 | |
| Clinical data | |
|---|---|
| Trade names | Afema |
| Routes of administration | By mouth |
| Drug class | Aromatase inhibitor; Antiestrogen |
| ATC code |
|
| Legal status | |
| Legal status |
|
| Identifiers | |
| |
| CAS Number |
 Y |
| PubChem CID | |
| ChemSpider |
|
| UNII |
Y |
| KEGG |
|
| ChEMBL | |
| CompTox Dashboard (EPA) | |
| Chemical and physical data | |
| Formula | C14H13N3 |
| Molar mass | 223.279 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
 NY (what is this?) (verify) | |
Fadrozole (INNTooltip International Nonproprietary Name), sold under the brand name Afema (byNovartis), is a selective, nonsteroidal aromatase inhibitor which is or has been used in Japan for the treatment of breast cancer.[1][2]
| Generation | Medication | Dosage | % inhibitiona | Classb | IC50c |
|---|---|---|---|---|---|
| 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. | |||||
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