Table 1.
Drugs that reverse chemoresistance via various mechanisms.
| Drugs | MOA | Clinical trial | References |
|---|---|---|---|
| ABC transporter inhibitors | |||
| Cyclosporine | 1st generation ABCB1 competitive inhibitors |
– | (22) |
| Nicardipine | (23) | ||
| Quinine | (24) | ||
| Tamoxifen | (25) | ||
| Verapamil | (26) | ||
| Cinchonine | 2nd generation ABCB1 competitive inhibitors |
– | (27) |
| Dexverapamil | (28) | ||
| Toremifene | (29) | ||
| Valspodar (PSC-833) | (30) | ||
| Biricodar (VX-710) | 2nd generation ABCB1 and ABCC1 competitive inhibitors |
– | (31) |
| Dofequidar (MS-209) | (32) | ||
| Laniquidar (R101933) | 3rd generation ABCB1 competitive inhibitors |
– | (33) |
| Lonafarnib (SCH66336) | (34) | ||
| Zosuquidar (LY335979) | (35) | ||
| Elacridar (GF120918) | 3rd generation ABCB1 and ABCG2 competitive inhibitors |
– | (36) |
| Tariquidar (XR9576) | (37) | ||
| Fumitremorgin C | ABCG2 competitive inhibitor | – | (38) |
| Flupentixol | ABCB1 allosteric modulators | – | (39) |
| Non-substrates of P-gp | |||
| Ixabepilone | Microtubule inhibitor | FDA approval | (40) |
| Cabazitaxel | (41) | ||
| Ortataxel | Phase 2 | (42) | |
| Vinflunine | Phase 3 | (43) | |
| ALDH1 inhibitors | |||
| Disulfiram | Copper-dependent proteasome inhibitor | Phase 2 | (44, 45) |
| Tretinoin | – | – | (46) |
| AMPK activators | |||
| Metformin | – | Phase 2/3 | (47, 48) |
| Thalidezine | Autophagic cell death inducer | – | (49) |
| VEGF inhibitor | |||
| Bevacizumab | Anti-VEGF antibody | FDA approval | (50) |
| RTK inhibitor | |||
| Sorafenib | Multikinase inhibitor | FDA approval | (51) |
| Vascular disrupting agents | |||
| Combretastatin A4 | Tubulin-binding agents | Phase 1/2 | (52) |
| Plocabulin | (53) | ||
| BET inhibitors | |||
| TEN-010 (JQ2) | – | Phase 1 | (54) |
| CC-90010 | BRD2 inhibitor | Phase 1 | (54) |
| ABBV-744 | BRD4 inhibitors | Phase 1 | (55) |
| CPI-0610 | (56) | ||
| I-BET151 | BRD2 and BRD4 inhibitor | Phase 1 | (57) |
| OTX015 | BRD2, BRD3, and BRD4 inhibitor | Phase 1 | (58, 59) |
| ABBV-075 | BRD2, BRD3, BRD4, and BRDT inhibitors | Phase 1 | (60) |
| FT-1101 | (54) | ||
| I-BET762 | Phase 1/2 | (61) | |
| HDAC inhibitors | |||
| Vorinostat | Pan-HDAC inhibitors | FDA approval | (62, 63) |
| Panobinostat | (64) | ||
| KDM1 inhibitors | |||
| Tranylcypromine | Non-selective irreversible inhibitor | Phase 1/2 | (65) |
| GSK-2879552 | Selective irreversible inhibitors | Phase 1 | (66) |
| IMG-7289 (Bomedemstat) | Phase 1/2 | (67) | |
| INCB-059872 | (68) | ||
| ORY-1001 (Iadademstat) | (69) | ||
| CC-90011 | Selective reversible inhibitors | Phase 1 | (70) |
| SP−2577 (Seclidemstat) | Phase 1/2 | (71) | |
| Notch signaling inhibitors | |||
| DAPT | γ-secretase inhibitors | – | (72, 73) |
| RO4929097 | Phase 2 | (74) | |
| Hh signaling inhibitors | |||
| Cyclopamine | Smo inhibitors | – | (75, 76) |
| Sonidegib | FDA approval | (77) | |
| Vismodegib | (77) | ||
| Wnt/β-catenin signaling inhibitors | |||
| Ipafricept | FZD8-Fc | Phase 1 | (78) |
| Rosmantuzumab | Anti-RSPO antibody | (79) | |
| Vantictumab | Anti-FZD1, 2, 5, 7, and 8 antibody | (79, 80) | |
| Foxy-5 | Wnt5a-mimicking peptide | Phase 2 | (81) |
| ETC-159 | Porcupine inhibitors | Phase 1 | (82) |
| LGK974 | Phase 2 | (83) | |
| CWP232291 | β-catenin inhibitors | Phase 1 | (84) |
| PRI-724 | (85) | ||