Chemical compound
Formestane 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 ATC code
(8R ,9S ,10R ,13S ,14S )-4-hydroxy-10,13-dimethyl-2,6,7,8,9,11,12,14,15,16-decahydro-1H -cyclopenta[a ]phenanthrene-3,17-dione
CAS Number 566-48-3 Y PubChem CID ChemSpider 10799 Y UNII KEGG D07260 Y ChEBI CHEBI:75172 N ChEMBL ChEMBL132530 Y CompTox Dashboard (EPA ) DTXSID3034113 ECHA InfoCard 100.153.838 Formula C 19 H 26 O 3 Molar mass 302.414 g·mol−1 3D model (JSmol)
O=C4C(/O)=C3/CC[C@@H]2[C@H](CC[C@@]1(C(=O)CC[C@H]12)C)[C@@]3(C)CC4
InChI=1S/C19H26O3/c1-18-10-8-15(20)17(22)14(18)4-3-11-12-5-6-16(21)19(12,2)9-7-13(11)18/h11-13,22H,3-10H2,1-2H3/t11-,12-,13-,18+,19-/m0/s1
Y Key:OSVMTWJCGUFAOD-KZQROQTASA-N
Y
N Y (what is this?) (verify)
Formestane , formerly sold under the brand name Lentaron among others, is a steroidal, selective aromatase inhibitor which is used in the treatment of estrogen receptor-positive breast cancer in postmenopausal 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was not approved by the United States FDA and the injectable form that was used in Europe in the past has been withdrawn from the market.[2] Formestane is an analogue of androstenedione.
Formestane is often used to suppress the production of estrogens from anabolic steroids or prohormones. It also acts as a prohormone to 4-hydroxytestosterone, an active steroid which displays weak androgenic activity in addition to acting as a weak aromatase inhibitor.
Pharmacodynamics of aromatase inhibitors
Generation
Medication
Dosage
% inhibitiona
Classb
IC50 c
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.
^ Pérez Carrión R, Alberola Candel V, Calabresi F, et al. (1994). "Comparison of the selective aromatase inhibitor formestane with tamoxifen as first-line hormonal therapy in postmenopausal women with advanced breast cancer". Ann. Oncol . 5 (Suppl 7): S19–24. PMID 7873457.
^ "Formestane".
Last Update: 2023-12-08T20:15:10Z
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