Generic
Inclisiran
1 brands available in the market
At a glance
Inclisiran is a small interfering RNA (siRNA) directed to PCSK9 mRNA used to reduce LDL-C levels in patients with hypercholesterolemia, heterozygous familial hypercholesterolemia (HeFH), and homozygous familial hypercholesterolemia (HoFH).
Description
Inclisiran is a double-stranded small interfering RNA (siRNA) conjugated on the sense strand with triantennary N-Acetylgalactosamine (GalNAc) to facilitate uptake by hepatocytes. In hepatocytes, inclisiran utilizes the RNA interference mechanism and directs catalytic breakdown of mRNA for PCSK9. This increases LDL-C receptor recycling and expression on the hepatocyte cell surface, which increases LDL-C uptake and lowers LDL-C levels in the circulation.
Indications
- Hypercholesterolemia in adults
- Heterozygous familial hypercholesterolemia (HeFH) in adults and pediatric patients aged 12 years and older
- Homozygous familial hypercholesterolemia (HoFH) in pediatric patients aged 12 years and older
Therapeutic class
Other Anti-anginal & Anti-ischaemic drugs
Pharmacological class
siRNA Therapy (PCSK9 Inhibitor)
Pharmacology
Inclisiran is a double-stranded small interfering RNA (siRNA) conjugated with GalNAc for hepatocyte uptake. In hepatocytes, it utilizes the RNA interference mechanism to direct catalytic breakdown of mRNA for PCSK9. This increases LDL-C receptor recycling and expression on the hepatocyte cell surface, increasing LDL-C uptake and lowering circulating LDL-C levels.
Mechanism of action
Directs catalytic breakdown of PCSK9 mRNA through RNA interference mechanism; increases LDL-C receptor expression and lowers circulating LDL-C levels.
Dosage
Adult and Pediatric (≥12 years) Dose (Subcutaneous):
- Recommended dose: 284 mg
- Initial dose, then at 3 months, then every 6 months
- If a planned dose is missed by <3 months: administer and maintain original schedule
- If a planned dose is missed by >3 months: restart with new schedule (initial, at 3 months, then every 6 months)
Administration
Administer as subcutaneous injection; assess LDL-C when clinically indicated; LDL-lowering effect may be measured as early as 30 days after initiation and anytime thereafter without regard to timing of dose.
Missed dose
If a planned dose is missed by less than 3 months, administer and maintain original schedule; if missed by more than 3 months, restart with new dosing schedule.
Side effects
Common Adverse Reactions (≥3%):
- Injection site reaction
- Arthralgia
- Bronchitis
Precautions & warnings
Precautions:
- Hypersensitivity reactions have been reported; advise patients on signs and symptoms and instruct them to seek medical attention promptly
Contraindications
Contraindications:
- Prior serious hypersensitivity to inclisiran or any of the excipients
Drug interactions
No significant drug interactions known.
Food interactions
No food interaction found/established.
Use in pregnancy
Use in Pregnancy: Advise pregnant patients and patients who can become pregnant of potential risk to fetus; inform healthcare provider of known or suspected pregnancy to discuss if inclisiran should be discontinued.
Use in lactation
Use in Lactation: No information on presence of inclisiran in human milk, effects on breastfed infant, or effects on milk production; present in milk of lactating rats.
Pediatric use
Recommended for pediatric patients aged 12 years and older; safety and efficacy not established in children under 12 years.
Geriatric use
No specific dosage adjustment needed for elderly.
Renal / hepatic impairment
No specific data for renal or hepatic impairment.
Overdose effects
No information on overdose.
Storage conditions
Keep below 30°C temperature, away from light & moisture; keep out of reach of children.
Chemical structure
Inclisiran