AMG837 (amg-837) is a novel small molecule agonist of the G-protein coupled receptor 40 (GPR40), also known as free fatty acid receptor 1 (FFAR1). This compound has been developed by Amgen for the treatment of type 2 diabetes and related metabolic disorders. In this article, we will provide an overview of AMG837, its chemical properties, health benefits, potential effects, mechanism of action, safety, side effects, and dosing information.
Chemical Properties:
The chemical name of AMG837 is (2S)-2-(4-(4-(4-fluorophenyl)piperazin-1-yl)phenyl)acetic acid. Its molecular formula is C20H21FN2O2, and its formula weight is 342.39 g/mol. The CAS number of AMG837 is 865231-46-5.
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Health Benefits:
AMG837 has been shown to have several health benefits, particularly in the management of type 2 diabetes and related metabolic disorders. It works by activating GPR40, which is predominantly expressed in pancreatic beta-cells and intestinal enteroendocrine cells. This activation leads to increased glucose-dependent insulin secretion, improved glucose homeostasis, and enhanced beta-cell function.
Potential Effects:
AMG837 has demonstrated significant potential in preclinical and clinical studies. In a phase 2a study, AMG837 was found to improve glycemic control and increase insulin secretion in patients with type 2 diabetes. Additionally, it showed favorable effects on body weight and lipid metabolism. In preclinical studies, AMG837 has been shown to reduce glucose intolerance, improve insulin sensitivity, and prevent or reverse the development of fatty liver disease.
Product Mechanism:
AMG837 works by activating GPR40, a G-protein coupled receptor that plays a key role in glucose homeostasis and insulin secretion. GPR40 is predominantly expressed in pancreatic beta-cells and intestinal enteroendocrine cells. When activated by AMG837, GPR40 triggers a signaling cascade that leads to increased insulin secretion in response to glucose. This improves glucose homeostasis and enhances beta-cell function.
Safety:
AMG837 has been well-tolerated in preclinical and clinical studies. In a phase 2a study, no serious adverse events were reported, and the most common adverse events were gastrointestinal in nature. However, like any medication, AMG837 may cause side effects, which are discussed below.
Side Effects:
The most common side effects reported in clinical studies of AMG837 were nausea, diarrhea, vomiting, and abdominal pain. These side effects were generally mild to moderate in severity and resolved without intervention. However, some patients may experience more severe side effects, such as allergic reactions, pancreatitis, or liver toxicity.
Dosing Information:
The optimal dosing regimen for AMG837 has not yet been established. In clinical studies, patients received doses ranging from 25 mg to 600 mg once daily. Further studies are needed to determine the most effective and safe dosing regimen for AMG837.
Conclusion:
AMG837 is a novel GPR40 agonist that has shown significant potential in the treatment of type 2 diabetes and related metabolic disorders. By activating GPR40, AMG837 improves glucose homeostasis, enhances beta-cell function, and reduces insulin resistance. While AMG837 has been well-tolerated in clinical studies, further research is needed to establish its safety and efficacy in larger patient populations. Overall, AMG837 represents a promising new approach to the management of type 2 diabetes and related metabolic disorders
