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Table 2 Phosphatidylinositol 3-kinase pathway inhibitors in clinical development
| Kinase target | Drug | Manufacturer | Mechanism of action |
|---|---|---|---|
| Pan-PI3K | BKM120 | Novartis | ATP-competitive |
| XL-147 | Exelixis | ATP-competitive | |
| PX-866 | Oncothyreon | ATP-competitive | |
| GDC-0941 | Genentech/Roche | ATP-competitive | |
| CH5132799 | Chugai Pharma | ATP-competitive | |
| p110δ-specific | CAL-101 | Calistoga | ATP-competitive |
| p110α-specific | BYL719 | Novartis | ATP-competitive |
| GDC-0032 | Genentech/Roche | ATP-competitive | |
| INK-1117 | Intellikine | ATP-competitive | |
| PI3K/mTOR | PKI-587 | Pfizer | ATP-competitive |
| BEZ235 | Novartis | ATP-competitive | |
| BGT226 | Novartis | ATP-competitive | |
| PF-4691502 | Pfizer | ATP-competitive | |
| GDC-0980 | Genentech/Roche | ATP-competitive | |
| XL-765 | Exelixis | ATP-competitive | |
| SF1126 | Semafor | ATP-competitive/peptide-conjugate | |
| GSK1059615 | GSK | ATP-competitive | |
| TORC1 | Everolimus (RAD001) | Novartis | Indirect, FKBP12-mediated |
| Temsirolimus (CCI-779) | Wyeth/Pfizer | Indirect, FKBP12-mediated | |
| Ridaferolimus (AP-23573) | Merck/Ariad | Indirect, FKBP12-mediated | |
| TORC1/TORC2 | INK-128 | Intellikine | ATP-competitive |
| OSI-027 | OSI Pharm. | ATP-competitive | |
| AZD-8055 | Astrazeneca | ATP-competitive | |
| AKT | AZD5363 | Astrazeneca | ATP-competitive |
| GDC-0068 | Genentech/Roche | ATP-competitive | |
| GSK690693 | GSK | ATP-competitive | |
| MK-2206 | Merck | Allosteric | |
| VQD002 | Vioquest | ATP-competitive |
