Leqvio Inclisiran Sodium Injection

1. Indications and Usage
Primary Hyperlipidemia and Mixed Dyslipidemia:
Indicated as an adjunct to diet and maximally tolerated statin therapy for the treatment of adults with primary hyperlipidemia (including heterozygous familial hypercholesterolemia [HeFH]) or mixed dyslipidemia, to lower LDL-C levels.
Atherosclerotic Cardiovascular Disease (ASCVD):
Indicated in adults with clinical ASCVD who require additional lowering of LDL-C.
Limitation of Use:
The effect of Inclisiran on cardiovascular morbidity and mortality has not been determined.
2. Dosage and Administration
Route of Administration:
For Subcutaneous Injection ONLY. (Must be administered by a healthcare professional).
Recommended Dosage:
Dosing Schedule: 284 mg administered as a single subcutaneous injection initially, again at 3 months, and then every 6 months thereafter.
Missed Dose:
If missed and within 21 days of the scheduled date: Administer as soon as possible and continue with the original schedule.
If missed and >21 days past the scheduled date: Reschedule for the next available appointment (effectively restarting the 6-month cycle from that point).
Administration Instructions:
Inject into the abdomen, upper arm, or thigh. Do not inject into areas with active skin disease, lesions, or inflammation.
3. Mechanism of Action
RNA Interference (RNAi):
Inclisiran is a double-stranded siRNA that targets PCSK9 messenger RNA (mRNA).
Intracellular Inhibition:
Unlike monoclonal antibodies (like Alirocumab) that bind to the PCSK9 protein outside the cell, Inclisiran enters liver cells and prevents the production of the PCSK9 protein. This leads to increased recycling of LDL receptors (LDLR) on the hepatocyte surface, thereby lowering circulating LDL-C levels.
4. Safety and Warnings
Hypersensitivity Reactions:
Hypersensitivity reactions (e.g., rash, urticaria) have been reported. Discontinue if severe.
Pregnancy:
Limited data; use only if clearly needed.
5. Adverse Reactions
Most Common:
Injection site reactions (erythema, pain, swelling, induration), arthralgia, urinary tract infection, diarrhea, bronchitis.
Comparison to Antibodies:
Generally has a similar safety profile to placebo regarding systemic adverse events, with injection site reactions being the primary concern.
6. Drug Interactions
Statin Therapy:
Inclisiran is compatible with statins and does not affect their metabolism. No dose adjustment is required for concomitant use.
7. Pharmaceutical Information
Chemical Composition:
Active Ingredient: Inclisiran Sodium (chemically modified siRNA).
Appearance: Clear to slightly opalescent, colorless to pale yellow solution.
Storage:
Store in a refrigerator at 2°C to 8°C (36°F to 46°F).