|
Synonyms: ALN-60212 | ALN-PCSsc | Leqvio®
inclisiran is an approved drug (EMA (2020), FDA & UK MHRA (2021))
Compound class:
Nucleic acid
Comment: Inclisiran is a small interfering RNA (siRNA) class drug that targets the proprotein convertase subtilisin kexin type 9 (PCSK9) mRNA, to reduce production of the PCSK9 protein [6].
Individual nucleotides are chemically modified to improve stability, and the structure has terminal GalNac (sugar) conjugation for hepatic targeted delivery. We have been unable to locate a full chemical SMILES for the drug, or its HELM notation. |
| References |
|
1. Hovingh GK, Lepor NE, Kallend D, Stoekenbroek RM, Wijngaard PLJ, Raal FJ. (2020)
Inclisiran Durably Lowers Low-Density Lipoprotein Cholesterol and Proprotein Convertase Subtilisin/Kexin Type 9 Expression in Homozygous Familial Hypercholesterolemia: The ORION-2 Pilot Study. Circulation, 141 (22): 1829-1831. [PMID:32479195] |
|
2. Hughes-Hubley F, Iskander M, Cheng-Lai A, Frishman WH, Nawarskas J. (2022)
Inclisiran: Small Interfering Ribonucleic Acid Injectable for the Treatment of Hyperlipidemia. Cardiol Rev, 30 (4): 214-219. [PMID:35666780] |
|
3. Lamb YN. (2021)
Inclisiran: First Approval. Drugs, 81 (3): 389-395. [PMID:33620677] |
|
4. Raal FJ, Kallend D, Ray KK, Turner T, Koenig W, Wright RS, Wijngaard PLJ, Curcio D, Jaros MJ, Leiter LA et al.. (2020)
Inclisiran for the Treatment of Heterozygous Familial Hypercholesterolemia. N Engl J Med, 382 (16): 1520-1530. [PMID:32197277] |
|
5. Ray KK, Wright RS, Kallend D, Koenig W, Leiter LA, Raal FJ, Bisch JA, Richardson T, Jaros M, Wijngaard PLJ et al.. (2020)
Two Phase 3 Trials of Inclisiran in Patients with Elevated LDL Cholesterol. N Engl J Med, 382 (16): 1507-1519. [PMID:32187462] |
|
6. Tsamoulis D, Rallidis LS, Kosmas CE. (2024)
Inclisiran: the preclinical discovery and development of a novel therapy for the treatment of atherosclerosis. Expert Opin Drug Discov, 19 (7): 773-782. [PMID:38804735] |
