AI Article Synopsis
- Sulfasalazine's pharmacokinetics are influenced by the ABCG2 transporter, which affects how the drug is absorbed and processed in the body.
- The drug's low passive permeability means that its effectiveness relies on specific uptake transporters, making it challenging to study these interactions in lab settings.
- Detailed kinetic analysis of sulfasalazine's interaction with ABCG2 revealed Km values of 0.70 and 0.66 microM at pH 7.0 and pH 5.5, indicating how efficiently the drug is transported by this protein.
Article Abstract
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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| http://dx.doi.org/10.1248/bpb.32.497 | DOI Listing |
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