Lopinavir Derivative as Potent P-gp Inhibitor Enables Delivery through HPMA Copolymer Conjugates and Overcoming Tumor Chemoresistance to Conventional Cytostatic Drugs.

LD was highly potent in sensitizing P388/MDR cells to the cytostatic activity of DOX, resulting in approximately 86-fold lower IC 50 value of the drug compared to that in cells incubated with DOX alone ( Figure A upper panel). Moreover, a highly significant sensitization of P388/MDR cells to the cytostatic activity of P-DOX was obtained in the presence of P-LD, although the effects were not as potent as those achieved with the free cytostatic drug and LD ( Figure B upper panel).

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