Dose proportionality and population characteristics of oral fadrozole hydrochloride, an aromatase inhibitor, in postmenopausal women. 1993

G M Kochak, and R L Choi, and E A Entwistle
Clinical Pharmacokinetics and Disposition Section, Ciba-Geigy Corporation, Ardsley, New York 10502.

The dose proportionality of the pharmacokinetics of fadrozole was investigated in 18 healthy postmenopausal women. Fadrozole hydrochloride was administered as 0.3-, 1.0-, and 2.0-mg oral doses continuously every 12 hr for 5 days each in a Latin square design. At steady state, the dose-normalized pharmacokinetic parameters AUC and Cmax were found to be independent of the dose. In addition, no statistically significant differences in tmax were detected. It was concluded that the pharmacokinetics of fadrozole were dose proportional in the projected therapeutic dose range. The relationship between oral clearance and the demographic factors, age, weight, and height, was assessed. Oral clearance was related to total body weight but not age or height. Prospective estimates of the population components of variance showed that intersubject variance accounted for 91.7% of the total random variance. Weight variance accounted for 36.1% of the intersubject variance.

UI MeSH Term Description Entries
D008875 Middle Aged An adult aged 45 - 64 years. Middle Age
D011446 Prospective Studies Observation of a population for a sufficient number of persons over a sufficient number of years to generate incidence or mortality rates subsequent to the selection of the study group. Prospective Study,Studies, Prospective,Study, Prospective
D001827 Body Height The distance from the sole to the crown of the head with body standing on a flat surface and fully extended. Body Heights,Height, Body,Heights, Body
D001835 Body Weight The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms. Body Weights,Weight, Body,Weights, Body
D005260 Female Females
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000328 Adult A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available. Adults
D000368 Aged A person 65 years of age or older. For a person older than 79 years, AGED, 80 AND OVER is available. Elderly
D000375 Aging The gradual irreversible changes in structure and function of an organism that occur as a result of the passage of time. Senescence,Aging, Biological,Biological Aging
D017316 Fadrozole A selective aromatase inhibitor effective in the treatment of estrogen-dependent disease including breast cancer. CGS 020286A,CGS-020286A,CGS-16949A,CGS020286A,FAD 286,FAD-286,FAD286,Fadrozole Hydrochloride,Fadrozole Monohydrochloride,CGS 16949A,CGS16949A,Hydrochloride, Fadrozole,Monohydrochloride, Fadrozole

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