By Toshihisa Ishikawa, John Schuetz
ABC Transporters and Cancer offers worthwhile details at the intriguing and fast-moving box of melanoma study. the following, amazing and unique experiences are provided on numerous themes. This quantity covers ABC transporters and melanoma, and is appropriate for researchers and scholars alike.
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This, of course, would lead to the idea that there is no point in targeting the protective mechanisms of the BBB for chemotherapy of brain tumors. , 2010). Usually, this barrier close to and inside a large tumor is disrupted; however, there are nearly always substantial areas around and in the tumor where this barrier is intact. , 2010). Chemotherapy is only effective if virtually all tumor cells can be hit. Even a partially intact BBB, protecting just a few percent of the tumor cells, will severely compromise this aim.
We observed that, even at the highly increased plasma concentrations of taxanes after boosting with both elacridar and ritonavir, relative brain accumulation was still similar as seen after oral single administration of paclitaxel or docetaxel. It thus appears that oral taxane bioavailability can be boosted with ritonavir and elacridar, without compromising the protective action of ABCB1 in the blood–brain barrier (BBB) in keeping the potentially neurotoxic taxanes out of the brain. ). Retrospective analysis of our data suggests that only at very high taxane plasma levels, which are obtained shortly after intravenous but not oral administration, ABCB1 plays a substantial role in limiting taxane brain accumulation.
2012b)SorafenibVEGFR, PDGFR, and Raf––Lagas, Fan, et al. (2010) and Lagas, van Waterschoot, et al. (2010)SunitinibFGFR, PDGFR, and VEGFR––Tang, Lagas, et al. (2012) and Tang, Lankheet, et al. (2012)TandutinibFLT3, PDGFR beta, and c-Kit++Yang et al. Vaidhyanathan et al. Minocha et al. (2012a)VemurafenibBRAF+++Durmus et al. , not determined. , 2011). Lagas, van Waterschoot, et al. (2009) found that Abcb1a/1b, but not Abcg2, limits oral uptake of dasatinib. 0-fold in the absence of both transporters.