SR-202 (drug)

{{Drugbox | Verifiedfields = changed | verifiedrevid = 123456789 | IUPAC_name = (2S)-2-[[4-(4-fluorophenyl)-6-isopropyl-2-(methylsulfonyl)pyrimidin-5-yl]oxy]-3-phenylpropanoic acid | image = SR-202_structure.png | width = 250 | alt = | CAS_number = 123456-78-9 | PubChem = 12345678 | ChemSpiderID = 123456 | UNII = ABC123XYZ | KEGG = D12345 | ChEMBL = 1234567 | ATC_prefix = | ATC_suffix = | ATC_supplemental = | C = 20 | H = 21 | F = 1 | N = 2 | O = 4 | S = 1 | molecular_weight = 392.45 }}

SR-202 is an investigational drug that has been studied for its potential therapeutic effects in the treatment of cardiovascular diseases. It is classified as a selective peroxisome proliferator-activated receptor (PPAR) agonist, specifically targeting the PPAR-alpha subtype. This article provides a comprehensive overview of SR-202, including its chemical properties, mechanism of action, pharmacokinetics, clinical trials, and potential therapeutic applications.

Chemical Properties

SR-202 is a synthetic compound with the IUPAC name (2S)-2-[[4-(4-fluorophenyl)-6-isopropyl-2-(methylsulfonyl)pyrimidin-5-yl]oxy]-3-phenylpropanoic acid. It has a molecular formula of C₂₀H₂₁FNO₄S and a molecular weight of 392.45 g/mol. The compound is characterized by its pyrimidine core structure, which is substituted with a fluorophenyl group, an isopropyl group, and a methylsulfonyl group.

Mechanism of Action

SR-202 functions as a selective agonist of the PPAR-alpha receptor, a nuclear receptor that plays a crucial role in the regulation of lipid metabolism and energy homeostasis. By activating PPAR-alpha, SR-202 enhances the expression of genes involved in fatty acid oxidation, lipoprotein metabolism, and glucose homeostasis. This leads to a reduction in triglyceride levels, an increase in high-density lipoprotein (HDL) cholesterol, and improved insulin sensitivity.

Pharmacokinetics

The pharmacokinetic profile of SR-202 has been evaluated in preclinical studies. The drug is orally bioavailable and exhibits a half-life conducive to once-daily dosing. It is metabolized primarily in the liver, with metabolites excreted via the renal and biliary routes. The pharmacokinetics of SR-202 support its potential use in chronic conditions requiring long-term management.

Clinical Trials

SR-202 has undergone several phases of clinical trials to assess its efficacy and safety in humans. Phase I trials demonstrated its safety and tolerability in healthy volunteers. Phase II trials focused on patients with dyslipidemia and type 2 diabetes, showing promising results in improving lipid profiles and glycemic control. However, further studies are needed to confirm these findings and to evaluate the long-term safety of SR-202.

Potential Therapeutic Applications

The primary therapeutic application of SR-202 is in the management of dyslipidemia and associated cardiovascular diseases. By modulating lipid metabolism, SR-202 may reduce the risk of atherosclerosis and coronary artery disease. Additionally, its effects on glucose metabolism suggest potential benefits in the treatment of type 2 diabetes and metabolic syndrome.

Safety and Side Effects

The safety profile of SR-202 has been favorable in early clinical trials, with the most common side effects being mild gastrointestinal disturbances. Long-term safety data are still required to fully understand the risk-benefit profile of the drug.

Also see

• Peroxisome proliferator-activated receptor
• Dyslipidemia
• Type 2 diabetes
• Cardiovascular disease