Instructions and marketing status of inclisiran sodium

1. Name:inclisiran, inclisiran sodium

Product name:Leqvio, Leqvio

2. Indications:

Inclisiran is indicated as an adjunct to diet and statins in the treatment of adults with primary hyperlipidemia, including heterozygous familial hypercholesterolemia [HeFH], to lower low-density lipoprotein cholesterol (LDL-C).

3. Usage and dosage:

1. Recommended dose: The recommended dose of inkslan sodium and statin combination therapy is284mg. It should be injected as a single subcutaneous injection at the beginning, then injected after 3 months, and then injected every 6 months. If the planned dose is missed by less than 3 months, use Inkslan sodium and maintain the dose according to the patient's original schedule. If a scheduled dose is missed by more than 3 months, restart a new dosing schedule with inkslan sodium initially, restart after 3 months, and then every 6 months. Assess LDL-C when clinically indicated. The LDL-lowering effect of inkslan sodium can be measured 30 days after initiation and at any time thereafter, regardless of the time of administration.

2. Medication management: Inkslan sodium should be administered by health care professionals. Inkslan sodium is injected subcutaneously into the abdomen, upper arm, or thigh. Do not inject into areas of active skin disease or injury, such as sunburn, rash, inflammation, or skin infection. Visually inspect Inkslan Sodium before use. It should be clear, colorless to pale yellow. Do not use if particulate matter or discoloration is seen. For more detailed instructions on administering prefilled syringes, see Instructions for Use.

4. Adverse reactions:

In clinical studies of Inkslan sodium, the most common adverse reactions include injection site reactions (pain, redness and rash), joint stiffness, urinary tract infection, diarrhea, bronchitis, limb pain and dyspnea.

5. Supply and storage:

Inkslan Sodium Injection is a transparent, colorless to light yellow solution containing 284mg/1.5mL (189mg/mL) of Inkslan Sodium. Store it at a controlled room temperature of 20°C to 25°C (68°F to 77°F) with tolerances Between 15°C and 30°C (59°F and 86°F).

6. Taboo:

Inkslan sodium is contraindicated in patients who have had a previous severe hypersensitivity reaction to inkslan sodium or any of its excipients, including angioedema.

7. Mechanism of action:

Inkslan sodium is a double-stranded small interfering ribonucleic acid (siRNA) that binds to trimeric N-acetylgalactosamine (GalNAc) on the sense strand to promote hepatocyte uptake. In liver cells, Inkslan sodium utilizes theRNA interference mechanism and directs the catalytic breakdown of PCs K9mRNA. This increases recycling and expression of LDL-C receptors on the surface of hepatocytes, thereby increasing LDL-C uptake and reducing circulating LDL-C levels.

8. Listing situation:

Inkslan sodium was approved by the European Medicines Agency (EMA) in December 2020 for use in the European Union. The trade name isLeqvio. In August 2021, it received NICE approval from the British National Health Service. In December 2021, it was approved for medical use in the United States. The U.S. Food and Drug Administration (FDA) considers it a first-in-class drug. In August 2023, the State Administration of Medical Products approved the use of Inkslan sodium in China, with the trade name of Lecowe.

Reference materials:https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=6fc0afca-4513-4c35-b594-6544aee29a44