Inclisiran

Inclisiran is a double-stranded small interfering ribonucleic acid (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.

• LEQVIO ® is indicated as an adjunct to diet and exercise to reduce low-density lipoprotein cholesterol (LDL-C) in: adults with hypercholesterolemia. adults and pediatric patients aged 12 years and older with heterozygous familial hypercholesterolemia (HeFH).ICD-10: E78.00

• LEQVIO is contraindicated in patients with a prior serious hypersensitivity reaction to inclisiran or any of the excipients in LEQVIO. Serious hypersensitivity reactions have included anaphylaxis and angioedema [see Adverse Reactions (6.2)] .contraindicated

The recommended dosage of LEQVIO for adults and pediatric patients aged 12 years and older is 284 mg administered as a single subcutaneous injection initially, again at 3 months, and then every 6 months. ( 2.1 ) LEQVIO should be administered by a healthcare professional. ( 2.2 ) Inject LEQVIO subcutaneously into the abdomen, upper arm, or thigh. ( 2.2 ) 2.1 Recommended Dosage The recommended dosage of LEQVIO for adults and pediatric patients aged 12 years and older is 284 mg administered as a single subcutaneous injection initially, again at 3 months, and then every 6 months. If a planned dose is missed by less than 3 months, administer LEQVIO and maintain dosing according to the patient’s original schedule. If a planned dose is missed by more than 3 months, restart with a new dosing schedule - administer LEQVIO initially, again at 3 months, and then every 6 months. Assess LDL-C when clinically indicated. The LDL-lowering effect of LEQVIO may be measured as early as 30 days after initiation and anytime thereafter without regard to timing of the dose. 2.2 Important Administration Instructions LEQVIO should be administered by a healthcare professional. Inject LEQVIO subcutaneously into the abdomen, upper arm, or thigh. Do not inject in areas of active skin disease or injury, such as sunburns, skin rashes, inflammation, or skin infections. Inspect LEQVIO visually before use. It should appear clear and colorless to pale yellow. Do not use if particulate matter or discoloration is seen.

Hypersensitivity Reactions: Have been reported in patients treated with LEQVIO. Advise patients on the signs and symptoms of hypersensitivity reactions and instruct patients to seek medical attention promptly. ( 5.1 ) 5.1 Hypersensitivity Reactions Hypersensitivity reactions, including anaphylaxis and angioedema, have been reported in patients treated with LEQVIO [see Adverse Reactions (6.2)] . Advise patients on the signs and symptoms of hypersensitivity reactions and instruct patients to seek medical attention promptly. LEQVIO is contraindicated in patients with a prior serious hypersensitivity reaction to inclisiran or any of the excipients in LEQVIO.

The following adverse reactions are also discussed in other sections of the label: Hypersensitivity Reactions [see Warnings and Precautions (5.1)] Common adverse reactions in clinical trials (≥ 3%): injection site reaction, arthralgia, and bronchitis. ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Novartis Pharmaceuticals Corporation at 1-888-669-6682 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Adverse Reactions in Adults with Hypercholesterolemia The data in Table 1 are derived from 3 placebo-controlled trials that included 1,833 adults with hypercholesterolemia treated with LEQVIO, including 1,682 exposed for 18 months (median treatment duration of 77 weeks) [see Clinical Studies (14)] . The mean age of the population was 64 years, 32% of the population were female, 92% were White, 6% were Black or African American, 1% were Asian, and < 1% were other races; 6% identified as Hispanic or Latino ethnicity. At baseline, 12% of patients had a diagnosis of HeFH and 85% had clinical atherosclerotic cardiovascular disease (ASCVD). Adverse reactions reported in at least 3% of LEQVIO-treated patients, and more frequently than in placebo-treated patients, are shown in Table 1.

8.1 Pregnancy Risk Summary Discontinue LEQVIO when pregnancy is recognized. Alternatively, consider the ongoing therapeutic needs of the individual patient. Inclisiran increases LDL-C uptake and lowers LDL-C levels in the circulation, thus decreasing cholesterol and possibly other biologically active substances derived from cholesterol; therefore, LEQVIO may cause fetal harm when administered to pregnant patients based on the mechanism of action [see Clinical Pharmacology (12.1)] . In addition, treatment of hypercholesterolemia is not generally necessary during pregnancy. Atherosclerosis is a chronic process and the discontinuation of lipid-lowering drugs during pregnancy should have little impact on the outcome of long-term therapy of hypercholesterolemia for most patients. There are no available data on the use of LEQVIO in pregnant patients to evaluate for a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes. In animal reproduction studies, no adverse developmental effects were observed in rats and rabbits with subcutaneous administration of inclisiran during organogenesis at doses up to 5 to 10 times the maximum recommended human dose (MRHD) based on body surface area (BSA) comparison ( see Data ).

Metabolism

Absorption Following a single subcutaneous administration, systemic exposure to inclisiran increased in a linear and dose proportional manner over a range from 25 mg to 800 mg of inclisiran sodium. At the recommended dosing regimen of 284 mg of LEQVIO, plasma concentrations reached peak in approximately 4 hours post dose with a mean C max of 509 ng/mL.

• Dec 22, 2021NDANDA214012Novartis

1. 1Arthralgia78711%
2. 2Myalgia6268.4%
3. 3Injection Site Pain5317.1%
4. 4Low Density Lipoprotein Increased4796.4%
5. 5Pain In Extremity4576.1%
6. 6Pain3885.2%
7. 7Drug Ineffective3865.2%
8. 8Fatigue3845.1%
9. 9Diarrhoea3474.6%
10. 10Dyspnoea3344.5%
11. 11Headache2783.7%
12. 12Rash2613.5%
13. 13Muscle Spasms2393.2%
14. 14Product Storage Error2152.9%
15. 15Dizziness2142.9%

The 10 most recently updated of 77 ClinicalTrials.gov registrations naming Inclisiran as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Study of Inclisiran to Prevent Cardiovascular Events in High-risk Primary Prevention Patients.
  Active not recruiting · Phase 3 · Interventional · 14,012 enrolled · Novartis Pharmaceuticals
  NCT05739383updated 2026-06-11
• Study of Inclisiran to Prevent Cardiovascular (CV) Events in Participants With Established Cardiovascular Disease
  Active not recruiting · Phase 3 · Interventional · 17,004 enrolled · Novartis Pharmaceuticals
  NCT05030428updated 2026-06-11
• Inclisiran Versus Placebo for the Prevention of Major Adverse Cardiovascular and Limb Events in Patients Undergoing Percutaneous Coronary Intervention or Peripheral Endovascular Intervention
  Recruiting · Phase 4 · Interventional · 6,000 enrolled · Duke University
  NCT06909565updated 2026-06-10
• Assessment of Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of a New Formulation of Inclisiran Containing Polysorbate 80 Compared to the Currently Marketed Formulation
  Not yet recruiting · Phase 1 · Interventional · 120 enrolled · Novartis Pharmaceuticals
  NCT07626281updated 2026-06-04
• The Belgian REAL (BE.REAL) Registry
  Active not recruiting · Observational · 600 enrolled · Novartis Pharmaceuticals
  NCT05726838updated 2026-06-02
• Intravascular Imaging Study of the Effect of Inclisiran on Plaque in Patients With Acute Myocardial Infarction
  Recruiting · Phase 4 · Interventional · 318 enrolled · Novartis Pharmaceuticals
  NCT06372925updated 2026-06-02
• Dual PCSK9 Inhibition With Inclisiran and Alirocumab in Secondary Prevention
  Recruiting · Phase 4 · Interventional · 60 enrolled · University Medical Centre Ljubljana
  NCT07581808updated 2026-06-02
• Coronary Computed Tomography Study to Assess the Effect of Inclisiran in Addition to Maximally Tolerated Statin Therapy on Atherosclerotic Plaque Progression in Participants With a Diagnosis of Non-obstructive Coronary Artery Disease Without Previous Cardiovascular Events
  Active not recruiting · Phase 3 · Interventional · 608 enrolled · Novartis Pharmaceuticals
  NCT05360446updated 2026-06-01
• Evaluation of Efficacy and Safety of Early in Hospital Initiation of Inclisiran Treatment in Patients With Acute Coronary Syndromes
  Recruiting · Phase 3 · Interventional · 300 enrolled · Novartis Pharmaceuticals
  NCT07102628updated 2026-06-01
• Inclisiran (Leqvio®) in Patients With Atherosclerotic Vascular Disease and/or Heterozygous Familial Hypercholesterolemia Treated in Spain: the INSPIRE Study
  Active not recruiting · Observational · 198 enrolled · Novartis Pharmaceuticals
  NCT06958315updated 2026-06-01

Frequently asked questions

How does Inclisiran work?

Inclisiran is a double-stranded small interfering ribonucleic acid (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.

What is Inclisiran used for?

According to FDA labeling, Inclisiran carries indications including: LEQVIO ® is indicated as an adjunct to diet and exercise to reduce low-density lipoprotein cholesterol (LDL-C) in: adults with hypercholesterolemia. adults and pediatric patients aged 12 years and older with heterozygous familial hypercholesterolemia (HeFH).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Inclisiran?

Inclisiran is classified as Other lipid modifying agents.

What are the brand names for Inclisiran?

Inclisiran is marketed under brand names including Leqvio.

What are the contraindications for Inclisiran?

Inclisiran labeling lists contraindications including: LEQVIO is contraindicated in patients with a prior serious hypersensitivity reaction to inclisiran or any of the excipients in LEQVIO. Serious hypersensitivity reactions have included anaphylaxis and angioedema [see Adverse Reactions (6.2)] .. Always consult the full prescribing information and a clinician.