Fadrozole HCl (CGS-16949A)

Description: Fadrozole (CGS 16949A) is a highly potent and selective nonsteroidal aromatase inhibitor (IC50 of 6.4 nM) with potential antineoplastic activity. Aromatase, a member of the cytochrome P-450 superfamily, is found in many tissues; overexpression has been linked to the development of preneoplastic and neoplastic changes in breast tissue. Check for active clinical trials or closed clinical trials using this agent. Fadrozole specifically inhibits aromatase, blocking the aromatization of androstenedione and testosterone into estrone and estradiol, respectively, the final step in estrogen biosynthesis; the reduction in estrogen levels may inhibit growth in estrogen-dependent cancers.

References:

1. Browne LJ, et al. Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease. J Med Chem. 1991 Feb; 34(2):725-36.

2. Gunson DE, et al. Prevention of spontaneous tumours in female rats by fadrozole hydrochloride, an aromatase inhibitor. Br J Cancer. 1995 Jul; 72(1):72-5.

3. Morales-Montor J, et al. Inhibition of p-450 aromatase prevents feminisation and induces protection during cysticercosis. Int J Parasitol. 2002 Oct; 32(11):1379-87.

4. Brixius-Anderko S, Scott EE. Structure of human cortisol-producing cytochrome P450 11B1 bound to the breast cancer drug fadrozole provides insights for drug design. J Biol Chem. 2018 Nov 13. pii: jbc.RA118.006214. doi: 10.1074/jbc.RA118.006214.

Related CAS #: 102676-31-3 (HCl) 176702-70-8 (HCl hydrate) 102676-47-1 (free base)