Table 1.
Current UPS-targeting anti-cancer drugs in clinical trials. (current as of 07.30.2012 from the National Institutes of Health; www.clinicaltrials.gov)
| Inhibitors | Target | Company | Disease | Stage |
|---|---|---|---|---|
| Bortezomib (Velcade) | Proteasome | Millennium | Multiple myeloma and mantle cell lymphoma | Approved |
| Bortezomib (Velcade) | Proteasome | Millennium | Glioblastoma, Non-small cell lung cancer, | Phase II |
| MLN9708 | Proteasome | Millennium | Multiple myeloma and other cancers | Phase III |
| Carfilzomib (PR-171) | Proteasome | ONYX | Multiple myeloma | Phase III |
| Carfilzomib (PR-171) | Proteasome | ONYX | Ovarian Cancer; Renal Cancer; Non-small Cell Lung Cancer | Phase II |
| Onx 0912 (PR-047) | Proteasome | ONYX | Multiple myeloma and other cancers | Phase II |
| CEP-18770 | Proteasome | Cephalon | Multiple myeloma and other cancers | Phase II |
| NPI-0052 | Proteasome | Nereus | Multiple myeloma and leukemia | Phase I |
| MLN4924 | E1 (Nedd8 activating E1, NAE) | Millennium | Diffuse Large B-cell Lymphoma | Phase II |
| Nutlin (RG7112) | E3 (Mdm2) | Roche | Advanced solid tumors | Phase I |
| JNJ-26854165 | E3 (Mdm2) | Johnson & Johnson | Advanced or refractory solid tumors | Phase I |
| GDC-0152 | E3 (IAPs) | Genentech | Advanced or metastatic malignancies | Phase I |
| GDC-0917 | E3 (IAPs) | Genentech | Refractory Solid Tumors or Lymphoma | Phase I |
| LCL-161 | E3 (IAPs) | Novartis | Breast cancer and other advanced solid tumors | Phase II |
| AT-406 | E3 (IAPs) | Ascenta Therapeutics | Solid tumors and lymphomas, Acute Myelogenous Leukemia | Phase I |
| AEG-40826 (HGS1029) | E3 (IAPs) | Aegera Therapeutics | Advanced Solid Tumors | Phase I |
| TL-32711 | E3 (IAPs) | Tetralogics Pharma | Metastatic solid tumors and Acute Myelogenous Leukemia | Phase II |
Note: only Smac-mimetic inhibitors of E3 IAP were listed. Additional IAP-targeting antagonists undergoing clinical trials, such as AEG 35156 (XIAP, antisense oligos) and YM155 (Survivin inhibitor), were not included in the table.