4240. Formestane

Nomenclature

CAS number: 566-48-3
4-Hydroxyandrost-4-ene-3,17-dione; 4-OHA; CGP-32349; Lentaron (Novartis).
C19H26O3; mol wt 302.41.
C 75.46%, H 8.67%, O 15.87%.

Description and references

Selective aromatase inhibitor. Prepn: R. D. Burnett, D. N. Kirk, J. Chem. Soc. Perkin Trans. 1 1973, 1830; J. Mann, B. Pietrzak, ibid. 1983, 2681; P. G. Ciattini et al., Synth. Commun. 22, 1949 (1992). Aromatase inhibition and effect on estrogen-dependent processes in vivo: A. M. H. Brodie et al., Endocrinology 100, 1684 (1977). Radioimmunoassay in plasma: J. Khubieh et al., J. Steroid Biochem. 35, 377 (1990). GC determn in plasma and urine: P. H. Degen, W. Schneider, J. Chromatogr. 565, 67 (1991). Pharmacokinetics and endocrine effects in breast cancer patients: M. Dowsett et al., Eur. J. Cancer 28, 415 (1992). Clinical evaluation in breast cancer: R. C. Coombes, J. Steroid Biochem. Mol. Biol. 43, 145 (1992).

Chemical structure

Properties

Needles from aq methanol, mp 199-202° (Burnett, Kirk); also reported as crystals from ethyl acetate, mp 203.5-206° (Brodie). uv max (99.5% ethanol): 278 nm (ε 11030). [α]D20 +181° (c = 7.7 in chloroform).

Therapeutic Category

Antineoplastic (hormonal).

Keywords

Antineoplastic (Hormonal); Aromatase Inhibitors; Aromatase Inhibitors