MMP and integrin antagonists in clinical trials
Inhibitors . | Structure . | Specificity . | Status/indication . |
|---|---|---|---|
| MMPs | |||
| Batimastat (BB-94) | Peptidomimetic | MMP-1, -2, -3, -7, -9 | Development halted |
| Marimastat (BB-2516) | Peptidomimetic | MMP-1, -2, -7, -9 | Phase 3/gastric cancer; phase 2/pancreatic cancer |
| BAY12-9566 | Nonpeptidomimetic | MMP-2, -3, -9 | Development halted |
| AG3340 | Nonpeptidomimetic | MMP-2, -3 | Phase 2/3/no benefit |
| BMS-275291 | Nonpeptidomimetic | Broad spectrum | Phase 1/2/NSCL |
| MMI270 | Nonpeptidomimetic | Broad spectrum | Phase 1/advanced cancer |
| Metastat (Col-3) | Tetracycline derivative | MMP-2, -9 | Phase 2/Kaposi sarcoma |
| Periostat | Tetracycline derivative | Broad spectrum | Phase M/periodontal disease |
| Neovastat (AE-941) | Shark cartilage extract | Broad spectrum | Phase 2/multiple myeloma; phase 3/NSCL |
| Not known | Green tea extract | MMP-2, -9 | Phase 3/cancer |
| Integrins | |||
| Efalizumab/Hu1124 | Humanized MAb | CD11α subunit | Phase 3/psoriasis |
| Anti-CD18 | Humanized MAb | CD18 | Phase 2/myocardial infarction |
| Anti-LFA1 | Murine | CD18 | Phase 3/allograft rejection |
| Hu23F2G | Humanized MAb | CD11/CD18 integrin | Phase 2/multiple sclerosis; phase 2/myocardial infarction; phase 3/stroke |
| LDP-01 | Humanized MAb | CD18 integrin subunit | Phase 2/allograft rejection/stroke |
| LDP-02 | Humanized MAb | α4β7-integrin | Phase 2/ulcerative colitis |
| Volociximab & erlotinnib | MAb | α5β1-integrin | Phase 2/metastatic NSCL |
| ATN-161 | PHSRN motif from FN | α5β1-integrin | Phase 1/NSCL |
| M200 | MAb | α5β1-integrin | Phase 2/kidney cancer |
| Vitaxin/LM609 | Humanized MAb | αVβ3-integrin | Phase 2/sarcoma |
| Antegren | Humanized MAb | α4β1-integrin | Phase 3/multiple sclerosis; phase 2/colitis, Crohn disease |
| Tysabri/natalizumab | MAb | α4β1-integrin | Phase M/multiple sclerosis |
| Abciximab | Chimeric Ab | αIIbβ3, αVβ3, αMβ2 | FDA approved |
| Eptifibatide | Cyclic heptapeptide | αIIbβ3-integrin | FDA approved |
| Tirofiban | Peptidomimetic | αIIbβ3-integrin | FDA approved/myocardial infarction |
| Cilengitide | Cyclic RGD peptide | αVβ3/αVβ5-integrin | Phase 2/GBM |
| Altocor/lovastatin | Chemical | αLβ2-integrin | FDA approval/atherosclerosis |
Inhibitors . | Structure . | Specificity . | Status/indication . |
|---|---|---|---|
| MMPs | |||
| Batimastat (BB-94) | Peptidomimetic | MMP-1, -2, -3, -7, -9 | Development halted |
| Marimastat (BB-2516) | Peptidomimetic | MMP-1, -2, -7, -9 | Phase 3/gastric cancer; phase 2/pancreatic cancer |
| BAY12-9566 | Nonpeptidomimetic | MMP-2, -3, -9 | Development halted |
| AG3340 | Nonpeptidomimetic | MMP-2, -3 | Phase 2/3/no benefit |
| BMS-275291 | Nonpeptidomimetic | Broad spectrum | Phase 1/2/NSCL |
| MMI270 | Nonpeptidomimetic | Broad spectrum | Phase 1/advanced cancer |
| Metastat (Col-3) | Tetracycline derivative | MMP-2, -9 | Phase 2/Kaposi sarcoma |
| Periostat | Tetracycline derivative | Broad spectrum | Phase M/periodontal disease |
| Neovastat (AE-941) | Shark cartilage extract | Broad spectrum | Phase 2/multiple myeloma; phase 3/NSCL |
| Not known | Green tea extract | MMP-2, -9 | Phase 3/cancer |
| Integrins | |||
| Efalizumab/Hu1124 | Humanized MAb | CD11α subunit | Phase 3/psoriasis |
| Anti-CD18 | Humanized MAb | CD18 | Phase 2/myocardial infarction |
| Anti-LFA1 | Murine | CD18 | Phase 3/allograft rejection |
| Hu23F2G | Humanized MAb | CD11/CD18 integrin | Phase 2/multiple sclerosis; phase 2/myocardial infarction; phase 3/stroke |
| LDP-01 | Humanized MAb | CD18 integrin subunit | Phase 2/allograft rejection/stroke |
| LDP-02 | Humanized MAb | α4β7-integrin | Phase 2/ulcerative colitis |
| Volociximab & erlotinnib | MAb | α5β1-integrin | Phase 2/metastatic NSCL |
| ATN-161 | PHSRN motif from FN | α5β1-integrin | Phase 1/NSCL |
| M200 | MAb | α5β1-integrin | Phase 2/kidney cancer |
| Vitaxin/LM609 | Humanized MAb | αVβ3-integrin | Phase 2/sarcoma |
| Antegren | Humanized MAb | α4β1-integrin | Phase 3/multiple sclerosis; phase 2/colitis, Crohn disease |
| Tysabri/natalizumab | MAb | α4β1-integrin | Phase M/multiple sclerosis |
| Abciximab | Chimeric Ab | αIIbβ3, αVβ3, αMβ2 | FDA approved |
| Eptifibatide | Cyclic heptapeptide | αIIbβ3-integrin | FDA approved |
| Tirofiban | Peptidomimetic | αIIbβ3-integrin | FDA approved/myocardial infarction |
| Cilengitide | Cyclic RGD peptide | αVβ3/αVβ5-integrin | Phase 2/GBM |
| Altocor/lovastatin | Chemical | αLβ2-integrin | FDA approval/atherosclerosis |
Phase M indicates on the market; NSCL, non-small-cell lung cancer; Mab, monoclonal antibody; FN, fibronectin; GBM, glioblastoma multiforme; and FDA, Food and Drug Administration