Lerochol (Lerodalcibep-liga) instructions in Chinese

1. Common names:Lerochol, Lerodalcibep-liga

2. Indications:

Lerochol (Lerodalcibep-liga) is indicated as an adjunct to diet and exercise to reduce low-density lipoprotein cholesterol in adults with hypercholesterolemia, including heterozygous familial hypercholesterolemia (HeFH).

3. Usage and dosage:

1. Recommended dose: The recommended dose of Lerochol is 300 mg, subcutaneous injection once a month. Assess LDL-C when clinically indicated. The LDL-lowering effect of Lerochol can be measured 4 weeks after initiation or, if monthly dosing is continued, at any time thereafter, regardless of the time of administration.

2. Adjustment of missing doses

1) Less than7 days later, instruct the patient to use Lerochol as soon as possible and resume the patient's original monthly dosage plan;

2) Seven (7) days or more, instruct patients to use Lerochol as soon as possible and start a new monthly dosage plan based on that date.

3. Medication management:

Train patients and/or their caregivers how to prepare anduse Lerochol according to the instructions for use, and instruct them to read and follow the instructions for use each time Lerochol is used. Before use, if Lerochol has been refrigerated, allow it to warm to room temperature25°C (77°F) for at least 30 minutes. Visually inspect LEROCHOL before dosing. LEROCHOL is a clear to slightly opalescent, brown to amber solution. Do not use if solution is cloudy or contains particles.

InjectLerochol subcutaneously into the abdomen or front of the thigh. If the injection is given by a medical professional or caregiver, the back of the upper arm can also be the injection site. Do not inject into areas of skin that are tender, bruised, red, or hardened. Rotate injection sites with each dose. Touse the full300 mg dose, push the plunger down until the syringe is empty before removing from the injection site.

4. Adverse reactions:

In clinical studies of Lerochol, the most common adverse reactions in patients with primary hyperlipidemia included nasopharyngitis, local injection site reactions, and peripheral edema; the most common adverse reactions in patients with HeFH were injection site reactions, nasopharyngitis, diarrhea, nausea, and peripheral edema.

5. Supply and storage:

Lerochol Injection 300mg/1.2mL (250mg/mL) is a clear to slightly opalescent, tan to amber, sterile, preservative-free solution in a single-dose prefilled syringe for subcutaneous injection. Lerochol is packaged in a carton containing a single-dose prefilled syringe (NDC 84685-300-01).

Store refrigerated in original carton at 2°C to 8°C (36°F to 46°F) to avoid light. Do not freeze. Don't shake. If desired, Lerochol can be stored in the original carton at room temperature, up to 25°C (77°F), and must be used within 3 months of removal from the refrigerator. Throw away Lerochol if not used within 3 months. Do not use beyond the expiration date on the container or packaging.

6. Mechanism of action:

Lerodalcibep is a novel third-generation PCSK9 inhibitor engineered as a recombinant fusion protein. It consists of a specific PCSK9-binding domain, called the appendage, fused to human serum albumin (HSA). The accessory component binds with high affinity to proprotein convertase subtilisin/kexin type 9 (PCSK9), a key regulator of cholesterol metabolism that normally promotes lysosomal degradation of the low-density lipoprotein receptor (LDLR) on the surface of hepatocytes. By inhibiting the interaction between PCSK9 and LDLR, lerodalcibep prevents receptor degradation, thereby increasing LDLR abundance and recycling. Upregulation of hepatic LDLRs enhances clearance of circulating LDL cholesterol (LDL-C). Fusion to human serum albumin exerts a key pharmacokinetic function by preventing rapid renal clearance and prolonging the plasma half-life of the drug, which facilitates convenient dosing regimens compared to native peptides.

Reference materials:https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=422f8b04-6ce8-4e64-a0a9-0ccc9a4a5860