Table 1.
Summary of PI3K–AKT-targeting drugs.
| Drugs | Mechanism | Combination with | Phase | Refs. |
|---|---|---|---|---|
| BKM120 | PI3K inhibitor | - Lapatinib Trastuzumab/Paclitaxel Fulvestrant Tamoxifen LDE225 |
Phase II Phase I/II Phase II Phase I Phase II Phase I |
[58] [59] [60] [61] [62] [63] |
| Tenalisib (RP6530) Taselisib (GDC-0032) |
PI3K δ/γ inhibitor PI3K inhibitor |
- Enzalutamide |
Phase II Phase I/II |
[64] [65] |
| BYL-719 (alpelisib) | PI3K α inhibitor | - Letrozole Nab-paclitaxel |
Phase II Phase I Phase I/II |
[66] [67] [68] |
| Pictilisib (GDC-0941) | PI3K inhibitor | Cisplatin Paclitaxel (with and without Bevacizumab or Trastuzumab) and Letrozole |
Phase I/II Phase I |
[69] [70] |
| GDC-0084 | PI3K inhibitor | Trastuzumab | Phase II | [71] |
| PF-05212384 (gedatolisib) |
PI3K/mTOR inhibitor | Docetaxel/Cisplatin/Dacomitinib Paclitaxel and carboplatin |
Phase I Phase I |
[72] [73] |
| AZD8186 | PI3K β Inhibitor | Docetaxel | Phase I | [74] |
| Serabelisib | PI3K α inhibitor | Canagliflozin | Phase I/II | [75] |
| Ipatasertib | AKT inhibitor | Trastuzumab and pertuzumab | Phase I | [76] |
| MK2206 | AKT inhibitor | Lapatinib ditosylate Paclitaxel - Anastrozole (with or without goserelin acetate) |
Phase I Phase I Phase II Phase II |
[77] [78] [79] [80] |