[PCSK9 inhibitors: emerging treatment to lower cholesterol?].
The achievement rate of recommended low-density lipoprotein cholesterol (LDL-C) targets of < 1.8 mmol/l for secondary prevention in very high risk patients is difficult. Observational studies reported that loss of function mutation of the PCS9 was associated with LDL-C decrease level and reduction of cardiovascular events. Monoclonal antibodies to PCSK9 (REGN727 and AMG 145, PSCK9 inhibitors) have been tested in clinical studies of phase I and II and showed LDL-C level reduction of 60-70% compared to placebo. This approach appears safe and well-tolerated. The PCSK9 inhibitors are now tested in large phase III clinical studies to assess the long-term safety and efficacy of this new promising approach.
B
B
Gencer
N
N
Rodondi
F
F
Mach
D000924:Anticholesteremic Agents / Q000494:pharmacology / Q000627:therapeutic use*; D008078:Cholesterol, LDL / Q000097:blood; D006801:Humans; D006938:Hyperlipoproteinemia Type II / Q000188:drug therapy*; D000071449:Proprotein Convertase 9; D043484:Proprotein Convertases / Q000037:antagonists & inhibitors*; D012697:Serine Endopeptidases
D000924:Anticholesteremic Agents; D008078:Cholesterol, LDL; C472125:PCSK9 protein, human; D000071449:Proprotein Convertase 9; D043484:Proprotein Convertases; D012697:Serine Endopeptidases