Raloxifene pharmacokinetics in males with normal and impaired renal function.

Czock, David; Keller, Frieder; Heringa, Mette; Rasche, Franz Maximilian

To compare raloxifene pharmacokinetics between renally impaired and healthy subjects.Raloxifene 120 mg was administered to 10 males with renal impairment (creatinine 2–4 mg dl−1) and to 10 healthy males. Data were analysed by two noncompartmental and one compartmental nonlinear regression methods.The medians (95% confidence interval) of the area under the curves (AUC) were 35.1 (25.8, 74) and 20.5 (16.8, 28.0) h ng ml−1 per mg kg−1,P < 0.01, and of the clearances (CL/F) were 28.5 (13.5, 38.8) and 48.8 (35.8, 59.4) l h−1 kg−1,P < 0.01, in renally impaired and healthy subjects, respectively. 95% Confidence intervals on the differences for AUC and CL/F were 6.5–44.1 and−35.1 to−7.9, respectively.Exposure to raloxifene was twice as high in males with renal impairment compared with healthy subjects.

RALOXIFENE; PHARMACOGENOMICS; PATIENTS; SELECTIVE estrogen receptor modulators; BIOCHEMICAL genetics; DRUG metabolism

British Journal of Clinical Pharmacology, 2005, Vol 59, Issue 4, p479

0306-5251

Academic Journal

10.1111/j.1365-2125.2004.02326.x