Quantitative structure–property relationships of camptothecins in humans

The purpose of this study was to develop quantitative structure property relationships (QSPR) for the pharmacokinetics and the susceptibility to BCRP-mediated efflux of ten drugs in the camptothecin family of topoisomerase I inhibitors.

Pharmacokinetic parameters (total and lactone clearance, total steady-state volume of distribution, and lactone:total area under the curve ratio) and IC50 values of cytotoxicity in both BCRP over-expressing and sensitive cell lines were extracted from the literature.

 

Chao Xu, Thomas M. Barchet, Donald E. Mager
January 1, 2010
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