Concomitant oral and intravenous pharmacokinetics of trametinib, a MEK inhibitor, in subjects with solid tumours.

@article{Leonowens2014ConcomitantOA,
  title={Concomitant oral and intravenous pharmacokinetics of trametinib, a MEK inhibitor, in subjects with solid tumours.},
  author={Cathrine Leonowens and Carolyn Pendry and John G. Bauman and Graeme Young and May M Ho and Frank Henriquez and Lei Fang and Royce A. Morrison and Keith Orford and Daniele Ouellet},
  journal={British journal of clinical pharmacology},
  year={2014},
  volume={78 3},
  pages={
          524-32
        }
}
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 μg radiolabelled i.v. microdose of trametinib was given concomitantly with an unlabelled 2 mg oral tablet formulation, was used to… CONTINUE READING
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