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The present invention relates to an antibody fragment capable of binding to P-glycoprotein associated with multidrug resistant (MDR) cells. The present invention also relates to compositions and methods utilizing such an antibody fragment for inhibiting drug efflux activity in MDR cancer cells. Cancer chemotherapy often fails due to the development of acquired or intrinsic resistance in cancerous cells. A key mechanism of MDR is the overexpression of an energy-dependant efflux pump, known as the multidrug transporter. The present invention demonstrates an antibody that selectively reacts with Pgp-overexpressing cells and is, therefore, an effective inhibitor of drug-efflux activity in multi-drug resistant cells.