Saroglitazar tablet is indicated for the treatment of diabetic dyslipidemia and hypertriglyceridemia in patients with type 2 diabetes mellitus not adequately controlled with statin therapy. Clinical studies have shown that Saroglitazar reduces triglycerides (TG), low-density lipoprotein (LDL), very-low-density lipoprotein (VLDL), and non-HDL cholesterol, while increasing HDL cholesterol. It also improves glycemic control by reducing fasting plasma glucose and glycosylated hemoglobin (HbA1c) levels in diabetic patients.

Saroglitazar is a potent, predominantly peroxisome proliferator-activated receptor (PPAR)-alpha agonist with moderate PPAR-gamma activity. PPARs are nuclear lipid-activated transcription factors that regulate genes involved in lipid metabolism, glucose homeostasis, and inflammatory processes. Saroglitazar exhibits both anti-dyslipidemic and anti-diabetic effects mainly through activation of PPAR-α and PPAR-γ pathways respectively.

Activation of PPAR-α by saroglitazar increases hepatic fatty acid oxidation and reduces triglyceride synthesis and secretion. This leads to increased diversion of fatty acids from peripheral tissues (such as skeletal muscle and adipose tissue) to the liver, thereby reducing fatty acid synthesis and triglyceride delivery to peripheral tissues. It also enhances lipolysis and clearance of triglyceride-rich particles from plasma by activating lipoprotein lipase (LPL) and reducing apolipoprotein C-III production. Additionally, it increases apolipoproteins A-I and A-II, thereby raising HDL cholesterol levels and reducing LDL cholesterol.

Although primarily a PPAR-α agonist, saroglitazar also activates PPAR-γ, regulating insulin-responsive genes involved in glucose production, transport, and utilization. It increases expression of genes such as adiponectin, fatty acid binding protein (aP2), LPL, fatty acid transport protein (FATP), and CD36. Through these actions, it reduces postprandial free fatty acids, improves hepatic insulin sensitivity, decreases metabolic load on liver and muscle, and enhances glucose utilization. Strong antidiabetic and insulin-sensitizing effects have been demonstrated in preclinical studies.

The recommended dose of Saroglitazar is two tablets of 2 mg once a day.

Pediatric Use: The safety and effectiveness of Saroglitazar in children less than 18 years of age have not been established.

Geriatric Use: Considering the comorbidity and concomitant medications in elderly patients, Saroglitazar should be used with caution in geriatric patients.

In vitro studies using recombinant human cytochrome P450 (CYP) enzymes indicate that saroglitazar does not significantly inhibit CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 at tested concentrations (10 μM). Similarly, it does not induce CYP3A4 activity in luciferase-based reporter assays in HepG2 cells at concentrations up to 100 μM. Although formal clinical drug–drug interaction studies have not yet been performed, the tested concentrations are much higher than the mean Cmax, suggesting that clinically significant CYP-mediated interactions are unlikely.

Saroglitazar is contraindicated in patients with known hypersensitivity to saroglitazar or any of its excipients.

In two controlled Phase III clinical trials of 12–24 weeks duration, the most commonly reported adverse events (≥2%) included gastritis, asthenia, and pyrexia. Most adverse events were mild to moderate and did not lead to treatment discontinuation. As clinical trials are conducted under controlled conditions, observed adverse event rates may not directly reflect real-world use.

Pregnancy Category C. The safety of saroglitazar in pregnant women has not been established due to lack of adequate and well-controlled studies. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Patients who become pregnant during treatment should consult their physician.

Lactation: It is not known whether saroglitazar is excreted in human breast milk; therefore, nursing mothers should avoid its use.

Saroglitazar should be used with caution in patients with impaired liver or renal function or a history of myopathy. It should also be used cautiously in type 2 diabetic patients with cardiac disease and episodic congestive heart failure, who should be monitored for signs of worsening heart failure. Patients with rapid weight gain should be evaluated for fluid retention and related conditions such as edema and congestive heart failure.

No cases of overdose have been reported in clinical studies. In suspected overdose, supportive care should be provided, including monitoring of vital signs and clinical condition.

Store below 25°C in a dry place, protected from light and moisture. Keep out of reach of children.