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| Clinical data | |
|---|---|
| Trade names | Lentaron, others |
| Other names | 4-Hydroxyandrost-4-ene-3,17-dione |
| AHFS/Drugs.com | International Drug Names |
| Routes of administration | Intramuscular injection |
| Drug class | Aromatase inhibitor;Antiestrogen |
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| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.153.838 |
| Chemical and physical data | |
| Formula | C19H26O3 |
| Molar mass | 302.414 g·mol−1 |
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Formestane, formerly sold under the brand nameLentaron among others, is asteroidal,selectivearomatase inhibitor which is used in the treatment ofestrogen receptor-positivebreast cancer inpostmenopausal women.[1] The drug is not active orally, and was available only as an intramuscular depot injection. Formestane was not approved by the United States FDA and the injectable form that was used in Europe in the past has been withdrawn from the market.[2] Formestane is ananalogue ofandrostenedione.
Formestane is often used to suppress the production of estrogens fromanabolic steroids orprohormones. It also acts as a prohormone to4-hydroxytestosterone, an active steroid which displays weakandrogenic activity in addition to acting as a weak aromatase inhibitor.
| Generation | Medication | Dosage | % inhibitiona | Classb | IC50c |
|---|---|---|---|---|---|
| First | Testolactone | 250 mg 4x/dayp.o. | ? | Type I | ? |
| 100 mg 3x/weeki.m. | ? | ||||
| Rogletimide | 200 mg 2x/dayp.o. 400 mg 2x/dayp.o. 800 mg 2x/dayp.o. | 50.6% 63.5% 73.8% | Type II | ? | |
| Aminoglutethimide | 250 mg mg 4x/dayp.o. | 90.6% | Type II | 4,500 nM | |
| Second | Formestane | 125 mg 1x/dayp.o. 125 mg 2x/dayp.o. 250 mg 1x/dayp.o. | 72.3% 70.0% 57.3% | Type I | 30 nM |
| 250 mg 1x/2 weeksi.m. 500 mg 1x/2 weeksi.m. 500 mg 1x/1 weeki.m. | 84.8% 91.9% 92.5% | ||||
| Fadrozole | 1 mg 1x/dayp.o. 2 mg 2x/dayp.o. | 82.4% 92.6% | Type II | ? | |
| Third | Exemestane | 25 mg 1x/dayp.o. | 97.9% | Type I | 15 nM |
| Anastrozole | 1 mg 1x/dayp.o. 10 mg 1x/dayp.o. | 96.7–97.3% 98.1% | Type II | 10 nM | |
| Letrozole | 0.5 mg 1x/dayp.o. 2.5 mg 1x/dayp.o. | 98.4% 98.9%–>99.1% | Type II | 2.5 nM | |
| Footnotes:a = Inpostmenopausal women.b = Type I:Steroidal,irreversible (substrate-binding site). Type II:Nonsteroidal,reversible (binding to and interference with thecytochrome P450hememoiety).c = Inbreast cancerhomogenates.Sources: See template. | |||||
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