01/03/2009 - Role of transporters in drug ADME

Kinetic characterization of sulfasalazine transport by human ABCG2 (BCRP)

M. Jani, P. Szabó, E. Kis, É. Molnár, H. Glavinas, P. Krajcsi

Biol Pharm Bull. 2009 Mar;32(3):497-9.


The pharmacokinetics of sulfasalazine, an anti-inflammatory drug is influenced by ATP-binding cassette G2 (ABCG2) (breast cancer resistance protein (BCRP), mitoxantrone resistance protein (MXR)) both in vitro and clinically. Due to its low passive permeability, the intracellular concentration of sulfasalazine is dependent on uptake transporters, rendering the characterization of transporter specific interactions in cell based experimental systems difficult. Applying membrane assays a detailed kinetic analysis of sulfasalazine ABCG2 interaction was conducted and Km values of 0.70 +/- 0.03 microM and 0.66 +/- 0.08 microM were obtained at pH 7.0 and pH 5.5, respectively.

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