Inclisiran 284mg/1.5ml solution for injection pre-filled syringes
Requires a prescription from a doctor or prescriber
Inclisiran is a long-acting, synthetic small interfering RNA (siRNA) directed against proprotein convertase subtilisin-kexin type 9 (PCSK9), which is a serine protease that regulates plasma low-density lipoprotein cholesterol (LDL-C) levels.
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MHRA alerts for Inclisiran
Safety monitoring data
Yellow Card reports
The MHRA Yellow Card scheme collects reports of suspected side effects from healthcare professionals and patients. View the Drug Analysis Profile (iDAP) for real-world adverse reaction data.
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Suspected adverse reactions reported for Inclisiran
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Data from the MHRA Yellow Card scheme. A reported reaction does not necessarily mean the medicine caused it. Contains public sector information licensed under the Open Government Licence v3.0.
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Suspected adverse reactions reported for Inclisiran
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1 branded products available
MHRA licensed products
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Leqvio 284mg/1.5ml solution for injection pre-filled syringes
This is the NHS Drug Tariff indicative price used for reimbursement purposes. It may not reflect the price paid by patients or pharmacies.
View full Drug TariffSource: NHS Drug Tariff via NHSBSA. Derived from dm+d VMPP (Virtual Medicinal Product Pack) pricing data. Contains public sector information licensed under the Open Government Licence v3.0.
WHO defined daily dose (DDD)
1.6 mg
Not a recommended dose. The DDD is the assumed average maintenance dose per day for a drug used for its main indication in adults. It is a statistical measure used for research and comparison purposes only.
Source: WHO Collaborating Centre for Drug Statistics Methodology, distributed via the NHS dm+d supplementary mapping files (NHSBSA). Contains public sector information licensed under the Open Government Licence v3.0.
Therapeutically similar medicines
Similarity is based on WHO Anatomical Therapeutic Chemical (ATC) classification and on a factual NHS dm+d therapeutic-grouping code prefix. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
NHS prescribing volume and spending trends
Guidelines from the National Institute for Health and Care Excellence
NICE clinical guidance(5)
Inclisiran for treating primary hypercholesterolaemia or mixed dyslipidaemia (TA733)
Cardiovascular disease: risk assessment and reduction, including lipid modification (NG238)
Icosapent ethyl with statin therapy for reducing the risk of cardiovascular events in people with raised triglycerides (TA805)
CaRi-Heart for predicting cardiac risk in suspected coronary artery disease: early value assessment (HTG663)
Evinacumab for treating homozygous familial hypercholesterolaemia in people 12 years and over (TA1002)
Source: National Institute for Health and Care Excellence (NICE). Contains public sector information licensed under the Open Government Licence v3.0.
Check stock at pharmacies and supply information
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Pharmacy links redirect to the retailer's own search and do not represent real-time stock levels. Shortage and safety information sourced from MHRA drug safety updates (gov.uk, Crown Copyright under OGL v3.0).
Codes for healthcare professionals and prescribing systems
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NHS UK identifiers
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SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).
Active and completed clinical studies from ClinicalTrials.gov
Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.
Academic studies and reviews for this medicine's active substance
Showing the 50 most relevant studies.
Reviews & meta-analyses: 38 · Randomised trials: 5 · 2017–2026
Showing the 50 most relevant studies, sorted by most relevant.
Sajjad Khan, Arshi Naz, Muhammad Qamar Masood, et al.
The American Journal of Cardiology, 2020
- Ezetimibe
- Injection Site Reaction
- Alanine Transaminase
Min Luo, Yihan Liu, Xinyi Xu, et al.
Frontiers in Pharmacology, 2023
Frederick J. Raal, Ronen Durst, Ran Bi, et al.
Circulation, 2023
- Homozygous Familial Hypercholesterolemia
- Anticholesteremic Agents
- Hydroxymethylglutaryl-CoA Reductase Inhibitors
Jiayi Li, Lei Xiang-Guo, Zihao Li, et al.
Medicine, 2023
- Hyperlipidemias
- Systematic Reviews as Topic
- Cholesterol, LDL
Siddhartha Dutta, Rima Shah, Shubha Singhal, et al.
Expert Opinion on Drug Safety, 2023
- Anticholesteremic Agents
- Cardiovascular Diseases
- Hyperlipidemias
Lawrence A. Leiter, Hwee Teoh, David Kallend, et al.
Diabetes Care, 2018
- Proprotein Convertase 9
- Apolipoproteins B
- Diabetes Mellitus
André Saad Cleto, João Matheus Schirlo, Victor Hugo Oliveira Gomes, et al.
Diabetes Obesity and Metabolism, 2024
- PCSK9 Inhibitors
- Dyslipidemias
- Antibodies, Monoclonal, Humanized
Shengxuan Zhang, Lei Sun, Xinyu Xu, et al.
BMC Cardiovascular Disorders, 2024
- Ezetimibe
- Network Meta-Analysis
- PCSK9 Inhibitors
Ábel T, Benczúr B, Csajbókné ÉC
2026
- Renal Insufficiency, Chronic
- Proprotein Convertase 9
- PCSK9 Inhibitors
Purpose of reviewChronic kidney disease (CKD) significantly increases the risk of atherosclerotic cardiovascular disease (ASCVD), with dyslipidemia-particularly elevated low-density lipoprotein cholesterol (LDL-C)-being a shared risk factor. While statin-based therapies are effective in early-stage CKD, their benefits in dialysis and kidney transplant patients remain inconclusive. Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a key regulator of lipid metabolism. This review aims to summarize the factors influencing PCSK9 levels in CKD patients and evaluate the safety and efficacy of PCSK9 inhibitors across different stages of CKD.Recent findingsMultiple factors have been associated with variations in plasma PCSK9 concentrations in CKD, including glycemic status, proteinuria, renal function, dialysis modality, lipid-lowering therapy, and circadian rhythms. PCSK9 inhibitors, such as alirocumab, evolocumab, and inclisiran, effectively reduce LDL-C and ASCVD risk in patients with mild-to-moderate CKD. However, evidence is limited in patients with advanced CKD (stages 4-5, end stage renal disease (ERSD)), particularly those undergoing dialysis. Elevated PCSK9 levels may not independently predict ASCVD risk in CKD populations. Nonetheless, PCSK9 inhibitors provide a well-tolerated and effective lipid-lowering option in early CKD. Large-scale prospective studies are warranted to clarify their role in patients with ESRD.
Abstract licence: CC BY
Z. Khan, Ajeet Singh, Muhammad Haseeb Ur Rasool, et al.
Annals of Medicine and Surgery, 2025
Sources: aggregated from Europe PMC (EMBL-EBI), OpenAlex, Crossref, PubMed and other open scholarly databases. Retracted articles are excluded. Study information is provided for research purposes and does not constitute medical advice.
Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
None known
Half-life
9 hours
Mechanism
Low-density lipoprotein (LDL) receptors expressed on hepatocytes are responsible…
Food interactions
None known
Human targets
1 target
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
24 mg
Half-life
9 hours
[L30468]
Protein binding
87%
[L30468]
Volume of distribution
500 L
Metabolism
Elimination
16%
[L30468]
Clearance
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
On December 11, 2020, the European Commission (EC) granted authorization for marketing inclisiran as the first and only approved siRNA for the treatment of adults with primary hypercholesterolemia (heterozygous familial and non-familial) or mixed dyslipidemia, alone or in combination with other lipid-lowering therapies.[L28178] Inclisiran was later approved by the FDA on December 22, 2021, for the treatment of heterozygous familial hypercholesterolemia (HeFH) or clinical atherosclerotic cardiovascular disease in adults.[L39593] It is marketed under the trade name Leqvio.
[L30468]
In the US, inclisiran is indicated as an adjunct to diet and exercise to reduce low-density lipoprotein cholesterol (LDL-C) in adults with hypercholesterolemia, including heterozygous familial hypercholesterolemia (HeFH).
[L47251]
[L30468]
Inclisiran is conjugated to triantennary N-acetylgalactosamine carbohydrates, which can bind to asialoglycoprotein receptors expressed in the liver. Binding to asialoglycoprotein receptors facilitates the uptake of inclisiran into the hepatocytes. Once inside the hepatocyte, inclisiran binds to the RNA-induced silencing complex (RISC), which is a ribonucleoprotein complex that serves as a template for recognizing the target complementary mRNA, activate RNAse, and cleave the target mRNA.[A225973] Inclisiran incorporated into the RISC allows the drug to cleave PCSK9 mRNA and prevent PCSK9 translation, thus decreasing hepatic production of PCSK9.[A225953] Less PCSK9 protein available allows more LDL receptors to be recycled to the hepatic membrane for circulating LDL-C uptake.[A225983]
The long-term effect of inclisiran on cardiovascular outcomes has not yet been elucidated,[A225963] although reductions in the levels of LDL-C have been associated with a reduction of cardiovascular risk.[A225953]
How the body processes this drug — absorption, distribution, metabolism, and elimination
The mean AUC0-inf was 7980 ng x h/mL. After 48 hours of dosing, drug plasma concentrations were undetectable. Pharmacokinetic findings following a single-dose administration of inclisiran were comparable to inclisiran administered in multiple doses.
[L30468]
[L30468]
[L30468]
[L30468]
[L30468]
[L30468]
Proteins and enzymes this drug interacts with in the body
PMID:18039658
Acts via a non-proteolytic mechanism to enhance the degradation of the hepatic LDLR through a clathrin LDLRAP1/ARH-mediated pathway. May prevent the recycling of LDLR from endosomes to the cell surface or direct it to lysosomes for degradation.
Can induce ubiquitination of LDLR leading to its subsequent degradation .
PMID:17461796 PMID:18197702 PMID:18799458 PMID:22074827
Inhibits intracellular degradation of APOB via the autophagosome/lysosome pathway in a LDLR-independent manner. Involved in the disposal of non-acetylated intermediates of BACE1 in the early secretory pathway .
PMID:18660751
Inhibits epithelial Na(+) channel (ENaC)-mediated Na(+) absorption by reducing ENaC surface expression primarily by increasing its proteasomal degradation. Regulates neuronal apoptosis via modulation of LRP8/APOER2 levels and related anti-apoptotic signaling pathways
ATC C10AX16
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
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Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Linked compound data from DrugBank Open Data (CC BY-NC 4.0)
Inclisiran
DrugBank citations
If you use DrugBank data in your research, please cite:
- DrugBank 6.02024Recommended citationKnox C., Wilson M., Klinger C.M., et alDrugBank 6.0: the DrugBank Knowledgebase for 2024Nucleic Acids Res. 2024 Jan 552(D1):D1265-D1275
- DrugBank 5.02018Wishart D.S., Feunang Y.D., Guo A.C., et alDrugBank 5.0: a major update to the DrugBank database for 2018Nucleic Acids Res. 2017 Nov 846(D1):D1074-D1082
- DrugBank 4.02014Law V., Knox C., Djoumbou Y., et alDrugBank 4.0: shedding new light on drug metabolismNucleic Acids Res. 2014 Jan 142(1):D1091-7
- DrugBank 3.02011Knox C., Law V., Jewison T., et alDrugBank 3.0: a comprehensive resource for 'omics' research on drugsNucleic Acids Res. 2011 Jan39(Database issue):D1035-41
- DrugBank 2.02008Wishart D.S., Knox C., Guo A.C., et alDrugBank: a knowledgebase for drugs, drug actions and drug targets.Nucleic Acids Research2008 Jan36(Database issue):D901-6
- DrugBank 1.02006Wishart D.S., Knox C., Guo A.C., et alDrugBank: a comprehensive resource for in silico drug discovery and exploration.Nucleic Acids Research2006 Jan 134(Database issue):D668-72