Reaction: Anastrozole to 1 product

Reaction
Reaction type
N-dealkylation
Direction
Major circulating metabolite?
No
Spontaneous?
No
Activity
inactive
References
  1. Kamdem LK, Liu Y, Stearns V, Kadlubar SA, Ramirez J, Jeter S, Shahverdi K, Ward BA, Ogburn E, Ratain MJ, Flockhart DA, Desta Z: In vitro and in vivo oxidative metabolism and glucuronidation of anastrozole. Br J Clin Pharmacol. 2010 Dec;70(6):854-69. doi: 10.1111/j.1365-2125.2010.03791.x. [Article]
  2. FDA Approved Drug Products: Arimidex (anastrozole) oral tablets [Link]
Comments
Triazole (a product of N-dealkylation of anastrozole) has long been considered a major circulating metabolite as per anastrozole's label. Follow-up studies on anastrozole metabolism (Kamdem, et. al. 2010) have failed to detect it in plasma, so the importance of triazole as a metabolite, as well as the process through which it is created, are unclear.
Enzymes
Not Available