5450. Letrozole

Nomenclature

CAS number: 112809-51-5
4,4′-(1H-1,2,4-Triazol-1-ylmethylene)bisbenzonitrile; 1-[bis(4-cyanophenyl)methyl]-1,2,4-triazole; 4-[1-(4-cyanophenyl)-1-(1,2,4-triazol-1-yl)methyl]benzonitrile; CGS-20267; Femara (Novartis).
C17H11N5; mol wt 285.30.
C 71.57%, H 3.89%, N 24.55%.

Description and references

Nonsteroidal aromatase inhibitor; structurally related to fadrozole, q.v. Prepn: R. M. Bowman et al., EP 236940; eidem, US 4978672 (1987, 1990 both to Ciba-Geigy). Pharmacology: A. S. Bhatnagar et al., J. Steroid Biochem. Mol. Biol. 37, 1021 (1990). Clinical suppression of estrogen biosynthesis: L. M. Demers et al., ibid. 44, 687 (1993). EIA and HPLC determn in biological fluids: C. U. Pfister et al., J. Pharm. Sci. 83, 520 (1994). Clinical evaluation in breast cancer: A. Lipton et al., Cancer 75, 2132 (1995). Review of clinical efficacy: P. E. Goss, R. E. Smith, Expert Rev. Anticancer Ther. 2, 249-260 (2002).

Chemical structure

Properties

mp 181-183°.

Therapeutic Category

Antineoplastic.

Keywords

Antineoplastic (Hormonal); Aromatase Inhibitors; Aromatase Inhibitors