Table 8.
Select candidate inhibitors of extracellular proteases in cancer
| Drug | Specificity | Highest phase completed | Reference |
|---|---|---|---|
| Rebimastat | MMP-2, -9 | Phase III | 97 |
| SB-3CT | MMP-2, -9 | Preclinical | 98 |
| CGS27023A | MMP-1, -2, -3 | Phase I | 99 |
| Minocycline | MMP-1, -2, -3 | Preclinical | 100 |
| Tanomastat | MMP-2, -3, -9 | Phase III | 101 |
| Batimastat | MMP-1, -2, -3, -7, -9 | Phase II | 102 |
| Neovastat | MMP-1, -2, -7, -9, -13 | Phase III | 103 |
| Metastat (COL-3) | MMP-1, -2, -8, -9, -13 | Phase II | 104 |
| Prinomastat | MMP-2, -3, -7, -9, -13 | Phase III | 105 |
| Genistein | MMP-2, -9, MT1-, MT2-, MT3-MMP | Phase II | 106 |
| Marimastat | MMP broad spectrum | Approved | 107 |
| GI254023X | ADAM-10 | Preclinical | 108 |
| PF-5480090 | ADAM-17 | Preclinical | 109 |
| KB-R7785 | ADAM-10, -12 | Preclinical | 110 |
| GW280264X | ADAM-10, -17 | Preclinical | 108 |
| INCB3619 | ADAM-10, -17 | Preclinical | 111 |
| INCB7839 | ADAM-10, -17 | Terminated | 112 |
| Upamostat (WX-671) | uPA | Phase II | 113 |
| Aprotinin | uPA | Terminated | 114 |
Abbreviations: MMP, matrix metalloproteinases; uPA, urokinase plasminogen activator; MT, membrane type.