Inclisiran
LEQVIO
What it isSmall interfering RNA that suppresses hepatic PCSK9 synthesis; FDA-approved 2021 for ASCVD and HeFH needing further LDL lowering.
Why this oneTwo maintenance doses a year (SC at day 0, month 3, then every six months) with roughly 50% LDL-C reduction — adherence built into the schedule.
What limits itInjection-site reactions and missed return visits are the main practical barriers.
FDA-approved for
- ASCVD / HeFH — LDL-C lowering (2021)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Hypercholesterolemia / LDL-C lowering (incl. HeFH; adjunct to diet ± other LDL-C-lowering therapies) | Adults | 284 mg SC (abdomen, upper arm, or thigh) once, then again at 3 months | 284 mg SC every 6 months thereafter | 284 mg per dose |
| HeFH or HoFH (adjunct to diet and other LDL-C-lowering therapies) | Peds ≥12 yr | 284 mg SC once, then again at 3 months | 284 mg SC every 6 months thereafter | 284 mg per dose |
Renal No adjustment needed (mild, moderate, or severe impairment; not studied in end-stage renal disease)
Hepatic No adjustment needed (mild to moderate impairment; not studied in severe impairment)
Missed dose <3 months late: administer and keep original schedule; >3 months late: restart schedule (initial dose, again at 3 months, then q6 months)
Instructions
- Administered by a healthcare professional; SC injection into abdomen, upper arm, or thigh
- Do not inject into areas of active skin disease or injury (sunburn, rash, inflammation, infection)
- Inspect visually: clear, colorless to pale yellow; do not use if particulates or discoloration
- LDL-C may be assessed as early as 30 days after initiation, anytime without regard to dose timing
Cautions
- Hypersensitivity reactions incl. anaphylaxis and angioedema reported; contraindicated after prior serious hypersensitivity reaction — advise patients on signs/symptoms and to seek prompt medical attention
Adverse reactions
- Injection site reaction (8%: pain, erythema, rash)
- Arthralgia
- Bronchitis
- Postmarketing: anaphylaxis, angioedema
Pregnancy Discontinue when pregnancy is recognized (or consider ongoing therapeutic needs); may cause fetal harm based on mechanism (LDL-C lowering); no human data; no adverse developmental effects in animals at 5–10x MRHD
Lactation No human data; present in rat milk, but oligonucleotides have poor oral bioavailability — adverse infant impact considered unlikely; weigh benefits against risk
NO BOXED WARNINGS
Classes and tags
Clinical profile
Mechanism of action: Inclisiran ballicule
Open Inclisiran in the interactive console ↗
Memory aids: mascots and interaction avatars
First-in-class PCSK9 siRNA — silences hepatic PCSK9 synthesis
SC at day 0, month 3, then every 6 months (twice-yearly maintenance)
