Drug intelligence / Profile preview

fadrozole

Development stage
Discontinued
Lead developer
Novartis
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Oral
01

Overview

Fadrozole is a nonsteroidal aromatase inhibitor developed as an oral small molecule for the treatment of estrogen-dependent diseases, most notably breast cancer. It acts by selectively inhibiting the enzyme aromatase (CYP19A1), thereby blocking the conversion of androgens (androstenedione and testosterone) to estrogens (estrone and estradiol). This reduction in estrogen levels can inhibit the growth of estrogen-dependent tumors. Fadrozole was primarily used in Japan under the brand name Afema for breast cancer, particularly in postmenopausal women with advanced or metastatic disease. Clinical studies have shown that it has similar efficacy to tamoxifen but may be better tolerated, with fewer severe toxic effects[6][7][9]. Its use outside Japan has been limited due to comparable or superior alternatives.

Brand names
Afema
Other names
fadrozole hydrochloridefadrozole monohydrochloride
02

Targets

CYP19A1 (Aromatase)

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