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CBT-1 + doxorubicin is a combination therapy designed for metastatic, unresectable sarcoma previously treated with doxorubicin. CBT-1 is an orally administered, bisbenzylisoquinoline small molecule that acts as a potent P-glycoprotein (P-gp/ABCB1) antagonist, inhibiting drug efflux and reversing resistance to chemotherapy. Doxorubicin, an anthracycline antibiotic, is a cytotoxic agent that intercalates DNA and inhibits topoisomerase II, leading to DNA damage and apoptosis. The combination is being developed to overcome P-gp-mediated multidrug resistance in sarcoma, aiming to improve doxorubicin efficacy. The main mechanism is the inhibition of P-gp drug efflux by CBT-1 to enhance doxorubicin's anti-tumor activity[1][3][5][7].
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