Pharmacokinetics of finrozole (MPV-2213ad), a novel selective aromatase inhibitor, in healthy men

Aims To investigate the pharmacokinetics of finrozole (MPV-2213ad) a novel competitive aromatase enzyme inhibitor. in healthy male volunteers. Methods The Study was all open, partly randomized cross-over study includin g 23 volunteers receiving single doses of 3, 9 mg or 30 mg of finrozole as tablets or solution with 14 days between the administrations. The highest d ose was given as tablets only. Serum concentrations of finrozole were deter mined using high performance liquid chromatography combined with mass spect rometry. Results The mean time to peak serum concentration ranged from 2.5 to 3.1, a nd 0.6-0.7 h after tablets and solution. respectively. The C-max values inc reased as the dose increased. The Calculated apparent mean elimination half -life (t(1/2.z)) was Approximately 3 h after the solution, and approximatel y 8 h after the tablet. The AUC(0, infinity) after finrozole tablets increa sed proportionally from 3 mg to 9 mg and from 3 to 30 mg. The calculated re lative mean bioavailabilities (AUC(0, infinity) - ratio) for the 3 mg and 9 mg doses of finrozole as tablets were 89% and 78%, respectively. Conclusions The absorption of finrozole from the tablet formulation was rel atively rapid, and the apparent elimination half-life was longer after the tablet than after the solution, probably reflecting overlap of the absorpti on with the elimination phase.