Naslov
Proprotein convertase subtilisin kexin 9 inhibitors: new class of lipid-lowering therapy

Autori
Bulum, Tomislav ; Duvnjak , Lea

Izvornik
Diabetologia Croatica (0351-0042) 44 (2015); 21-30

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
proprotein convertase subtilisin kexin 9; PCSK9; LDL-cholesterol; hypercholesterolemia; cardiovascular disease

Sažetak
Elevated LDL-cholesterol level is a major risk factor for cardiovascular disease (CVD) and atherosclerosis. LDL-cholesterol is cleared from circulation by the LDL receptor (LDL-R). Proprotein convertase subtilisin kexin 9 (PCSK9), an enzyme secreted into the plasma by the liver, binds the LDL-R in complex which is then subject to endocytosis and degradation in lysosomes. PCSK9 inhibitors prevent LDL-R degradation, the LDL-R recycling is preserved, with a consequent increase in receptor density on the hepatocyte surface and LDL-cholesterol clearance. In recent years, human monoclonal antibodies against PCSK9 have been identified as an innovative lipidlowering strategy. Clinical trials confirmed that treatment with PCSK9 antibodies combined with statins, as well as in monotherapy produces profoundreductions in total, LDL-cholesterol and lipoprotein(a), with a similar level of safety and survival benefit compared with no anti-PCSK9 treatment. Confirmation of these findings in ongoing, long-term trials will establish the role of these novel agents in reducing the risk of CVD.

Izvorni jezik
Engleski

Znanstvena područja
Kliničke medicinske znanosti

POVEZANOST RADA