Table 7.
A List of Reactive Oxygen Species-Modulating Anti-cancer Agents in Clinical Trial
| Agent | Mechanism | Cancer type | Clinical use | Reference |
|---|---|---|---|---|
| ROS elevators | ||||
| Motexafin gadolinium | ROS ↑, TrxR ↓ | Lymphocytic leukemia, lung, brain | Phase III trial, exhibited activity | (189, 207, 208) |
| Elesclomol (STA-4783) | ROS ↑ | Melanoma | Phase II trial, enhanced paclitaxel activity | (163, 304) |
| ATN-224 | SOD ↓ | Prostate | Phase II trial, exhibited activity | (187) |
| 2-ME | SOD ↓, superoxide ↑ | Prostate, breast | Phase II trial, well tolerated, exhibited activity | (128, 294) |
| BSO | GSH ↓, glutamyl synthetase ↓ | Random | Phase I trial, safe with melphalan | (23) |
| Imexon | GSH ↓, ROS ↑, apoptosis ↑, mitochondria function ↓ | Non-Hodgkin's lymphoma, melanoma | Phase I trial, well tolerated with dacarbazine | (79, 325) |
| ROS scavengers | ||||
| Minodronate | NOX ↓ | Multiple myeloma | Phase I trial | (279) |
| Histamine | NOX ↓ | Melanoma | Phase III trial, prolongs survival | (2) |
↓, down-regulation; ↑, up-regulation.
2-ME, 2-methoxyestradiol; ATN-224, choline tetrathiomolybdate; BSO, buthionine sulfoximine; GSH, glutathione reduced; NOX, NADPH oxidase; ROS, reactive oxygen species; SOD, superoxide dismutase; TrxR, thioredoxin reductase.