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Table 1 The characteristics of 4 generations of ABC transporter modulators

From: Tyrosine kinase inhibitors enhanced the efficacy of conventional chemotherapeutic agent in multidrug resistant cancer cells

Generation Representative In vitro In vivo PK Down-regulate ABC transporter
1st verapamil, cyclosporin A, tamoxifen + +
2nd PSC833, S97882, VX-710 + + +
3rd GF120918, XR9576, R101933, LY335979 + +
4th neochamaejasmin B, curcumin + + +
  1. “+” stands for positive effective; “-” stands for ineffective; “PK” stands for pharmacokinetics