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Saroglitazar

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{{Drugbox | drug_name = | IUPAC_name = (2S)-2-Ethoxy-3-[4-(2-{2-methyl-5-[4-(methylsulfanyl)phenyl]-1H-pyrrol-1-yl}ethoxy)phenyl]propanoic acid | image = Saroglitazar skeletal.svg

| tradename = Lipaglyn | Drugs.com = | MedlinePlus = | pregnancy_AU = | pregnancy_US = | pregnancy_category= C | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = Approved in India | routes_of_administration = Oral

| bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion =

| CAS_number = 495399-09-2 | ATCvet = | ATC_prefix = None | ATC_suffix = | PubChem = 60151560 | ChemSpiderID = 32079086

| C=25 | H=29 | N=1 | O=4 | S=1 | molecular_weight = 439.56 g/mol | smiles = CSc3ccc(cc3)-c(ccc1C)n1CCOc(cc2)ccc2CC(C(=O)O)OCC | StdInChI = 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 | StdInChIKey = MRWFZSLZNUJVQW-DEOSSOPVSA-N }}

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 favorable Anti-diabetic medication property by reducing the fasting plasma glucose and HBA1c in diabetes patients. The recommended dose of saroglitazar is one tablet of 4 mg once a day.

Mechanism of action

Saroglitazar is novel 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 at 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 (Lipaglyn) helps in controlling blood glucose and Lipid parameters especially high triglycerides and high non HDL-Cholesterol.[3] Lipaglyn effectively reduces triglycerides and non HDL-C and controlles high blood sugar, a typical situation in Insulin Resistance condition.[4][5]

Safety

Saroglitazar has not demonstrated any of the adverse effects like weight gain and edema that are usually identified with similar molecules like the glitazone class of drugs.[6] Because it is an insulin sensitizer, Saroglitazar (Lipaglyn) has less potential for hypoglycemia. No major serious adverse events have been reported; however, long-term cardiovascular safety has not been established.[7]

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. ^ "The nuances of atherogenic dyslipidemia in diabetes: focus on triglycerides and current management strategies". Indian Heart Journal.
  4. ^ "Observational Study of Effects of Saroglitazar on Glycaemic and Lipid Parameters on Indian Patients with Type 2 Diabetes". SCIENTIFIC REPORTS.
  5. ^ "From 'Make in India' to 'Made in India': the saroglitazar story". Indian Heart Journal.
  6. ^ "Observational study to evaluate the safety and efficacy of saroglitazar in Indian diabetic dyslipidemia patients". Indian Heart Journal.
  7. ^ Munigoti, SrinivasaP; Harinarayan, CV (2014). "Role of Glitazars in atherogenic dyslipidemia and diabetes: Two birds with one stone?". Indian Journal of Endocrinology and Metabolism. 18 (3): 283. doi:10.4103/2230-8210.131134. PMC 4056123. PMID 24944919.{{cite journal}}: CS1 maint: unflagged free DOI (link)