crosses the blood–brain barrier, so anastrozole would still expected to reduce estradiol levels in the central nervous system to a certain degree. The plasma protein binding of anastrozole is 40%. The metabolism of anastrozole is by N-dealkylation, hydroxylation, and glucuronidation. Inhibition of aromatase is due to anastrozole itself rather than to metabolites, with the major circulating metabolite being inactive. The elimination half-life of anastrozole is 40 to 50 hours (1.7 to 2.1 days). This allows for convenient once-daily administration. The medication is eliminated predominantly by metabolism in the liver (83 to 85%) but also by residual excretion by the kidneys unchanged (11%). Anastrozole is excreted primarily in urine but also to a lesser extent in feces. Chemistry Anastrozole is a nonsteroidal benzyltriazole. It is also known as α,α,α',α'-tetramethyl-5-(1H-1,2,4-triazol-1-ylmethyl)-m-benzenediacetonitrile. Anastrozole is structurally related to letrozole, fadrozole, and vorozole, with all being classified as azoles. History Anastrozole was patented by Imperial Chemical Industries (ICI) in 1987 and was approved for medical use, specifically the treatment of breast cancer, in 1995. Society and culture Generic names Anastrozole is the generic name of the drug and its , , , and . Brand names Anastrozole is primarily sold under the brand name Arimidex. However, it is also marketed under a variety of other brand names throughout the world. Availability Anastrozole is available widely throughout the world. Research Anastrozole is surprisingly ineffective at treating gynecomastia, in contrast to selective estrogen receptor modulators like tamoxifen. Anastrozole was under development for the treatment of female infertility but did not complete development and hence was never approved for this indication. An anastrozole and levonorgestrel vaginal ring (developmental code name BAY 98–7196) was under development for use as a hormonal contraceptive and treatment for endometriosis, but development was discontinued in November 2018 and the formulation was never marketed. Anastrozole increases testosterone levels in males and has been studied as an alternative method of androgen replacement therapy in men with hypogonadism. However, there are concerns about its long-term influence on bone mineral density in this patient population, as well as other adverse effects. References External links 27-Hydroxylase inhibitors Aromatase inhibitors AstraZeneca brands Hormonal antineoplastic drugs Nitriles Peripherally selective drugs Triazoles World Anti-Doping Agency prohibited substances World Health Organization essential medicines Wikipedia medicine articles ready to translate