title: Aromatase inhibitors: clinical pharmacology and therapeutic implications in breast cancer.
abstract: Aminoglutethimide was the first aromatase inhibitor to be used in breast cancer therapy but, since it interacts with the synthetic glucocorticoids, hydrocortisone must also be given as a replacement. The most important side-effects of aminoglutethimide are at the level of the central nervous system. Other aromatase inhibitors with greater potency and selectivity are being developed. Pyridoglutethimide, a compound resulting from modifications to the structure of aminoglutethimide, seems to be devoid of sedative properties according to preliminary tests on the central nervous system. 4-Hydroxyandrostenedione is significantly more potent and better tolerated than aminoglutethimide. Fadrozole (CGS 16,949 A) is 200-400 times more potent than aminoglutethimide and is now in phase II of its clinical development. CGS 20,267 has no effect on adrenal steroidogenesis and is currently in phase I of its clinical development. Availability of newer aromatase inhibitors could make a worthwhile contribution to endocrine therapy in breast cancer.
authors.affiliation: Medical Department, Ciba-Geigy SA, Barcelona, Spain.
authors.forename: N
authors.initials: N
authors.lastname: Pérez
authors.forename: J
authors.initials: J
authors.lastname: Borja
mesh_terms: D000616:Aminoglutethimide / Q000627:therapeutic use*; D000735:Androstenedione / Q000031:analogs & derivatives* / Q000627:therapeutic use; D000970:Antineoplastic Agents / Q000627:therapeutic use*; D047072:Aromatase Inhibitors; D001943:Breast Neoplasms / Q000188:drug therapy*; D017316:Fadrozole; D005260:Female; D006801:Humans; D007093:Imidazoles / Q000627:therapeutic use; D000077289:Letrozole; D009570:Nitriles / Q000627:therapeutic use; D014230:Triazoles / Q000627:therapeutic use
chemical_list: D000970:Antineoplastic Agents; D047072:Aromatase Inhibitors; D007093:Imidazoles; D009570:Nitriles; D014230:Triazoles; D000616:Aminoglutethimide; D000735:Androstenedione; D000077289:Letrozole; D017316:Fadrozole; C014594:formestane