Table 1. Synopsis of the MMP Inhibitors Discussed.
| Name of Inhibitor | Type of Inhibitor | MMPs Targeted | Type of Cancer Studied | Toxicity | Outcome |
|---|---|---|---|---|---|
| Batimastat (BB-94) *5362422 | Hydroxymate (zinc chelator) | Broad, including MMP-1, -2, -3, -7, -9, -14 | Malignant Ascites (Pancreatic, Colorectal, Gastric, Ovarian, Cholangiocarcinoma, Ovarian, Mesothelioma) Malignant Pleural Effusion (Non-Small Cell Lung, Breast, Melanoma, Renal, Mesothelioma) |
Musculoskeletal syndrome, Fever, Liver Function Abnormalities, pleural pain at site of injection, GI upset | Canceled in phase III clinical trials (local toxicity, slow accrual, Marimastat developed) |
| Marimastat (BB-2516) *119031 | Hydroxymate (zinc chelator) | Broad, including MMP-1. -2, -3, -7, -9 | Breast, Non-Small Cell Lung, Colorectal, Pancreatic, Gastric, Prostate, Glioblastoma | Musculoskeletal Syndrome, GI upset | Prolongation of survival in randomized Ph2 in gastric cancer, Canceled in phase III clinical trials |
| Tanomastat (BAY 12-9566)*6918336 | Carboxylate (zinc chelator) | MMP-2, -3, -8, -9, -13 | Pancreatic, Ovarian, Small Cell Lung | Hematologic (anemia, thrombocytopenia), electrolyte abnormalities, hyperbilirubinemia, GI upset | Canceled in phase III clinical trials |
| Prinomastat (AG3340) *466151 | Hydroxymate (zinc chelator) | MMP-2, -3, -9, -13, -14 | Non-Small Cell Lung, Esophageal | Musculoskeletal, Venous Thromboembolism, Hematologic, GI Upset | Canceled in phase III clinical trials |
| Rebimastat (BMS-275291) *9913881 | Sulfhydryl based mercaptoacyl zinc chelator | MMP-1, -2, -3, -8, -9, -13, -14 | Non-Small Cell Lung, Breast, Prostate | Dermatologic, Hypersensitivity | Canceled in phase III clinical trials |
| Andecaliximab (GS-5745) | Monoclonal Antibody | MMP-9 | Gastric, Breast, Pancreatic, Non-Small Cell Lung, Esophageal, Colorectal | Neutropenia, Nausea, Pain, GI Upset | Ongoing phase I, II and III clinical trials |
| AB0041, AB0046, GS-5745 | Monoclonal Antibody | MMP-9 | Colorectal | n/a | Active in preclinical studies |
| DX-2400 | Monoclonal Antibody | MMP-14 | Breast, Melanoma, Fibrosarcoma | n/a | Active in preclinical studies |
| Single Chain Fragment Variables | Monoclonal Antibody | MMP-1 MMP-2 MMP-3 | Breast | n/a | Active in preclinical studies |
*
PubChem Identification Number