Inclisiran: a small interfering RNA strategy targeting PCSK9 to treat hypercholesterolemia

Expert Opin Drug Saf. 2021 Oct 1. doi: 10.1080/14740338.2022.1988568. Online ahead of print.ABSTRACTINTRODUCTION: : Inclisiran is a novel post-transcriptional gene silencing therapy that inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9) synthesis by RNA interference, and has a potent, dose-dependent, durable effect in lowering LDL-C, and therefore is an effective drug to treat dyslipidemia, reducing the risk for acute cardiovascular (CV) events. It is safe and well-tolerated.AREAS COVERED: : This paper aims to review the mechanism of action inclisiran while evaluating its efficacy and safety in the treatment of dyslipidemia from data of the clinical trials in the ORION program.EXPERT OPINION: : Data from the clinical trials in the ORION program demonstrated efficacy and safety of inclisiran in patients with dyslipidemia. Adverse events were similar in the inclisiran and placebo groups in the clinical trials, although injection-site reactions were more frequent with inclisiran than with placebo. Although, the combination of efficacy and safety makes inclisiran a good option for treatment of dyslipidemia compared to other PCSK9 targeting therapeutic strategies, however, further studies should exclude the possibility that inclisiran, through lower-affinity interactions, may influence other mRNAs in the physiological milieu.PMID:34596005 | DOI:10.1080/14740338.2022.1988568
Source: Expert Opinion on Drug Safety - Category: Drugs & Pharmacology Authors: Source Type: research