Repatha

Evolocumab Instructions
Common name: Evolocumab
Trade name: Repatha
All names: Evolocumab, Repatha, Evolocumab

Indications:
For homozygous familial hypercholesterolemia in adults or adolescents over 12 years old.
It can be used in combination with dietary therapy and other low-density lipoprotein (LDL)-lowering treatments (such as statins, ezetimibe, LDL apheresis) for patients with homozygous familial hypercholesterolemia (HoFH) who need further lowering of low-density lipoprotein cholesterol (LDL-C).
For the treatment of adults with atherosclerotic cardiovascular disease (ASCVD) to reduce the risk of myocardial infarction, stroke and coronary revascularization.

Dosage:
Administered by subcutaneous injection
Primary hyperlipidemia with established clinical atherosclerotic CVD or HeFH: 140 mg every 2 weeks or 420 mg once monthly in the abdomen, thigh, or upper arm.
HoFH: 420 mg once monthly.
Administer 420 mg as 3 consecutive injections of REPATHA over 30 minutes.

Adverse Reactions:
Nasopharyngitis, upper respiratory tract infection, influenza, back pain, and injection site reactions.

Contraindications:
Patients with a history of severe allergic reaction to REPATHA.

Precautions:
Allergic Reactions: Rash and hives have occurred. If signs or symptoms of a serious allergic reaction occur, discontinue treatment with REPATHA, follow standard medical care, and monitor until signs and symptoms resolve.

Storage:
Save in refrigerator (2℃～8℃), do not freeze. Prefilled syringes and prefilled pens should be placed in the original carton to protect them from light. If taken out of the refrigerator, it can be stored in the original carton at room temperature of 20°C to 25°C, but it must be used within 30 days. Do not shake before removing.

Mechanism of action:
Evolocumab is a human monoclonal immunoglobulin G2 (IgG2) that targets human proprotein convertase subtilisin kexin type 9 (PCSK9).
Ebolocumab has high affinity for PCSK9 (LDL receptor degradation-promoting protein) and inhibits the binding of PCSK9 to LDL receptors. Furthermore, in cultured human hepatocyte cell lines, LDL uptake was reduced and PCSK9 stimulation was increased.
In hamsters, Ebolocumab increased the amount of LDL receptor protein in the liver and lowered non-HDL-cholesterol. LDL-cholesterol is reduced in monkeys.

Safety and efficacy:
The LAPLACE-2 trial is a 12-week randomized double-blind controlled trial that confirmed that the PCSK9 inhibitor Evolocumab + statin can significantly reduce LDL levels compared with statin alone.
For patients receiving high-intensity statin therapy, the addition of evolocumab can reduce LDL-C levels to 35 mg/dL at 12 weeks; for the high-intensity rosuvastatin group, the addition of evolocumab (once a month ) can reduce the 12-week LDL-C level to 33 mg/dL, and evolocumab (every 2 weeks) can reduce the 12-week LDL-C level to 37 mg/dL; compared with baseline, LDL-C has been reduced by 59%-65%.
For patients receiving moderate-intensity statin therapy, the addition of evolocumab reduced LDL-C levels to 39-49 mg/dL at 12 weeks, a 59%-66% reduction from baseline. The statin + ezetimibe group only reduced LDL-C by 24%.