Repatha Autoinjector

Repatha Autoinjector Uses, Dosage, Side Effects, Food Interaction and all others data.

Repatha Autoinjector is a monoclonal antibody designed for the treatment of hyperlipidemia by Amgen. It is a subcutaneous injection approved by the FDA for individuals on maximum statin therapy who still require additional LDL-cholesterol lowering. It is approved for both homozygous and heterozygous familial cholesterolemia as an adjunct to other first-line therapies. Repatha Autoinjector is a human IgG2 monoclonal antibody that targets the proprotein convertase subtilisin/kexin type 9 (PCSK9). PCSK9 is a protein that targets LDL receptors for degradation, therefore reducing the liver's ability to remove LDL-cholesterol (LDL-C), or "bad" cholesterol, from the blood. Repatha Autoinjector is designed to bind to PCSK9 and inhibit PCSK9 from binding to LDL receptors on the liver surface, resulting in more LDL receptors on the surface of the liver to remove LDL-C from the blood. Repatha Autoinjector is the second PCSK9 inhibitor on the market, first being alirocumab.

Repatha Autoinjector
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Trade Name	Repatha Autoinjector
Availability	Prescription only
Generic	Evolocumab
Evolocumab Other Names	Evolocumab
Related Drugs	Repatha, Nexletol, Nexlizet, Zetia, Praluent, atorvastatin, Xarelto, simvastatin, rosuvastatin, Lipitor
Weight	140mg/ml, 420mg/3.5ml
Type	Subcutaneous solution
Formula	C₆₂₄₂H₉₆₄₈N₁₆₆₈O₁₉₉₆S₅₆
Weight	141800.0 Da
Groups	Approved
Therapeutic Class
Manufacturer
Available Country	United States
Last Updated:	September 19, 2023 at 7:00 am

Uses

Repatha Autoinjector is a PCSK9 (proprotein convertase subtilisin kexin type 9) inhibitor antibody used as an adjunct to LDL cholesterol reducing therapies, aiding in the prevention of cardiovascular events and cardiovascular revascularization procedures.

For the treatment of heterozygous/homozygous familial hypercholesterolemia or clinical atherosclerotic cardiovascular disease in patients on maximum tolerated statin therapy requiring additional LDL-cholesterol lowering.

Repatha Autoinjector is also used to associated treatment for these conditions: Atherosclerotic Cardiovascular Diseases, Heterozygous Familial Hypercholesterolemia, Homozygous Familial Hypercholesterolemia

How Repatha Autoinjector works

Repatha Autoinjector is a human IgG monoclonal antibody which targets PCSK9 (proprotein convertase subtilisin/kexin type 9). PCSK9 is a serine protease produced by the liver which binds LDL receptors and creates a complex to be targeted for lysosomal degradation. LDL receptors typically bind LDL-cholesterol ("bad" cholesterol) for cellular reuptake, therefore the formation of these complexes with PCSK9 inhibits LDL receptor recycling to the cell surface, resulting in decreased cellular reuptake of LDL-C and increased levels of free LDL-C in the plasma. Individuals with familial hypercholesterolemia often may have "gain of function" mutations in the PCSK9 molecules in their body, resulting in increased LDL-C plasma levels and a consequent cardiovascular risk. Repatha Autoinjector is able to bind both the normal PCSK9 and the "gain of function" mutant, D374Y. The exact mechanism of the binding has not been published, however the precursor molecule, mAb1, is indicative of the interaction. The mAb1 molecule binds on the catalytic site of PCSK9 next to the binding site for the LDL receptor and creates hydrogen bonds and hydrophobic interactions, resulting in the steric inhibition of binding between PCSK9 and the LDL receptor. Because the formation of complexes between LDL receptor and PCSK9 are prevented, the internalized LDL receptors are less likely to be degrated by lysosomes and may recycle to the surface of the cell to serve their function of removing LDL from the blood.