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Dexverapamil is the R-enantiomer of verapamil, a phenylalkylamine calcium channel blocker. Unlike racemic verapamil or its S-enantiomer counterpart, dexverapamil exhibits significantly reduced calcium antagonistic activity and toxicity. Its primary mechanism of action is as a competitive inhibitor of the multidrug resistance efflux pump P-glycoprotein (MDR-1/ABCB1), which can increase the effectiveness of various antineoplastic drugs by preventing their expulsion from cancer cells. This property has led to its investigation as a chemosensitizer and modulator of multidrug resistance in oncology settings[1][4][5]. Developed primarily for experimental use in combination with cancer chemotherapy regimens to overcome drug resistance mechanisms[5].
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