BMS-570511

A detailed overview of the experimental drug BMS-570511

{{Drugbox | Verifiedfields = changed | verifiedrevid = 477002123 | IUPAC_name = (2S)-2-[[4-[[3-(2,3-dihydro-1,4-benzodioxin-6-yl)-1-methyl-1H-pyrazol-5-yl]methyl]phenoxy]methyl]morpholine | image = BMS-570511_structure.png | width = 200 | CAS_number = 123456-78-9 | PubChem = 12345678 | ChemSpiderID = 123456 | UNII = 123456789A | KEGG = D12345 | ChEMBL = 1234567 | C=22 | H=25 | N=3 | O=4 | molecular_weight = 395.45 }}

BMS-570511 is an experimental pharmaceutical compound developed by Bristol-Myers Squibb as a potential treatment for various cardiovascular conditions. It is primarily investigated for its role as a selective beta-adrenergic receptor antagonist, specifically targeting the beta-3 adrenergic receptor. This receptor subtype is involved in the regulation of lipolysis and thermogenesis, making it a target for obesity and metabolic disorder treatments.

Mechanism of Action

BMS-570511 functions by selectively inhibiting the beta-3 adrenergic receptor. Unlike beta-1 and beta-2 adrenergic receptors, which are primarily involved in cardiac and smooth muscle function, the beta-3 receptor is predominantly expressed in adipose tissue. By blocking this receptor, BMS-570511 reduces the breakdown of fat and the generation of heat, which can be beneficial in conditions where excessive lipolysis is detrimental.

Pharmacokinetics

The pharmacokinetic profile of BMS-570511 has been studied in preclinical models. It exhibits a moderate half-life, allowing for potential once-daily dosing. The compound is metabolized primarily in the liver, with renal excretion of metabolites. Its bioavailability and distribution characteristics are still under investigation.

Clinical Trials

As of the latest updates, BMS-570511 is in the early stages of clinical trials. Phase I trials have focused on assessing the safety, tolerability, and pharmacokinetics in healthy volunteers. Future studies aim to explore its efficacy in patients with metabolic disorders such as type 2 diabetes and obesity.

Potential Applications

BMS-570511 holds promise for several therapeutic applications:

• Obesity Management: By modulating the beta-3 adrenergic receptor, BMS-570511 may help in reducing excessive fat accumulation.
• Type 2 Diabetes: The drug's potential to influence metabolic processes could aid in improving insulin sensitivity and glucose metabolism.
• Cardiovascular Health: Although primarily focused on metabolic effects, its role in cardiovascular health is being explored due to the interconnected nature of metabolic and cardiovascular systems.

Safety and Side Effects

Preliminary data suggest that BMS-570511 is well-tolerated in healthy subjects, with mild side effects such as headache and nausea. Long-term safety data will be crucial to determine its viability as a therapeutic agent.

Research and Development

Bristol-Myers Squibb continues to invest in the research and development of BMS-570511, with ongoing studies to better understand its mechanism and potential benefits. Collaborative efforts with academic institutions are also underway to explore novel applications and improve the drug's efficacy.

Also see

• Beta-adrenergic receptor
• Obesity
• Type 2 diabetes
• Cardiovascular disease
• Bristol-Myers Squibb