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1637637-70-7

1637637-70-7 Structure

1637637-70-7 Structure
IdentificationBack Directory
[Name]

Pelacarsen
[CAS]

1637637-70-7
[Synonyms]

Pelacarsen
Chemical PropertiesBack Directory
[form ]

Solid
[color ]

White to off-white
[Sequence]

DNA, d([2′-O-(2-methoxyethyl)]m5rU-sp-[2′-O-(2-methoxyethyl)]rG-[2′-O-(2-methoxyethyl)]m5rC-[2′-O-(2-methoxyethyl)]m5rU-[2′-O-(2-methoxyethyl)]m5rC-m5C-sp-G-sp-T-sp-T-sp-G-sp-G-sp-T-sp-G-sp-m5C-sp-T-sp-[2′-O-(2-methoxyethyl)]m5rU-[2′-O-(2-methoxyethyl)]rG-[2′-O-(2-methoxyethyl)]m5rU-sp-[2′-O-(2-methoxyethyl)]m5rU-sp-[2′-O-(2-methoxyethyl)]m5rC), 5′-[26-[[2-(acetylamino)-2-deoxy-β-D-galactopyranosyl]oxy]-14,14-bis[[3-[[6-[[2-(acetylamino)-2-deoxy-β-D-galactopyranosyl]oxy]hexyl]amino]-3-oxopropoxy]methyl]-8,12,19-trioxo-16-oxa-7,13,20-triazahexacos-1-yl hydrogen phosphate]
Hazard InformationBack Directory
[Uses]

Pelacarsen (AKCEA-APO(a)-LRx) is a liver-specific antisense oligonucleotide against apolipoprotein(a) that reduces lipoprotein(a) up to 80% with good tolerability[1].
[in vivo]

Mice dosed with Pelacarsen at dose levels of 0.3, 1, 3, and 10?mg/kg once weekly for 6 weeks had dose-dependent reductions in target mRNA expression. The model-estimated doses for Pelacarsen that produced 50% of maximum drug-induced inhibitory effect (ED50) for liver apo(a) mRNA and plasma apo(a) protein levels were 0.32 and 0.54?mg/kg/week, respectively.

[References]

[1] Yu RZ, Graham MJ, Post N, et al. Disposition and Pharmacology of a GalNAc3-conjugated ASO Targeting Human Lipoprotein (a) in Mice. Mol Ther Nucleic Acids. 2016;5(5):e317. DOI:10.1038/mtna.2016.26
[2] Yu RZ, Gunawan R, Post N, et al. Disposition and Pharmacokinetics of a GalNAc3-Conjugated Antisense Oligonucleotide Targeting Human Lipoprotein (a) in Monkeys. Nucleic Acid Ther. 2016;26(6):372-380. DOI:10.1089/nat.2016.0623
[3] Yeang C, et al. Effect of Pelacarsen on Lipoprotein(a) Cholesterol and Corrected Low-Density Lipoprotein Cholesterol. J Am Coll Cardiol. 2022 Mar 22;79(11):1035-1046. DOI:10.1016/j.jacc.2021.12.032
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