TY - JOUR
T1 - Inclisiran for the treatment of cardiovascular disease
T2 - A short review on the emerging data and therapeutic potential
AU - Kosmas, Constantine E.
AU - Estrella, Alba Muñoz
AU - Skavdis, Andreas
AU - Genao, Edilberto Peña
AU - Martinez, Ian
AU - Guzman, Eliscer
N1 - Publisher Copyright:
© 2020 Kosmas et al.
PY - 2020
Y1 - 2020
N2 - Proprotein convertase subtilisin kexin 9 (PCSK-9)-targeting therapy has arisen as a new line for the treatment of hyperlipidemia. Inclisiran is a double-stranded small RNA molecule that works by blocking the transcription of PCSK-9, leading to a reduction of PCSK9 levels in the hepatocytes, resulting in an increased expression of low-density lipoprotein (LDL) receptors in the hepatocyte membrane and, as a consequence, it reduces the circulating levels of LDL cholesterol (LDL-C). Compared to the other LDL-C-lowering medications, such as statins, ezetimibe and PCSK-9 inhibitors, inclisiran proposes an infre-quent dosing of twice a year, while simultaneously providing a significant reduction of LDL-C. Its prolonged effect offers an advantage against medication non-compliance, which is one of the main causes for not achieving LDL-C goals with standard therapy. Inclisiran has also proven to have a relatively safe profile with adverse effects occurring in similar frequency as with placebo. This review aims to present and discuss the current clinical and scientific data pertaining to the role of inclisiran in the management of hypercholesterolemia and treatment of cardiovascular disease (CVD).
AB - Proprotein convertase subtilisin kexin 9 (PCSK-9)-targeting therapy has arisen as a new line for the treatment of hyperlipidemia. Inclisiran is a double-stranded small RNA molecule that works by blocking the transcription of PCSK-9, leading to a reduction of PCSK9 levels in the hepatocytes, resulting in an increased expression of low-density lipoprotein (LDL) receptors in the hepatocyte membrane and, as a consequence, it reduces the circulating levels of LDL cholesterol (LDL-C). Compared to the other LDL-C-lowering medications, such as statins, ezetimibe and PCSK-9 inhibitors, inclisiran proposes an infre-quent dosing of twice a year, while simultaneously providing a significant reduction of LDL-C. Its prolonged effect offers an advantage against medication non-compliance, which is one of the main causes for not achieving LDL-C goals with standard therapy. Inclisiran has also proven to have a relatively safe profile with adverse effects occurring in similar frequency as with placebo. This review aims to present and discuss the current clinical and scientific data pertaining to the role of inclisiran in the management of hypercholesterolemia and treatment of cardiovascular disease (CVD).
KW - CVD
KW - Cardiovascular disease
KW - Hypercholesterolemia
KW - Inclisiran
KW - PCSK-9
KW - Proprotein convertase subtilisin kexin 9
UR - https://www.scopus.com/pages/publications/85094661560
U2 - 10.2147/TCRM.S230592
DO - 10.2147/TCRM.S230592
M3 - Review article
AN - SCOPUS:85094661560
SN - 1176-6336
VL - 16
SP - 1031
EP - 1037
JO - Therapeutics and Clinical Risk Management
JF - Therapeutics and Clinical Risk Management
ER -