonstrated reduction oftriglycerides (TG), LDLcholesterol, VLDL cholesterol, non-HDL cholesterol and an increase in HDL cholesterol a characteristic hallmark of atherogenic diabetic dyslipidemia (ADD). It has also shownanti-diabetic medication properties by reducing the fasting plasma glucose andHBA1c in diabetes patients.
Saroglitazar is aninsulin sensitizer. It is a first in class drug which acts as a dualPPAR agonist at the subtypes α (alpha) and γ (gamma) of theperoxisome proliferator-activated receptor (PPAR). Agonist action onPPARα lowers high blood triglycerides, and agonist action onPPARγ improvesinsulin resistance and consequently lowers blood sugar.[3]
Being a dual PPAR agonist, saroglitazar helps in controlling blood glucose and lipid parameters, especially hightriglycerides and high non-HDL cholesterol.[4][5][6] A study done in rats concluded that saroglitazar has the potential to prevent the progression ofretinopathy in diabetes patients.[7] Using preclinical models, it has also been shown to be useful indiabetic nephropathy.[8]
No major serious adverse events have been reported; however, long-term cardiovascular safety has not been established.[9]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.[10]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.[11]
In December 2016, Zydus Discovery DMCC, a research subsidiaryZydus 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.[12]
