Transport of six tyrosine kinase inhibitors: active or passiveReportar como inadecuado

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ADMET and DMPK, Vol.4 No.1 March 2016. -

Transport of erlotinib, gefitinib, sorafenib, sunitinib, dasatinib and crizotinib can be active or passive, which was studied by measuring uptake at low 4 °C; passive and normal temperature 37 °C; active and passive and by the use of specific organic cation transporter OCT inhibitors. Intracellular accumulation was determined using Caco-2 as monolayers, while for gut permeation we used differentiated Caco-2 as model for intestinal epithelium in the Transwell system. Sorafenib and crizotinib uptake are likely to be dependent on passive transport. Gefitinib, dasatinib and sunitinib uptake seem to be active. Erlotinib’s transport also seems to be active. This study suggests that hOCTs might be involved in the apical to basolateral transport of gefitinib and crizotinib. Overall it can be concluded that the accumulation and transport of these six TKIs are very different, despite the fact that they are all tyrosine kinase inhibitors.

Tyrosine kinase; drug transport; erlorinib; gefitinib; sorafenib; sunitinib; dasatinib; crizotinib

Autor: Richard J. Honeywell - ; Department of Medical oncology, VU university medical center, Amsterdam, The Netherlands Sarina Hitzerd



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