3913. Exemestane

Nomenclature

CAS number: 107868-30-4
6-Methyleneandrosta-1,4-diene-3,17-dione; FCE-24304; Aromasin (Pharmacia & Upjohn).
C20H24O2; mol wt 296.40.
C 81.04%, H 8.16%, O 10.80%.

Description and 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).

Chemical structure

Properties

White to slightly yellow crystalline powder. mp 188-191°. uv max: 247 nm (ε 13750). Freely sol in DMF; sol in methanol. Practically insol in water.

Therapeutic Category

Antineoplastic (hormonal).

Keywords

Antineoplastic (Hormonal); Aromatase Inhibitors; Aromatase Inhibitors