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Pelacarsen

Cat. No. M21301
Pelacarsen Structure
Synonym:

AKCEA-APO(a)-LRx; TQJ230

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Biological Activity

Pelacarsen (AKCEA-APO(a)-LRx) is a liver-specific, antisense oligonucleotide targeting apolipoprotein(a) that reduces lipoprotein(a) by 80% and is well tolerated.

Chemical Information
CAS Number 1637637-70-7
Solubility (25°C) N/A
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Trent Wei, et al. Curr Opin Lipidol. Recent lipoprotein(a) trials

[2] Freddy Duarte Lau, et al. JAMA Cardiol. Lipoprotein(a) and its Significance in Cardiovascular Disease: A Review

[3] Calvin Yeang, et al. J Am Coll Cardiol. Effect of Pelacarsen on Lipoprotein(a) Cholesterol and Corrected Low-Density Lipoprotein Cholesterol

[4] Jennifer Hardy, et al. Am J Cardiovasc Drugs. A Review of the Clinical Pharmacology of Pelacarsen: A Lipoprotein(a)-Lowering Agent

[5] Massimiliano Ruscica, et al. Pharmacol Res. Lipoprotein(a): Knowns, unknowns and uncertainties

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