References of (8R,9S,10R,13S,14S)-10,13-dimethyl-6-methylidene-7,8,9,11,12,14,15,
16-octahydrocyclopenta[a]phenanthrene-3,17-dione
Title: Exemestane
CAS Registry Number: 107868-30-4
CAS Name: 6-Methyleneandrosta-1,4-diene-3,17-dione
Manufacturers' Codes: FCE-24304
Trademarks: Aromasin (Pharmacia & Upjohn)
Molecular Formula: C20H24O2
Molecular Weight: 296.40
Percent Composition: C 81.04%, H 8.16%, O 10.80%
Literature References: Irreversible aromatase inhibitor. Prepn: E. Di Salle
et al., DE 3622841; F. Buzzetti
et al., US 4808616 (1987, 1989 both to Farmitalia Carlo Erba). Pharmacology: D. Giudici
et al., J. Steroid Biochem. 30, 391 (1988). HPLC determn in plasma: M. Breda
et al., J. Chromatogr. 620, 225 (1993). Clinical pharmacology: T. R. J. Evans
et al., Cancer Res. 52, 5933 (1992). Review of clinical experience in primary and secondary therapy for breast cancer: J. M. Dixon,
Expert Rev. Anticancer Ther. 2, 267-275 (2002). Clinical trial in sequential therapy following tamoxifen in breast cancer: R. C. Coombes
et al., N. Engl. J. Med. 350, 1081 (2004).
Properties: White to slightly yellow crystalline powder. mp 188-191°. uv max: 247 nm (e 13750). Freely sol in DMF; sol in methanol. Practically insol in water.
Melting point: White to slightly yellow crystalline powder. mp 188-191°
Absorption maximum: uv max: 247 nm (e 13750)
Therap-Cat: Antineoplastic (hormonal).
Keywords: Antineoplastic (Hormonal); Aromatase Inhibitors; Aromatase Inhibitors.