Daily Medication Pearl: Evolocumab (Repatha)

Evolocumab is a PCSK9 inhibitor indicated to reduce the risk of myocardial infarction, stroke, and coronary revascularization in adults with established cardiovascular disease.

Medication Pearl of the Day: Evolocumab (Repatha)

Indication: Evolocumab is a proprotein convertase subtilisin kexin type 9 (PCSK9) inhibitor antibody indicated to reduce the risk of myocardial infarction, stroke, and coronary revascularization in adults with established cardiovascular disease.

Insight:

  • Evolocumab is also indicated as an adjunct to diet, alone or in combination with other lipid-lowering therapies (e.g., statins, ezetimibe) for the treatment of adults with primary hyperlipidemia to reduce low-density lipoprotein (LDL) cholesterol and as an adjunct to diet and other LDL-lowering therapies (e.g., statins, ezetimibe) in patients with homozygous familial hypercholesterolemia (HoFH) who require additional lowering of LDL-C.
  • Dosing: 140 mg every 2 weeks or 420 mg once monthly in abdomen, thigh, or upper arm.
  • Dosage form: 140 mg/mL solution in a single-use prefilled syringe, 140 mg/mL solution in a single-use prefilled SureClick autoinjector, and 420 mg/3.5 mL solution in a single-use Pushtronex system.
  • Adverse events (AEs): Common AEs include nasopharyngitis, upper respiratory tract infection, influenza, back pain, and injection site reactions.
  • Mechanism of action: Evolocumab is a human monoclonal IgG2 directed against human PCSK9, which binds to PCSK9 and inhibits circulating PCSK9 from binding to the LDL receptor (LDLR), preventing PCSK9-mediated LDLR degradation and permitting LDLR to recycle back to the liver cell surface. By inhibiting the binding of PCSK9 to LDLR, evolocumab increases the number of LDLRs available to clear LDL from the blood, thereby lowering LDL-C levels.
  • Manufacturer: Amgen

Source:

REPATHA (evolocumab) injection, for subcutaneous use (fda.gov)