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Our intention was to (a) to investigate the safety and tolerability of a potent P-glycoprotein modulator, zosuquidar trihydrochloride (LY335979), when administered i.v. alone or in combination with doxorubicin, (b) to determine the pharmacokinetics of zosuquidar and correlate exposure to inhibition of P-glycoprotein function in a surrogate assay, and (c) to compare the pharmacokinetics of doxorubicin in the presence and absence of zosuquidar.

clinical cancer research

A Phase I Trial of a Potent P-Glycoprotein Inhibitor, Zosuquidar Trihydrochloride (LY335979), Administered Intravenously in Combination with Doxorubicin in Patients with Advanced Malignancy