Saroglitazar
Also called Lipaglyn, Bilypsa
Part of the metabolic pathway of Saroglitazar. See the timeline on the metabolic highway.
Enzymes that break it down: CYP2C8 and CYP3A4. Wikipedia’s drug infobox says: “Liver (CYP2C8, CYP3A4)” (revision 1369643786).
Overview
Saroglitazar (INN, trade names Lipaglyn, Bilypsa) 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. 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.[1]
Risks and side effects
Safety
No major serious adverse events have been reported; however, long-term cardiovascular safety has not been established.
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.
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.[3]
Pharmacology
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.[6] WP
Chemistry
- Formula
- C25H29NO4S PC
- CAS number
- 495399-09-2 PC
- Molar mass (g/mol)
- 439.6 PC
- IUPAC name (computed by PubChem)
- (2S)
- PC2- ethoxy- 3- [4- [2- [2- methyl- 5- (4- methylsulfanylphenyl) pyrrol- 1- yl] ethoxy] phenyl] propanoic acid - SMILES
- CCO[C@@H]
(CC1=CC=C(C=C1) PCOCCN2C(=CC=C2C3=CC=C(C=C3) SC) C) C(=O) O - InChIKey
- MRWFZSLZNUJVQW-
DEOSSOPVSA- PCN - PubChem CID
- 60151560
Harm reduction information
No harm reduction data is on file for this compound yet. That means no dose, timing or combination data from PsychonautWiki or TripSit. Please don't guess a dose from similar compounds. If you have taken it and feel unwell, contact emergency services or a poison control center.
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Sources
- Other Ramalingam A. Zydus Group launches new diabetic drug. 6 June 2013
- Other Pilla, Viswanath. Zydus bets big on proprietary drugs to boost revenue. Nov 3, 2023
- Journal / agency Munigoti SP, Harinarayan CV. Role of Glitazars in atherogenic dyslipidemia and diabetes: Two birds with one stone?. Indian Journal of Endocrinology and Metabolism. May 2014. doi:10.4103/2230-8210.131134 · PMID 24944919 · PMC4056123
- Journal / agency 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. Nov–Dec 2020. doi:10.1016/j.dsx.2020.08.039 · PMID 32937280
- Journal / agency Gawrieh S, Noureddin M, Loo N, Mohseni R, Awasty V, Cusi K, Kowdley KV, Lai M, Schiff E, Parmar D, Patel P, Chalasani N. Saroglitazar, a PPAR-α/γ Agonist, for Treatment of NAFLD: A Randomized Controlled Double-Blind Phase 2 Trial. Hepatology. October 2021. doi:10.1002/hep.31843 · PMID 33811367
- Other Lipaglyn (Saroglitazar) for Treating Hypertriglycerdemia in Type II Diabetes, India
Text and values on this page are quoted from Wikipedia (CC BY-SA 4.0), PubChem (public domain). Each value links to the exact revision it came from.