Synonyms: Afema® | CGS 16949 A [1] | CGS-16949A | FAD 286 | FAD-286
fadrozole is an approved drug (Japan only)
Compound class:
Synthetic organic
Comment: Fadrozole was designed and reported as a selective aromatase (CYP19A1) inhibitor having only weak effects on aldosterone and cortisol production [1]. More recent evidence suggests that fadrozole is in fact a potent inhibitor of the cytochrome P450 enzymes, CYP11B1 (11-beta-hydroxylase) and CYP11B2 (aldosterone synthase) responsible for cortisol and aldosterone synthesis respectively [2].
![]() Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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References |
1. Browne LJ, Gude C, Rodriguez H, Steele RE, Bhatnager A. (1991)
Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease. J Med Chem, 34 (2): 725-36. [PMID:1825337] |
2. LaSala D, Shibanaka Y, Jeng AY. (2009)
Coexpression of CYP11B2 or CYP11B1 with adrenodoxin and adrenodoxin reductase for assessing the potency and selectivity of aldosterone synthase inhibitors. Anal Biochem, 394 (1): 56-61. [PMID:19622340] |
3. Raats JI, Falkson G, Falkson HC. (1992)
A study of fadrozole, a new aromatase inhibitor, in postmenopausal women with advanced metastatic breast cancer. J Clin Oncol, 10 (1): 111-6. [PMID:1530798] |