Products
Evolocumab was approved in the EU and US in 2015 and in many countries in 2016 in the form of a solution for injection (Repatha).
Structure and properties
Evolocumab is a human IgG2 monoclonal antibody with a molecular mass of 141.8 kDa. It is produced by biotechnological methods.
Effects
Evolocumab (ATC C10AX13) has lipid-lowering properties. It selectively binds to PCSK9 (proprotein convertase subtilisin kexin type 9). This serine protease binds to LDL-C receptors on the surface of liver cells and directs them to degradation in hepatocyte lysosomes. Binding of Evolocumab to PCSK9 increases the concentration of LDL receptors in the cell membrane, resulting in a reduction of LDL-C (low density lipoprotein cholesterol) in the blood as more LDL-C is taken up into liver cells. Evolocumab has a long half-life of 11 to 17 days.
Indications
- Hypercholesterolemia (including heterozygous familial hypercholesterolemia).
- Homozygous familial hypercholesterolemia.
- Reduction in the risk of cardiovascular events in patients at high cardiovascular risk.
Dosage
According to the professional information. The antibody is administered subcutaneously with a pre-filled syringe.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Interaction with statins has been described.
Adverse effects
The most common possible adverse effects include nasopharyngitis, upper respiratory tract infections, influenza, back pain, joint pain, and nausea.
