| DB00003 | Dornase alfa | approved | yes | | Details |
| DB00242 | Cladribine | approved, investigational | yes | other/unknown | Details |
| DB00236 | Pipobroman | approved | yes | cross-linking/alkylation | Details |
| DB00262 | Carmustine | approved, investigational | yes | other/unknown | Details |
| DB00276 | Amsacrine | approved, investigational | yes | intercalation | Details |
| DB00291 | Chlorambucil | approved | unknown | cross-linking/alkylation | Details |
| DB00305 | Mitomycin | approved | yes | cross-linking/alkylation | Details |
| DB00352 | Tioguanine | approved | yes | intercalation | Details |
| DB00406 | Gentian violet cation | approved | yes | intercalation | Details |
| DB00428 | Streptozocin | approved, investigational | yes | cross-linking/alkylation | Details |
| DB00488 | Altretamine | approved | yes | other/unknown | Details |
| DB00515 | Cisplatin | approved | yes | cross-linking/alkylation | Details |
| DB00526 | Oxaliplatin | approved, investigational | yes | adductcross-linking/alkylation | Details |
| DB00531 | Cyclophosphamide | approved, investigational | yes | cross-linking/alkylation | Details |
| DB00553 | Methoxsalen | approved | yes | intercalation | Details |
| DB00614 | Furazolidone | experimental, vet_approved | yes | cross-linking/alkylation | Details |
| DB00694 | Daunorubicin | approved | yes | intercalation | Details |
| DB00709 | Lamivudine | approved, investigational | yes | binder | Details |
| DB00738 | Pentamidine | approved, investigational | unknown | intercalation | Details |
| DB00779 | Nalidixic acid | approved, investigational | yes | other | Details |
| DB00791 | Uracil mustard | approved | unknown | intercalation | Details |
| DB00827 | Cinoxacin | approved, investigational, withdrawn | unknown | intercalation | Details |
| DB00853 | Temozolomide | approved, investigational | yes | cross-linking/alkylation | Details |
| DB00958 | Carboplatin | approved | yes | cross-linking/alkylation | Details |
| DB00970 | Dactinomycin | approved, investigational | yes | adduct | Details |
| DB01008 | Busulfan | approved, investigational | yes | cross-linking/alkylation | Details |
| DB14753 | Hydroxystilbamidine | approved | yes | other/unknown | Details |
| DB01042 | Melphalan | approved | yes | cross-linking/alkylation | Details |
| DB01096 | Oxamniquine | approved | yes | other/unknown | Details |
| DB01103 | Quinacrine | investigational | yes | intercalation | Details |
| DB01123 | Proflavine | approved | yes | intercalation | Details |
| DB01168 | Procarbazine | approved, investigational | yes | cross-linking/alkylation | Details |
| DB01206 | Lomustine | approved, investigational | yes | cross-linking/alkylation | Details |
| DB00888 | Mechlorethamine | approved, investigational | yes | intercalation | Details |
| DB01280 | Nelarabine | approved, investigational | yes | incorporation into and destabilization | Details |
| DB01262 | Decitabine | approved, investigational | yes | other/unknown | Details |
| DB01611 | Hydroxychloroquine | approved | yes | cross-linking/alkylation | Details |
| DB01702 | 2-(3,4-Dihydroxyphenyl)Acetic Acid | experimental | unknown | | Details |
| DB00131 | Adenosine phosphate | approved, investigational, nutraceutical, withdrawn | unknown | component of | Details |
| DB00693 | Fluorescein | approved | no | other | Details |
| DB02379 | Beta-D-Glucose | experimental | unknown | | Details |
| DB00173 | Adenine | approved, nutraceutical | unknown | | Details |
| DB03148 | Adenosine 5'-methylenediphosphate | experimental | unknown | | Details |
| DB00536 | Guanidine | approved | unknown | | Details |
| DB00126 | Ascorbic acid | approved, nutraceutical | unknown | cleavage | Details |
| DB04858 | Tirapazamine | investigational | unknown | | Details |
| DB04874 | Picoplatin | investigational | unknown | | Details |
| DB05129 | Elsamitrucin | investigational | unknown | | Details |
| DB04996 | Satraplatin | investigational | unknown | | Details |
| DB04950 | Ranpirnase | investigational | unknown | | Details |
| DB04992 | AP5346 | investigational | unknown | | Details |
| DB04967 | Lucanthone | investigational | yes | intercalation | Details |
| DB04961 | Troxacitabine | investigational | unknown | | Details |
| DB05706 | 13-deoxydoxorubicin | investigational | unknown | | Details |
| DB00997 | Doxorubicin | approved, investigational | yes | intercalation | Details |
| DB06263 | Amrubicin | investigational | unknown | | Details |
| DB06328 | Methoxyamine | investigational | unknown | | Details |
| DB06331 | 4-O-Demethylpenclomedine | investigational | unknown | | Details |
| DB06408 | Taribavirin | investigational | unknown | | Details |
| DB06420 | Annamycin | investigational | unknown | | Details |
| DB06421 | Declopramide | investigational | unknown | | Details |
| DB00249 | Idoxuridine | approved, investigational | yes | other | Details |
| DB00442 | Entecavir | approved, investigational | yes | other | Details |
| DB01610 | Valganciclovir | approved, investigational | yes | adduct | Details |
| DB01265 | Telbivudine | approved, investigational | yes | | Details |
| DB01181 | Ifosfamide | approved | yes | other/unknown | Details |
| DB00928 | Azacitidine | approved, investigational | yes | other | Details |
| DB00445 | Epirubicin | approved | unknown | intercalation | Details |
| DB00631 | Clofarabine | approved, investigational | yes | other/unknown | Details |
| DB05109 | Trabectedin | approved, investigational | yes | binder | Details |
| DB01177 | Idarubicin | approved | yes | intercalation | Details |
| DB00432 | Trifluridine | approved, investigational | yes | other/unknown | Details |
| DB00385 | Valrubicin | approved | yes | intercalation | Details |
| DB00441 | Gemcitabine | approved | yes | cross-linking/alkylation | Details |
| DB00987 | Cytarabine | approved, investigational | yes | cross-linking/alkylation | Details |
| DB01099 | Flucytosine | approved, investigational | yes | cross-linking/alkylation | Details |
| DB01204 | Mitoxantrone | approved, investigational | yes | intercalation | Details |
| DB01004 | Ganciclovir | approved, investigational | yes | incorporation into and destabilization | Details |
| DB00290 | Bleomycin | approved, investigational | yes | cleavage | Details |
| DB01041 | Thalidomide | approved, investigational, withdrawn | yes | intercalation | Details |
| DB06810 | Plicamycin | approved, investigational, withdrawn | yes | antagonist | Details |
| DB01073 | Fludarabine | approved | yes | incorporation into and destabilization | Details |
| DB00544 | Fluorouracil | approved | yes | incorporation into and destabilization | Details |
| DB01101 | Capecitabine | approved, investigational | yes | incorporation into and destabilizationinhibition of synthesis | Details |
| DB06803 | Niclosamide | approved, investigational, vet_approved | unknown | antagonist | Details |
| DB04572 | Thiotepa | approved, investigational | yes | cross-linking/alkylation | Details |
| DB04571 | Trioxsalen | approved | yes | cross-linking/alkylation | Details |
| DB00851 | Dacarbazine | approved, investigational | yes | cross-linking/alkylation | Details |
| DB05245 | Silver sulfadiazine | approved, vet_approved | yes | binder | Details |
| DB00911 | Tinidazole | approved, investigational | yes | binder | Details |
| DB01030 | Topotecan | approved, investigational | yes | intercalation | Details |
| DB00127 | Spermine | experimental, nutraceutical | yes | binder | Details |
| DB02842 | 9-amino-n-[3-(dimethylamino)propyl]acridine-4-carboxamide | experimental | unknown | intercalation | Details |
| DB13145 | Nedaplatin | approved, investigational | yes | ligand | Details |
| DB09327 | Tegafur-uracil | approved, investigational | yes | | Details |
| DB09348 | Propiolactone | approved, withdrawn | yes | adduct | Details |
| DB15466 | Tallimustine | experimental | unknown | binder | Details |
| DB12674 | Lurbinectedin | approved, investigational | unknown | adduct | Details |
| DB16627 | Melphalan flufenamide | approved, withdrawn | yes | cross-linking/alkylation | Details |