Drugs Aromatase inhibitors

The optimal drug, dose, sequence, and duration of administration of aromatase inhibitors in the adjuvant setting are not known. 

Morales L, Neven P, Timmerman D, Christiaens MR, Vergote I, Van Limbergen E, et al. (2004) Acute effects of tamoxifen and third-generation aromatase inhibitors on menopausal symptoms of breast cancer patients. Anticancer Drugs 15 753-760... 

Drugs that can be used to control tumour cell proliferation inhibit a variety of enzymes, including thymidylate synthase and topoisomerase (Chapter 20). The enzyme aromatase converts a ring in a steroid to an aromatic ring. It converts, for example, adrenal steroid hormones into female sex hormones, which bind to oestrogenic receptors in the ovary or breast and increase the risk of ovarian or breast cancer. Aromatase inhibitors are used to treat patients with breast or ovarian cancers that are sensitive to oestrogen. Unfortunately, none of the inhibitors is specific for enzymes in tumour cells and they can therefore have severe side-effects (Chapter 21). 

The increasing clinical importance of tamoxifen in the 1980s prompted development of drugs that indirectly target the estrogen receptor, for example the aromatase inhibitor anastrozole (ARIMIDEX ), a selective inhibitor of estrogen biosynthesis [28]. Progress in treatment of hormone-dependent prostate cancer followed advances in breast cancer, with demonstration that... 

Baston, E., Klein, C. D., Grimminger, W., Hebecker, N., and Hartmann, R. W. (2001) Synthesis, evaluation and QSAR studies of highly potent aromatase inhibitors of the piperidinedione type. Anticancer Drug Des. 16, 37-47. 

Uses Advanced breast CA in postmenopausal Action Nonst oidal aromatase inhibitor Dose 2.5 mg/d PO Caution [D, ] Contra PRO Disp Tabs SE Anemia, N, hot flashes, arthralgia Interactions t Risk of interference w/ action of drug W/ estrogens and OCPs EMS None OD May cause N s5rmptomatic and supportive... 

Miller WR, Jackson J. The therapeutic potential of aromatase inhibitors. Exp Opin Invest Drugs 2003 12 337-51. 

Androgen antagonists are drugs that directly Inhibit the actions of androgens, or indirecdy inhibit production of androgens, and are also used in medicine. See ANTIANDROGENS AROMATASE INHIBITORS. 

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