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