Fadrozole (INN ), sold under the brand name Afema (by Novartis), is a selective, nonsteroidal aromatase inhibitor which is or has been used in Japan for the treatment of breast cancer.[1][2]
Clinical data | |
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Trade names | Afema |
Routes of administration | By mouth |
Drug class | Aromatase inhibitor; Antiestrogen |
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Chemical and physical data | |
Formula | C14H13N3 |
Molar mass | 223.279 g·mol−1 |
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Generation | Medication | Dosage | % inhibitiona | Classb | IC50c |
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First | Testolactone | 250 mg 4x/day p.o. | ? | Type I | ? |
100 mg 3x/week i.m. | ? | ||||
Rogletimide | 200 mg 2x/day p.o. 400 mg 2x/day p.o. 800 mg 2x/day p.o. |
50.6% 63.5% 73.8% |
Type II | ? | |
Aminoglutethimide | 250 mg mg 4x/day p.o. | 90.6% | Type II | 4,500 nM | |
Second | Formestane | 125 mg 1x/day p.o. 125 mg 2x/day p.o. 250 mg 1x/day p.o. |
72.3% 70.0% 57.3% |
Type I | 30 nM |
250 mg 1x/2 weeks i.m. 500 mg 1x/2 weeks i.m. 500 mg 1x/1 week i.m. |
84.8% 91.9% 92.5% | ||||
Fadrozole | 1 mg 1x/day p.o. 2 mg 2x/day p.o. |
82.4% 92.6% |
Type II | ? | |
Third | Exemestane | 25 mg 1x/day p.o. | 97.9% | Type I | 15 nM |
Anastrozole | 1 mg 1x/day p.o. 10 mg 1x/day p.o. |
96.7–97.3% 98.1% |
Type II | 10 nM | |
Letrozole | 0.5 mg 1x/day p.o. 2.5 mg 1x/day p.o. |
98.4% 98.9%–>99.1% |
Type II | 2.5 nM | |
Footnotes: a = In postmenopausal women. b = Type I: Steroidal, irreversible (substrate-binding site). Type II: Nonsteroidal, reversible (binding to and interference with the cytochrome P450 heme moiety). c = In breast cancer homogenates. Sources: See template. |
References
edit- ^ Browne LJ, Gude C, Rodriguez H, Steele RE, Bhatnager A (February 1991). "Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease". J. Med. Chem. 34 (2): 725–36. doi:10.1021/jm00106a038. PMID 1825337.
- ^ Raats JI, Falkson G, Falkson HC (January 1992). "A study of fadrozole, a new aromatase inhibitor, in postmenopausal women with advanced metastatic breast cancer". J. Clin. Oncol. 10 (1): 111–6. doi:10.1200/jco.1992.10.1.111. PMID 1530798.[permanent dead link ]