PCSK9 Inhibitors: Are We on the Verge of a Breakthrough?

摘要: Statins are first-line therapy for lowering cholesterol and reducing cardiovascular events. A significant need new lipid-modifying therapies remains patients unable to tolerate statins or achieve guideline-based targets. Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a key regulator of LDL receptor recycling. Gain-of-function PCSK9 mutations associated with high low-density lipoprotein (LDL-C) levels increased risk coronary artery disease, while loss-of-function variants result in low LDL-C decreased monoclonal antibody inhibitors have been developed lower up 70% clinical trials. These well tolerated, serious adverse event rates. Phase III outcome trials these agents ongoing will determine their efficacy events address long-term safety concerns.