Daily Medication Pearl: Inclisiran (Leqvio) Injection

Inclisiran treats adults with heterozygous familial hypercholesterolemia or clinical atherosclerotic cardiovascular disease who require additional lowering of low-density lipoprotein cholesterol.

Medication Pearl of the Day: Inclisiran (Leqvio) Injection

Indication: Inclisiran is a small interfering RNA directed to proprotein convertase subtilisin kexin type 9 (PCSK9) mRNA indicated as an adjunct to diet and maximally tolerated statin therapy for the treatment of adults with heterozygous familial hypercholesterolemia or clinical atherosclerotic cardiovascular disease, who require additional lowering of low-density lipoprotein cholesterol (LDL-C).

Insight:

  • Dosing: The recommended dosage of inclisiran, in combination with maximally tolerated statin therapy, is 284 mg administered as a single subcutaneous injection initially, again at 3 months, and then every 6 months.
  • Dosage forms: Injection 284 mg/1.5 mL (189 mg/mL) in a single-dose prefilled syringe.
  • Adverse events: Common adverse reactions in clinical trials (≥ 3%) are injection site reaction, arthralgia, urinary tract infection, diarrhea, bronchitis, pain in extremity, and dyspnea.
  • Mechanism of action: Inclisiran is a double-stranded small interfering ribonucleic acid, conjugated on the sense strand with triantennary N-Acetylgalactosamine to facilitate uptake by hepatocytes. In hepatocytes, inclisiran uses 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.
  • Manufacturer: Novartis

Sources:

Physician's Labeling Rule_Content (novartis.us)

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