MK-0616 由默克公司发现和开发,是一种在研的、可能是首个口服 PCSK9 抑制剂,旨在降低低密度脂蛋白 (LDL) 胆固醇。MK-0616 是一种大环肽,可结合 PCSK9 并抑制 PCSK9 与 LDL 受体的相互作用,旨在通过抑制PCSK9可增加LDL-C在血液中的清除。如果不及时治疗,高LDL-C会导致动脉粥样硬化性心血管疾病(ASCVD)事件...
“These data reinforce our confidence that MK-0616 could become the first oral PCSK9 inhibitor, with the potential to change the way patients with hypercholesterolemia who need additional LDL-C reduction are treated. This may allow many more patients ...
(proprotein convertase subtilisin/kexin type 9)-low density lipoprotein receptor interaction with injectable monoclonal antibodies or small interfering RNA lowers plasma low density lipoprotein-cholesterol, but despite nearly 2 decades of effort, an oral inhibitor of PCSK9 is not available. Macrocyclic ...