Inclisiran Application Scope

Inclisiran (Leqvio) is indicated for adult patients with elevated LDL‑C—due to primary hypercholesterolemia, HeFH, ASCVD, or elevated cardiovascular risk—as an adjunct to lifestyle and statin-based therapy, with an indication expanded in July 2023 to include earlier intervention in high-risk individuals without prior events.

Inclisiran Characteristics

Ingredients:
- Active: Synthetic small-interfering RNA (siRNA) targeting PCSK9 mRNA
- Inactive: Formulation-specific excipients (proprietary per FDA label)
Properties:
- Specifically harnesses RNA interference to reduce hepatic PCSK9 production → increases LDL receptors → ~50 % LDL‑C reduction
- Restricted to liver, no impact on DNA, half-life ~9 hours but prolonged effect due to RISC activity

Packaging Specification: Single-dose, prefilled syringe containing 284 mg/1.5 mL (189 mg/mL) clear, colorless to pale yellow solution
Storage: Refrigerated at 2–8 °C; may be kept at room temperature (≤ 25 °C) up to 30 days before use
Expiry Date: (Shelf life) 36 months (3 years) from manufacture
Executive Standard: FDA-approved as a biologic (BLA 125562); meets European Medicines Agency (EMA) and WHO criteria
Approval Number: FDA: BLA 125562, approved December 22, 2021
Date of Revision: Label updates ongoing; safety and dosing information current as of early 2024
Manufacturer: Novartis Pharmaceuticals Corp.

Guidelines for the Use of Inclisiran

Dosage and Administration:
- Initial: 284 mg SC injection on Day 1, then at 3 months, followed by every 6 months
- Administered by a healthcare professional in the thigh, abdomen, or upper arm
- No dose adjustments needed for renal or mild/moderate hepatic impairment
Adverse Reactions:
- ≥ 3% and more frequent than placebo: injection-site reactions (8%), arthralgia (5%), bronchitis (4%), urinary tract infection (4.4%), diarrhea (3.9%), extremity pain (3.3%), dyspnea (3.2%)
- Hypersensitivity including angioedema (rare)
Contraindications: History of serious hypersensitivity reaction to Inclisiran or excipients (e.g., injection components)
Precautions:
- Monitor for hypersensitivity reactions post-injection
- Use caution in severe hepatic or renal impairment (limited data)
- No routine lab monitoring mandated beyond standard lipid panels and safety labs

Inclisiran Interactions

Drug Interactions:
No known clinically meaningful interactions with CYP substrates.
Safe to use with statins, ezetimibe, PCSK9 inhibitors (antibodies)

Note:

If there is a new packaging for the drug, the new packaging shall prevail. The above information is sourced from DengYue Medicine.
It is only for internal discussion among medical staff and does not serve as a basis for medication. For specific medication guidelines, please consult the attending physician.