Table 3.
Inducers of Apoptosis [2]
| Inducers of Apoptosis | Mechanism of Action | Effects | Clinical Trials* |
|---|---|---|---|
| bortezomib | Inhibits 26S proteosome | Decreased degradation of cell cycle and transcription proteins | FDA approved as first-line treatment of multiple myeloma, and as second line treatment of mantle cell lymphoma. |
| suberoylanilide hydroxamic acid (SAHA) | Inhibits histone deacetylase | Suppress tumorigenic gene expression | FDA approved as third-line treatment of cutaneous T cell lymphoma; Phase III (advanced mesothelioma) |
| TLK286 | Formation of a toxic metabolite | Induces apoptosis | Phase III (refractory gynecologic malignancies), combination therapy |
| ONYX015 | Adenovirus; invades and replicates in p53 mutated cells, inactivates p53 gene | Lyses p53 mutated tumor cells | Phase I/II (combination therapy for solid tumors). |
| FTI-R115777 | Blocks farnesylation of Ras, disrupts mitochondrial membrane, induces caspase-9 activation | Inhibit cell growth and induce apoptosis | Phase III (colorectal cancer and AML; no significant improvement in progression frees survival or overall survival, respectively). Phase I/II (pediatric leukemias, glioma) |
| 17AAG | Inhibits HSP90 | Inhibit cell motility and invasion | Phase I/II (multiple myeloma) |
| mapatumumab | TRAILR1 agonist | Inhibit TRAIL ligand binding and apoptotic signal cascade | Phase I/II (several solid tumors) |
| lexatumumab | TRAILR2 agonist |