Women's Health Weekly
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Breast Cancer
Study findings from J.S. Lagas et al broaden understanding of breast cancer
May 28th, 2009
According to a study from Netherlands, "Imatinib, a BCR-ABL tyrosine kinase inhibitor, is a substrate of the efflux transporters P-glycoprotein (P-gp, ABCB1) and ABCG2 (breast cancer resistance protein), and its brain accumulation is restricted by both transporters. For dasatinib, an inhibitor of SCR/BCR-ABL kinases, in vivo interactions with P-gp and ABCG2 are not fully established yet." "We used Abcb1a/1b(-/-), Abcg2(-/-), and Abcb1a/1b;Abcg2(-/-) mice to establish the roles of P-gp and ABCG2 in the pharmacokinetics and brain accumulation of dasatinib. We found that oral uptake of dasatinib is limited by P-gp. Furthermore, relative brain accumulation, 6 hours after...
Source: Women's Health Weekly (2009-05-28)
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