Zosuquidar is a
compound of
antineoplastic drug candidates currently under development. It is now in "Phase 3" of clinical tests in the United States. Its action mechanism consists of the inhibition of P-
glycoproteins; other drugs with this mechanism include tariquidar and laniquidar. P-glycoproteins are
proteins which convert the
energy derived from the
hydrolysis of
ATP to structural changes in protein molecules, in order to perform
coupling, thus discharging
medicine from cells. If P-glycoprotein coded with the MDR1
gene manifests itself in
cancer cells, it discharges much of the antineoplastic drugs from the cells, making
cancer cells medicine tolerant, and rendering antineoplastic drugs ineffective. This protein also manifests itself in normal organs not affected by the cancer (such as the liver, small intestine, and skin cells in blood vessels of the brain), and participates in the transportation of medicine. The compound Zosuquidar
inhibits this P-glycoprotein, causing the cancer cells to lose their medicine tolerance, and making antineoplastic drugs effective.
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A substance that is being studied for its ability to reverse resistance to chemotherapy. Also called LY335979.
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