New technology in the hypolipidemic drugs development. Inclisiran (LEQVIO)

Česká verzia

Authors: Hana Rosolová
Authors place of work: Centrum preventivní kardiologie LF UK v Plzni, 2. interní klinika FN Plzeň
Published in the journal: Vnitř Lék 2022; 68(7): 458-460
Category:
doi: https://doi.org/10.36290/vnl.2022.096

Summary

The development of lipid modifying drugs was expanding during the past 30 years. Statins stay to be the first choice drugs in dyslipidemia treatment. Inhibitors of proprotein convertase subtilisin– kexin type 9 (PCSK9) enzyme in combination with statin and/or ezetimibe represent very effective therapy and better atherosclerotic cardiovascular disease (ASCVD) prevention. Antisense therapy based on oligonucleotides belongs to the new technology drugs. This therapy inhibits translation of some proteins important for the production of atherogenic lipid particles. Inclisiran is a small interfering RNA that suppresses translation of PCSK9 in the liver cells. It is applied subcutaneously twice a year and it represents a big chance for the improvement of ASCVD treatment and prevention.

Keywords:

RNA interference – antisense therapy – statins – inclisiran – dyslipidemia therapy

Zdroje

1. Yamamoto T, Wada F, Harada‑Shiba M. Development of Antisense Drugs for Dyslipidemia. J Atheroscler Thromb. 2016;23(9):1011-1025.

2. Ricotta DN, Frishman W. Mipomersen. A Safe and Effective Antisense Therapy Adjunct to Statins in Patients with Hypercholesterolemia. Cardiol Rev. 2012;20(2):90-95.

3. Warden BA, Duell PB. Volanesorsen for treatment of patients with familial chylomicronemia syndrome. Drugs Today (Barc). 2018;54(12):721-735.

4. Henney NC, Banach M et al. RNA silencing in the management of dyslipidemias. Current Atherosclerosis Reports 2021;23:69.

5. Raal FJ, Kallend D, Ray KK. [ORION-9 Investigators]. Inclisiran for the Treatment of Heterozygous Familial Hypercholesterolemia. N Engl J Med. 2020; 382(16):1520-1530.

6. Ray KK, Wright RS, Kallend D. [ORION-10 and ORION-11 Investigators]. Two Phase 3 Trials of Inclisiran in Patients with Elevated LDL Cholesterol. N Engl J Med. 2020;382(16):1507-1519.