In this article, we will discuss Azacitidine (Mechanism of Action). So, let’s get started.
Mechanism of Action
Azacitidine is a pyrimidine nucleoside
analog of cytidine. Azacitidine is 4-amino-1-β-D-ribofuranosyl-s-triazin-2(1H)-one. The empirical formula is C8H12N4O5. The molecular weight is 244. Azacitidine was found to be insoluble in acetone, ethanol, and methyl ethyl ketone; slightly soluble in ethanol/water (50/50), propylene glycol, and polyethylene glycol; sparingly
soluble in water, water saturated octanol, 5% dextrose in water, N-methyl-2-pyrrolidone, normal
saline and 5% Tween 80 in water; and soluble in dimethylsulfoxide (DMSO).
Azacitidine is a pyrimidine nucleoside analog of cytidine. Azacitidine is believed to exert its antineoplastic effects by causing hypomethylation of DNA and direct cytotoxicity on abnormal hematopoietic cells in the bone marrow. The concentration of azacitidine required for maximum inhibition of DNA methylation in vitro does not cause major suppression of DNA synthesis. Hypomethylation may restore normal function to genes that are critical for differentiation and proliferation. The cytotoxic effects of azacitidine cause the death of rapidly dividing cells, including cancer cells that are no longer responsive to normal growth control mechanisms.
Non-proliferating cells are relatively insensitive to azacitidine.