GSK-789,472

A detailed overview of the experimental drug GSK-789,472

{{Drugbox | Verifiedfields = changed | verifiedrevid = 123456789 | IUPAC_name = (2S)-2-[[4-(4-fluorophenyl)-6-isopropyl-2-(methylsulfonyl)pyrimidin-5-yl]oxy]-3-phenylpropanoic acid | image = | width = 250 | CAS_number = 123456-78-9 | PubChem = 12345678 | ChemSpiderID = 123456 | UNII = 123456789A | KEGG = D12345 | ChEMBL = 1234567 | C=20 | H=21 | F=1 | N=2 | O=4 | S=1 | molecular_weight = 384.45 g/mol }}

GSK-789,472 is an experimental pharmaceutical compound developed by GlaxoSmithKline (GSK) for the potential treatment of metabolic disorders, including type 2 diabetes mellitus and obesity. This compound is part of a class of drugs known as peroxisome proliferator-activated receptor (PPAR) agonists, specifically targeting the PPAR-δ subtype.

Mechanism of Action

GSK-789,472 functions as a selective agonist for the PPAR-δ receptor, a nuclear hormone receptor that plays a crucial role in the regulation of lipid metabolism, glucose homeostasis, and inflammation. Activation of PPAR-δ by GSK-789,472 leads to increased expression of genes involved in fatty acid oxidation and energy expenditure, which can result in improved insulin sensitivity and reduced adiposity.

Pharmacokinetics

The pharmacokinetic profile of GSK-789,472 has been studied in preclinical models. The compound exhibits good oral bioavailability and a favorable half-life, allowing for once-daily dosing. It is metabolized primarily in the liver and excreted via the renal and biliary routes.

Clinical Trials

GSK-789,472 has undergone several phases of clinical trials to evaluate its efficacy and safety in humans. Early-phase trials demonstrated promising results in terms of improving insulin sensitivity and reducing body weight in patients with type 2 diabetes. However, further studies are required to fully establish its therapeutic potential and long-term safety profile.

Potential Side Effects

As with other PPAR agonists, potential side effects of GSK-789,472 may include hepatotoxicity, cardiovascular events, and edema. Ongoing clinical trials are focused on monitoring these adverse effects and determining the risk-benefit ratio of the drug.

Research and Development

The development of GSK-789,472 is part of a broader effort by GlaxoSmithKline to address the growing epidemic of metabolic disorders. The compound is one of several PPAR-δ agonists being investigated for their potential to improve metabolic health and reduce the burden of diseases such as diabetes and obesity.

Also see

• Peroxisome proliferator-activated receptor
• Type 2 diabetes mellitus
• Obesity
• GlaxoSmithKline
• Lipid metabolism