A phase I study of the P-glycoprotein antagonist tariquidar in combination with vinorelbine.

ABSTRACT:

Purpose

P-glycoprotein (Pgp) antagonists have had unpredictable pharmacokinetic interactions requiring reductions of chemotherapy. We report a phase I study using tariquidar (XR9576), a potent Pgp antagonist, in combination with vinorelbine.

Experimental design

Patients first received tariquidar alone to assess effects on the accumulation of (99m)Tc-sestamibi in tumor and normal organs and rhodamine efflux from CD56+ mononuclear cells. In the first cycle, vinorelbine pharmacokinetics was monitored after the day 1 and 8 doses without or with tariquidar. In subsequent cycles, vinorelbine was administered with tariquidar. Tariquidar pharmacokinetics was studied alone and with vinorelbine.

Results

Twenty-six patients were enrolled. Vinorelbine 20 mg/m(2) on day 1 and 8 wa

SUBMITTER: Abraham J 

PROVIDER: S-EPMC7213754 | biostudies-literature | 2009 May

REPOSITORIES: biostudies-literature