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Deprecated: Implicit conversion from float 265.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Br+J+Clin+Pharmacol 2014 ; 78 (3): 524-32 Nephropedia Template TP
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Concomitant oral and intravenous pharmacokinetics of trametinib, a MEK inhibitor, in subjects with solid tumours #MMPMID24606567
Leonowens C; Pendry C; Bauman J; Young GC; Ho M; Henriquez F; Fang L; Morrison RA; Orford K; Ouellet D
Br J Clin Pharmacol 2014[Sep]; 78 (3): 524-32 PMID24606567show ga
Aims: The aim of this phase 1, single centre, open label study in four patients with solid tumours was to determine the absolute bioavailability of a 2 mg oral dose of trametinib. Trametinib is an orally bioavailable, reversible and selective allosteric inhibitor of MEK1 and MEK2 activation and kinase activity. Methods: A microtracer study approach, in which a 5 ?g radiolabelled i.v. microdose of trametinib was given concomitantly with an unlabelled 2 mg oral tablet formulation, was used to recover i.v. and oral pharmacokinetic parameters, simultaneously. Results: The least-squares mean (90% confidence interval) absolute bioavailability of trametinib (2 mg tablet) was 72.3% (50.0%, 104.6%). Median tmax after oral administration was 1.5 h and the geometric mean terminal half-life was 11 days. The geometric mean clearance and volume of distribution after i.v. administration were 3.21 l h?1 and 976 l, respectively, resulting in a terminal elimination half-life of 11 days. Conclusions: Trametinib absolute bioavailability was moderate to high, whereas first pass metabolism was low.