Established and Emerging Approaches for the Management of Dyslipidaemia

Figure 1

Emerging targets for dyslipidemia. The novel drugs that are under development for the treatment of dyslipidemia present several mechanisms of action. Emerging therapeutic agents for LDL lowering will: (a) interfere with lipoprotein synthesis in the liver by silencing apolipoprotein B (apoB) expression (1) or inhibiting microsomal triglyceride transfer protein (MTP) activity (2); (b) promote LDL-receptor activity by silencing (3) or blocking (4) proprotein convertase subtilisin/kexin type 9 (PCSK9). Emerging therapeutic agents affecting HDL will: (c) increase HDL-C plasma levels by blocking cholesteryl ester transfer protein (CETP) (5), or inducing apolipoprotein A-I (apoA-I) expression (6), (d) improve HDL activity by mimicking apoA-I (7) or nascent HDL (8) or increase the expression of receptors favoring cholesterol efflux from cells (9). Emerging therapeutic agents for triglycerides lowering will improve the catabolism of triglycerides and the handling fatty acids by peripheral organs (10), by new formulation of omega 3 fatty acids (11) and by inhibiting the expression of apolipoprotein C-III in the liver (12). Specific silencing of apolipoprotein (a) is also under investigation (13).