Azacitidine is not an inhibitor, an inducer or a substrate of CYP-enzymes and it is therefore probably not porphyrinogenic. Side effects such as nausea, vomiting, stress, anxiety and insomnia may be potentially porphyrinogenic.

Amino ribofuranosyl triazine. One terminal and three cyclic tertiary amine functions. One furane heterocyclic component.

Antineoplastic agent effective via multiple mechanisms. Common side effects that can be confused with an acute porphyria attack are vomiting, nausea, abdominal pain, diarrhoea, obstipation and musculoskeletal pain. Other common side effects are neutropenic infections (upper respirtory tract infection, urinary infection, sinuitis, pharyngitis, rhinitis, and herpes simplex), stress, anxiety and insomnia.

Significant

In vitro studies have shown that azactidine is not an inhibitor of CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6 and CYP3A4, or an inducer of CYP1A2, CYP2C19 and CYP3A4/5 via activation of CAR or PXR nuclear receptors (Chen 2010, Keating 2012). In vitro studies have also shown that azacitidine is not metabolized by CYP450-enzymes, UDP-glucuronosyltransferases (UGTs), sulfotransferases (SULTs) and glutathione transferases (GSTs) (SPC). Azacitidine is metabolized by cytidine deaminase (Chabner 1973) and spontaneous hydrolysis (Beisler 1978). 50-85% is excreted in urine, while less than 1% is excreted in faeces. Elimination half-life is 41 ± 8 minutes.