Repatha Evolocumab Injection

1. Indications and Usage
Primary Hypercholesterolemia and Mixed Dyslipidemia: Used as an adjunct to diet and maximally tolerated statin therapy, or as an alternative in patients who are intolerant to statins, to lower LDL-C levels.
Heterozygous Familial Hypercholesterolemia: Used in combination with other lipid-lowering therapies to lower LDL-C.
Homozygous Familial Hypercholesterolemia: Used in combination with diet and other lipid-lowering treatments (e.g., statins, ezetimibe, LDL apheresis) in patients aged 12 years and older.
Cardiovascular Disease: Reduces the risk of myocardial infarction, stroke, and coronary revascularization in adult patients with established atherosclerotic cardiovascular disease (ASCVD).
2. Dosage and Administration
Route of Administration: For Subcutaneous (SC) Injection ONLY.
Recommended Dosage:
ASCVD, HeFH, or Mixed Dyslipidemia: 140 mg every 2 weeks OR 420 mg once monthly.
Homozygous Familial Hypercholesterolemia (HoFH): 420 mg once monthly.
Critical Administration Instructions:
Site Selection: Administer in the abdomen, thigh, or upper arm. Rotate injection sites within the same area.
High-Dose Administration: For the 420 mg once-monthly dose, three consecutive 140 mg injections must be given within a 30-minute period.
Missed Dose: If a missed dose occurs within 7 days of the scheduled date, administer immediately and resume the original schedule. If more than 7 days have passed, wait for the next scheduled dose.
Preparation: Allow the pre-filled syringe or autoinjector to reach room temperature for at least 30 minutes before administration. Do not heat using other methods.
3. Mechanism of Action
PCSK9 Inhibition: Evolocumab is a human monoclonal antibody that specifically binds to and inhibits human proprotein convertase subtilisin/kexin type 9 (PCSK9).
LDL Receptor Recycling: By inhibiting PCSK9, it prevents the degradation of LDL receptors on the surface of hepatocytes, leading to increased hepatic uptake and clearance of LDL-C from the bloodstream.
4. Safety and Warnings
Hypersensitivity: Contraindicated in patients with severe hypersensitivity to evolocumab or any excipients (e.g., anaphylaxis, urticaria).
Hypersensitivity Monitoring: Monitor patients for signs of allergic reactions during and after administration. Discontinue the drug if a serious reaction occurs.
Pregnancy and Lactation: Safety data in pregnant women are limited. The risk-benefit balance must be carefully evaluated before use.
5. Adverse Reactions and Clinical Research
Most Common Adverse Reactions: Injection site reactions (erythema, swelling, pain, pruritus), nasopharyngitis, influenza, back pain, and arthralgia.
Clinical Research Highlights: The FOURIER trial demonstrated that evolocumab significantly reduced the risk of major adverse cardiovascular events (MACE) and lowered LDL-C levels without increasing the risk of new-onset diabetes or neurocognitive impairment.
6. Drug Interactions
Statins and Other Lipid-Lowering Agents: No clinically significant pharmacokinetic interactions have been observed. It is designed to be used in combination with these agents.
CYP450 Substrates: Evolocumab does not affect CYP450 enzymes and has no potential for pharmacokinetic interactions with drugs metabolized by these enzymes.
7. Pharmaceutical Information
Chemical Composition: Active Ingredient: Evolocumab. Excipients: Acetic acid, polysorbate 80, proline, sodium hydroxide, and water for injection.
Appearance: Clear to slightly opalescent, colorless to pale yellow solution.
Packaging: 1 mL single-use pre-filled syringe or SureClick® autoinjector (140 mg/mL).
Storage: Store in a refrigerator at 2°C to 8°C. Do not freeze or shake. It may be stored in the original packaging at room temperature up to 25°C for a single period of no more than 30 days.