Evolocumab

Generic name: evolocumab
Brand name: Repatha

Drug Class: PCSK9 Inhibitor

Dosage Form: Injection, Pre-filled Syringe, Autoinjector

Route of Administration: Subcutaneous

Dose:

• Pre-filled Syringe: 140 mg/mL
• Autoinjector: 140 mg/mL
• Single-use Vial: 420 mg/3.5 mL

Mechanism of Action: Evolocumab is a monoclonal antibody that inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9). PCSK9 binds to LDL receptors on the surface of hepatocytes, promoting their degradation. By inhibiting PCSK9, evolocumab increases the number of LDL receptors available to clear LDL-C from the blood, thereby lowering low-density lipoprotein cholesterol (LDL-C) levels.

Drug Usage Cases: Evolocumab is used in adults and children aged 10 years and older with homozygous familial hypercholesterolemia (HoFH) or clinical atherosclerotic cardiovascular disease (ASCVD) who require additional lowering of LDL cholesterol. It’s also indicated as an adjunct to diet, alone or in combination with other lipid-lowering therapies.

Drug Contraindications: Contraindicated in patients with a history of a serious hypersensitivity reaction to evolocumab, including angioedema.

Side Effects: Common side effects include injection site reactions, nasopharyngitis, upper respiratory tract infections, and flu-like symptoms. Serious side effects may include allergic reactions.

Warnings: Patients should be monitored for signs of serious hypersensitivity reactions, including angioedema. Evolocumab should be used with caution in patients with a history of hypersensitivity reactions to other monoclonal antibodies.

Use During Pregnancy or Breastfeeding: The safety of evolocumab in pregnant women has not been established. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. There is no information on the excretion of evolocumab into human milk, the effects on the breastfed infant, or the effects on milk production. Therefore, caution should be exercised when evolocumab is administered to a nursing mother.