• Antimetabolites, Antineoplastic
• Enzyme Inhibitors

• 5 AZC
• Azacitidina [INN-Spanish]
• Azacitidine [USAN:INN]
• Azacitidinum [INN-Latin]
• Azacytidine
• Ladakamycin
• Mylosar
• Vidaza

C₈H₁₂N₄O₅

http://www.rxlist.com/cgi/generic3/vidaza.htm

No information avaliable

244.205 g/mol

229 ^oC

8.9E+004 mg/L

Solid

-3.017

Azacitidine for injectable suspension is supplied as a lyophilized powder in 100 mg single-use vials packaged in cartons of 1 vial.

For treatment of patients with the following myelodysplastic syndrome subtypes: refractory anemia or refractory anemia with ringed sideroblasts (if accompanied by neutropenia or thrombocytopenia or requiring transfusions), refractory anemia with excess blasts, refractory anemia with excess blasts in transformation, and chronic myelomonocytic leukemia.

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.

Azacitidine is rapidly absorbed after subcutaneous administration. The bioavailability of subcutaneous azacitidine relative to IV azacitidine is approximately 89%, based on area under the curve.

One case of overdose with azacitidine was reported during clinical trials. A patient experienced diarrhea, nausea, and vomiting after receiving a single IV dose of approximately 290 mg/m2, almost 4 times the recommended starting dose.

Humans and other mammals