Table I.
Apoptosis pathway–targeting drugs in clinical trials.
| Approach/Drug | Other names | Target | Type | Clinical Trial Status |
Company |
|---|---|---|---|---|---|
| Targeting Antiapoptotic BCL-2 Proteins | |||||
| Oblimersen sodium | G3139, Genasense, Augmerosen | BCL-2 | Antisense oligonucleotide | Phase 3 | Genta Incorporated |
| Obatoclax mesylate | GX15-070 | BCL-2, BCL-XL, BCL-w and MCL-1 | Small-molecule inhibitor | Phase 1/2 | Gemin X/Teva Pharmaceutical Industries |
| AT-101 | (−)-gossypol | BCL-2, BCL-XL and MCL-1 | Small-molecule inhibitor | Phase 2 | Ascenta Therapeutics |
| Navitoclax | ABT-263 | BCL-XL, BCL-2 and BCL-w | Small-molecule inhibitor | Phase 2 | AbbVie and Genentech |
| GDC-0199 | ABT-199 | BCL-2 | Small-molecule inhibitor | Phase 1 | AbbVie and Genentech |
| Targeting IAPs | |||||
| AEG35156 | GEM640 | XIAP | Antisense oligonucleotide | Phase 1/2 | Aegera Therapeutics |
| YM155 | survivin | Small-molecule antagonist | Phase 2 | Astellas Pharma | |
| AT-406 | Debio 1143 | XIAP, cIAP1 and cIAP2 | SMAC mimetic | Phase 1 | Ascenta Therapeutics and Debiopharm S.A. |
| TL32711 | Birinapant | cIAP1 | SMAC mimetic | Phase 1/2 | TetraLogic Pharma |
| GDC-0917 | IAPs | SMAC mimetic | Phase 1 | Genentech | |
| LCL161 | IAPs | SMAC mimetic | Phase 1/2 | Novartis | |
| AEG40826-2HCl | HGS1029 | IAPs | SMAC mimetic | Phase 1 | Aegera Therapeuics and GlaxoSmithKline/Human Genome Science? |
| LY2181308 | Gataparsen | survivin | Antisense oligonucleotide | Phase 2 | Eli Lilly and Company |
| Targeting Death Receptors | |||||
| rhApo2L/TRAIL | Dulanermin | DR4, DR5 | Soluble ligand | Phase 2 | Genentech and Amgen |
| Mapatumumab | HGS-ETR1, TRM-1 | DR4 | Monoclonal antibody | Phase 2 | GlaxoSmithKline/Human Genome Sciences |
| Lexatumumab | HGS-ETR2 | DR5 | Monoclonal antibody | Phase 1 | GlaxoSmithKline/Human Genome Sciences |
| Drozitumab | PRO95780, Apomab | DR5 | Monoclonal antibody | Phase 2 | Genentech |
| AMG655 | Conatumumab | DR5 | Monoclonal antibody | Phase 2 | Amgen |
| CS-1008 | Tigatuzumab | DR5 | Monoclonal antibody | Phase 2 | Daiichi |
| LBY-135 | DR5 | Monoclonal antibody | Novartis | ||
| TAS266 | DR5 | Nanobody | Phase 1 | Novartis |
IAP, inhibitor of apoptosis proteins; SMAC, second mitochondria-derived activator of caspase