NCIt definition : A synthetic quinoline derivative with multidrug resistance (MDR) modulating properties.
Dofequidar fumarate, like many other MDR reversal agents, binds competitively to the
drug-binding site of the transmembrane P-glycoprotein efflux pump (P-gp). Once bound
to the P-gp efflux pump, dofequidar is transported out of transformed cells by a mechanism
similar to that used by cytotoxic drugs, thereby blocking the efflux of these compounds
from the cell. Inhibition of the efflux pump by this agent leads to a retention of
the cytotoxic drug resulting in increased intracellular drug concentrations, thereby
enhancing cytotoxicity. Dofequidar has demonstrated reversal of the MDR phenotype
in those cells exposed to various chemotherapeutic agents, such as vinca alkaloids
and anthracyclines.;
Alternative definition : NCI-GLOSS: A substance that is being studied for its ability to make cancer cells
respond better to chemotherapy drugs to which they have become resistant. It belongs
to the family of drugs called quinolone antibiotics.;