| DB00276 | Amsacrine | approved, investigational | yes | inhibitor | Details |
| DB00380 | Dexrazoxane | approved, withdrawn | yes | inhibitor | Details |
| DB00385 | Valrubicin | approved | yes | inhibitor | Details |
| DB00444 | Teniposide | approved | yes | inhibitor | Details |
| DB00773 | Etoposide | approved | yes | inhibitor | Details |
| DB00997 | Doxorubicin | approved, investigational | yes | inhibitor | Details |
| DB01177 | Idarubicin | approved | yes | inhibitor | Details |
| DB01204 | Mitoxantrone | approved, investigational | yes | inhibitor | Details |
| DB00445 | Epirubicin | approved | unknown | inhibitor | Details |
| DB01179 | Podofilox | approved | yes | inhibitor | Details |
| DB01645 | Genistein | investigational | unknown | | Details |
| DB00537 | Ciprofloxacin | approved, investigational | unknown | inhibitor | Details |
| DB00467 | Enoxacin | approved, investigational | no | inhibitor | Details |
| DB04576 | Fleroxacin | experimental | yes | inhibitor | Details |
| DB00978 | Lomefloxacin | approved, investigational | unknown | inhibitor | Details |
| DB00218 | Moxifloxacin | approved, investigational | unknown | inhibitor | Details |
| DB01059 | Norfloxacin | approved | unknown | inhibitor | Details |
| DB00487 | Pefloxacin | approved | unknown | inhibitor | Details |
| DB01208 | Sparfloxacin | approved, investigational, withdrawn | yes | inhibitor | Details |
| DB00685 | Trovafloxacin | approved, investigational, withdrawn | unknown | inhibitor | Details |
| DB01165 | Ofloxacin | approved | unknown | inhibitor | Details |
| DB05129 | Elsamitrucin | investigational | unknown | | Details |
| DB04975 | Banoxantrone | investigational | unknown | | Details |
| DB04978 | SP1049C | investigational | unknown | | Details |
| DB04967 | Lucanthone | investigational | yes | inhibitor | Details |
| DB05022 | Amonafide | investigational | unknown | | Details |
| DB06042 | ZEN-012 | investigational | unknown | | Details |
| DB05920 | RTA 744 | investigational | unknown | | Details |
| DB05706 | 13-deoxydoxorubicin | investigational | unknown | | Details |
| DB06263 | Amrubicin | investigational | unknown | | Details |
| DB06362 | Becatecarin | investigational | unknown | | Details |
| DB06420 | Annamycin | investigational | unknown | | Details |
| DB06421 | Declopramide | investigational | unknown | | Details |
| DB00694 | Daunorubicin | approved | yes | inhibitor | Details |
| DB09047 | Finafloxacin | approved, investigational | yes | inhibitor | Details |
| DB06013 | Aldoxorubicin | investigational | yes | inhibitor | Details |