Inclisiran

LEQVIO is a small interfering RNA (siRNA) directed to proprotein convertase subtilisin kexin type 9 (PCSK9) mRNA indicated as an adjunct to diet and exercise to reduce low-density lipoprotein cholesterol (LDL-C) in:
adults with hypercholesterolemia.
adults and pediatric patients aged 12 years and older with heterozygous familial hypercholesterolemia (HeFH).
pediatric patients aged 12 years and older with homozygous familial hypercholesterolemia (HoFH).

Dosage & Administration

The recommended dosage of Inclisiran for adults and pediatric patients aged 12 years and older is 284 mg administered as a single subcutaneous injection initially, again at 3 months, and then every 6 months.
If a planned dose is missed by less than 3 months, administer Inclisiran and maintain dosing according to the patient’s original schedule.
If a planned dose is missed by more than 3 months, restart with a new dosing schedule - administer Inclisiran initially, again at 3 months, and then every 6 months.
Assess LDL-C when clinically indicated. The LDL-lowering effect of Inclisiran may be measured as early as 30 days after initiation and anytime thereafter without regard to timing of the dose.

Common adverse reactions in clinical trials (≥ 3%): injection site reaction, arthralgia, and bronchitis.

Inclisiran is a double-stranded small interfering ribonucleic acid (siRNA), conjugated on the sense strand with triantennary N-Acetylgalactosamine (GalNAc) to facilitate uptake by hepatocytes. In hepatocytes, inclisiran utilizes the RNA interference mechanism and directs catalytic breakdown of mRNA for PCSK9. This increases LDL-C receptor recycling and expression on the hepatocyte cell surface, which increases LDL-C uptake and lowers LDL-C levels in the circulation.