✦ LIBER ✦

Absolute bioavailability of letrozole in healthy postmenopausal women

✍ Scribed by A. Sioufi; N. Gauducheau; V. Pineau; F. Marfil; A. Jaouen; J. M. Cardot; J. Godbillon; C. Czendlik; H. Howald; CH. Pfister; F. Vreeland

Publisher: John Wiley and Sons
Year: 1997
Tongue: English
Weight: 143 KB
Volume: 18
Category: Article
ISSN: 0142-2782
DOI: 10.1002/(sici)1099-081x(199712)18:9<779::aid-bdd64>3.0.co;2-5

No coin nor oath required. For personal study only.

✦ Synopsis

Letrozole is a new non-steroidal inhibitor of the aromatase enzyme system. It is currently under development for the treatment of postmenopausal women with advanced breast cancer. Absolute bioavailability of letrozole when given orally as one 2´5 mg ®lm-coated tablet in comparison to the same dose given intravenously as a bolus injection was studied in 12 healthy postmenopausal women. Letrozole absolute systemic bioavailability after p.o. administration was 99´9+16´3%. Elimination of letrozole was slow. Total-body clearance of letrozole from plasma after i.v. administration was low (2.21 L h 71 ). The calculated distribution volume at steady state (1.87 L kg 71 ) suggests a rather high tissue distribution. Biotransformation of letrozole is the main elimination mechanism with the glucuronide conjugate of the secondary alcohol metabolite being the predominant species found in urine. The two study treatments were tolerated equally well. &1997 John Wiley & Sons, Ltd.

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