Table 1.
Selected PI3K inhibitors approved or in clinical trials.
| Inhibitor | Structure | IC50 (nmol/L) |
Isoform specificity | Selectivity over mTOR | Organization (development status) | |||
|---|---|---|---|---|---|---|---|---|
| p110α | p110β | p110δ | p110γ | |||||
| Idelalisib |  |
820 | 565 | 2.5 | 89 | p110δ specific | unknown | Gilead (launched) |
| IPI-145 |  |
1602 | 85 | 3 | 27 | PI3Kδ, γ specific | unknown | Infinity Pharmaceuticals (phase III) |
| NVP-BEZ235 |  |
4 | 76 | 5 | 7 | pan | No | Novartis (phase I) |
| BKM-120 |  |
52 | 166 | 116 | 262 | pan | Yes | Novartis (phase III) |
| BYL-719 |  |
5 | 1200 | 290 | 250 | PI3Kα specific | Yes | Novartis (phase III) |
| GDC-0941 |  |
3 | 33 | 3 | 75 | pan | Yes | Genentech (phase I) |
| GDC-0980 |  |
5 | 27 | 7 | 14 | pan | No | Genentech (phase II) |
| SF1126 |  |
NA | NA | NA | NA | pan | No | SignalRx (phase I) |
| PX-866 |  |
6 | >300 | 3 | 9 | pan | unknown | Oncothyreon (phase II) |
| PF-04691502 |  |
1.8a | 2.1a | 1.6a | 1.9a | pan | No | Pfizer (phase I) |
| BAY-80-6946 |  |
0.5 | 3.7 | 6.4 | 0.7 | pan | Yes | Bayer (phase III) |
| XL-765 |  |
39 | 113 | 43 | 9 | pan | No | Sanofi (phase I/II) |
| XL-147 |  |
39 | 383 | 36 | 23 | pan | Yes | Sanofi (phase I) |
| GSK2126458 |  |
0.019 | 0.13 | 0.024 | 0.06 | pan | No | GlaxoSmithKline (phase I) |
| ZSTK474 |  |
16 | 44 | 5 | 49 | pan | Yes | Zenyaku (phase I/II) |
NA, not available.
a
Ki.