Table 2.

Summary of the Main Scientific and Clinical Attributes of ANGPTL3 Inhibitors

ANGPTL3 protein is implicated in the metabolism of lipids by inhibiting lipoprotein lipase (LPL) and endothelial lipase (EL) in tissues.

Carriers of ANGPTL3 loss-of-function mutations have decreased plasma levels of TG, LDL-C and HDL-C and enjoy a lower risk of CAD by 34–41% compared to non-carriers.

ANGPTL3 inhibitors is a novel lipid-modifying class of agents, capable of reducing circulating LDL-C levels via a mechanism independent of LDL receptors.

Evinacumab is a fully human monoclonal antibody targeting ANGPTL3, which was recently approved by the FDA as a complementary agent to other LDL-C lowering regimens for patients aged 12 or older with HoFH.

In primary studies, evinacumab possesses a favorable safety and tolerability profile, as no serious adverse events were observed.

Evinacumab, administered in patients with hypercholesterolemia, has been shown to significantly reduce LDL-C, TG, and HDL-C by an average of 33.123%, 50.959%, and 12.773%, respectively, as compared with placebo.

ASOs targeting the ANGPTL3 gene mRNA coding sequence may represent an alternative therapeutic strategy for the management of dyslipidemias.