PCSK9 inhibitors have demonstrated their good safety and tolerability in a large number of subjects with different clinical conditions, including statin-intolerance, enlarging their potential use in a broader range of patients. Proprotein convertase subtilisin/kexin type 9 (PCSK9) is an enzyme that binds to low-density lipoprotein receptors (LDL receptors), which stops LDL being removed from the blood, leading to an increase in blood levels of LDL. Further data on long-term mipomersen safety are required. Mechanism of Action of PCSK9 Inhibitors. ... Cardiovascular safety and efficacy of the PCSK9 inhibitor evolocumab in patients with and without diabetes and the effect of evolocumab on glycaemia and risk of new‐onset diabetes: a prespecified analysis of the FOURIER randomised controlled trial. ... current evidence base for use in clinical practice from an efficacy, safety, and cardiovascular outcome. Mechanism of action of PCSK9 inhibitors. This review discusses the mechanisms of action, pharmacokinetics, safety and clinical outcomes of the Alirocumab. On July 24, 2015, the United States Food and Drug Administration (FDA) approved Alirocumab, the first converged proprotein of the Subtilisin Kexin 9 (PCSK9) inhibitor. PCSK9 inhibitors What are PCSK9 inhibitors?