| DB00762 | Irinotecan | approved, investigational | yes | inhibitor | Details |
| DB01030 | Topotecan | approved, investigational | yes | inhibitor | Details |
| DB04690 | Camptothecin | experimental | unknown | inhibitor | Details |
| DB04882 | Edotecarin | investigational | unknown | | Details |
| DB05129 | Elsamitrucin | investigational | unknown | | Details |
| DB04967 | Lucanthone | investigational | yes | inhibitor | Details |
| DB05482 | SN-38 | investigational | unknown | | Details |
| DB05806 | Cositecan | investigational | unknown | | Details |
| DB06069 | XMT-1001 | investigational | unknown | | Details |
| DB06159 | Rubitecan | investigational | unknown | | Details |
| DB05630 | Sodium stibogluconate | approved, investigational | yes | inhibitor | Details |
| DB07354 | 2,3-DIMETHOXY-12H-[1,3]DIOXOLO[5,6]INDENO[1,2-C]ISOQUINOLIN-6-IUM | experimental | unknown | | Details |
| DB08159 | 4-(5,11-DIOXO-5H-INDENO[1,2-C]ISOQUINOLIN-6(11H)-YL)BUTANOATE | experimental | unknown | | Details |
| DB11254 | Hexylresorcinol | approved | unknown | inhibitor | Details |
| DB14962 | Trastuzumab deruxtecan | approved, investigational | yes | inhibitor | Details |
| DB14962 | Trastuzumab deruxtecan | approved, investigational | unknown | inhibitor | Details |
| DB12893 | Sacituzumab govitecan | approved, investigational | yes | inhibitor | Details |
| DB00997 | Doxorubicin | approved, investigational | yes | inhibitor | Details |
| DB00970 | Dactinomycin | approved, investigational | unknown | inhibitor | Details |