Drug intelligence / Profile preview

inclisiran + atorvastatin

Development stage
Unknown
Lead developer
Novartis
Modality
Small Molecules, Chemically Modified siRNA → Small Interfering RNA (siRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Conjugated siRNA → Small Interfering RNA (siRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics
Administration
Subcutaneous, Oral
01

Overview

Inclisiran + atorvastatin is a combination of two lipid-lowering drugs used to reduce elevated low-density lipoprotein cholesterol (LDL-C) and manage primary hypercholesterolemia or mixed dyslipidemia in adults who are unable to achieve target LDL-C levels with maximally tolerated statin therapy. - **Inclisiran** is a double-stranded small interfering RNA (siRNA) conjugated with N-acetylgalactosamine (GalNAc), which targets hepatic proprotein convertase subtilisin/kexin type 9 (PCSK9) mRNA, leading to decreased synthesis of PCSK9 and increased expression of LDL receptors on hepatocytes, thereby lowering circulating LDL-C. - **Atorvastatin** is a synthetic small molecule that competitively inhibits 3-hydroxy-3-methylglutaryl-CoA (HMG-CoA) reductase, the rate-limiting enzyme in cholesterol biosynthesis, resulting in upregulation of hepatic LDL receptors and enhanced clearance of LDL-C. When coadministered, inclisiran and atorvastatin produce **greater reductions in LDL-C and total cholesterol compared with either agent alone**, without evidence of increased toxicity in non-clinical studies, and are both used as part of a lipid-lowering regimen in high-risk cardiovascular patients[1][4][6].

Other names
inclisiran plus atorvastatininclisiran and atorvastatin
02

Targets

PCSK9 (Proprotein convertase subtilisin/kexin type 9)HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)

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