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Topotecan oral bioavailability increased dramatically by inhibiting BCRP
Topotecan, an anti-cancer drug, is being administered IV, since its
oral absolute bioavailability (F) is 42 +/- 13 %. This relatively
low value for F is primary due to the effect of the gut efflux
transporter breast cancer resistance protein (BCRP). By blocking the
effect of BCRP with elacridar, the oral absolute bioavailability of
topotecan increases to 100%. The reference cited below deals with
A phase I, randomized, open-label, parallel-cohort, dose-finding
study of elacridar (GF120918) and oral topotecan in cancer patients.
Clin Cancer Res, 2007 Jun 1;13(11):3276-85.
Kuppens IE, Witteveen EO, Jewell RC, Radema SA, Paul EM, Mangum SG,
Beijnen JH, Voest EE, Schellens JH.
Harold Boxenbaum, Ph.D.
14621 Settlers Landing Way
North Potomac, MD 20878-4305
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