Leqvio

Novartis' blockbuster small interfering RNA lipid-lowering new drug LEQVIQ is commercially launched in Hong Kong! Twice a year, long-term lipid reduction, good news for high-end sterolemia!

Its innovative small interfering nucleic acid action mechanism allows patients to obtain lipid-lowering effects with only two subcutaneous injections per year.

Common name: inclisiran

Trade name: Leqvio

Full names: inclisiran, Leqvio

Indications:

For the treatment of primary hypercholesterolemia in adults (heterozygous familial and non- Familial) or mixed dyslipidemia: (1) Leqvio is used in combination with statins or statins and other lipid-lowering therapies to treat patients who cannot achieve LDL-C treatment goals on maximally tolerated statins; (2) Leqvio is used in combination with other lipid-lowering therapies to treat patients who are intolerant to statins or have contraindications to statin drugs.

Usage and dosage:

Administered by subcutaneous injection. After administration once in the 0th and 3rd months, administration once every 6 months in the maintenance period, only 2 injections are needed in a year.

Administration: Subcutaneous Injection Use: Leqvio (inclisiran) is for subcutaneous injection into the abdomen; alternative injection sites include the upper arm or thigh. Injections should not be given in areas with active skin disease or injury, such as sunburn, rash, inflammation, or skin infection.

1. Leqvio (inclisiran) should be visually inspected before administration. The solution should be clear, colorless to pale yellow, and essentially free of particles. The solution should not be used if it contains visible particulate matter.

2. Use a single prefilled syringe for each 284 mg dose; each prefilled syringe is for single use only. This product should only be administered and used by professional medical staff.

Missed dose:

(1) If the planned dose is missed for less than 3 months, Leqvio should be given promptly and continued administration according to the patient's original plan.

(2) If the planned dose is missed for more than 3 months, a new dosing schedule should be started - after one dose in the 0th and 3rd months, and one dose every 6 months in the maintenance period.

Transitioning from treatment with a monoclonal antibody PCSK9 inhibitor to this product: This product can be used immediately after the last use of a monoclonal antibody PCSK9 inhibitor. To maintain low LDL-C, it is recommended to administer this product within 2 weeks after the last use of a monoclonal antibody PCSK9 inhibitor.

Specifications:

284mg/1.5ml

Adverse reactions:

Common adverse reactions include: injection site reactions, such as pain, redness or rash.

Contraindications:

Allergy to the active substance or any excipients listed (water for injection, sodium hydroxide, concentrated phosphoric acid).

Precautions:

Hemodialysis: The effect of hemodialysis on the pharmacokinetics of inclisiran has not been studied. Considering that inclisiran is eliminated by the kidneys, hemodialysis should not be performed for at least 72 hours after inclisiran administration.

Inclisiran is not an inhibitor or inducer of cytochrome P450 enzymes or common drug transporters. Therefore, inclisiran is not expected to cause clinically significant interactions with other drugs. Based on the limited data available, no clinically significant interactions with atorvastatin, rosuvastatin, or other statins are expected.

Use in special populations:

1. The elderly (age ≥65 years): No dose adjustment is required for elderly patients

2. Hepatic impairment: For patients with mild (Child-Pugh Class A) or moderate (Child-Pugh Class B) hepatic impairment, no dose adjustment is required. As there are no data on patients with severe hepatic impairment (Child-Pugh class C), this product should be used with caution in patients with severe hepatic impairment.

3. Renal Impairment: No dosage adjustment is necessary for patients with mild, moderate, or severe renal insufficiency or patients with end-stage renal disease. There is limited experience with the use of this product in patients with severe (severe) renal impairment and this product should be used with caution in these patients.

4. Children: The safety and effectiveness of this product in children under 18 years of age have not been determined.

5. Pregnancy or planning pregnancy: This product should be avoided during pregnancy.

6. Breastfeeding or planning to breastfeed: It is unclear whether this product will pass into breast milk.

Storage:

This medicine does not require any special storage conditions. Does not freeze.

Mechanism of action:

Leqvio is an siRNA therapy. The use of this drug can continuously reduce the incidence of cardiovascular diseases caused by LDL-C in patients. Leqvio can bind to the mRNA encoding PCSK9 protein and prevent the liver from producing PCSK9 protein through RNA interference. The role of the PCSK9 protein is to inhibit the recycling and recycling of LDL receptors. Reducing the level of PCSK9 in the body allows more LDL receptors to return to the surface of liver cells, bind to more LDL, and then remove them from the blood.

Safety and efficacy:

In three series of experiments, ORION-9, ORION-10 and ORION-11, the persistence, effectiveness and safety of Inclisiran in reducing lipids have been verified.

The ORION-9 trial was conducted in 482 adult patients with heterozygous FH. Patients were randomly assigned to receive subcutaneous injections of Inclisiran 300 mg or placebo on days 1, 90, 270, and 450. The final results of the trial showed that at 17 months, compared with baseline, LDL-C levels in the Inclisiran group decreased by 39.7%, while those in the placebo group increased by 8.2%, and the inter-group difference in the rate of change in LDL-C levels was 47.9%. And LDL-C was significantly reduced in FH patients of all genotypes.