TABLE 2.
Classification, highest clinical phase, status, and application of PI3K/Akt/mTOR inhibitors in various tumor types based on the GlobalData database.
| Target | Drug Name | Tumor types | Highest phase and ID number of the clinical trial | Status |
|---|---|---|---|---|
| PI3K inhibitors | ||||
| Non-subunit-specific PI3K inhibitor | AZD8186 | Solid Tumor | Phase II—NCT04001569 | Active |
| buparlisib (NVP-BKM120) | Head and Neck Cancer | Phase III—NCT04338399 | Active | |
| copanlisib | Lymphoma | — | Marketed | |
| duvelisib | Leukemia, Lymphoma | — | Marketed | |
| MEN1611 (CH5132799) | Colorectal Cancer | Phase II—NCT04495621 | Active | |
| tenalisib (RP6530) | Breast Cancer | Phase II—NCT05021900 | Active | |
| TQB-3525 | Breast Cancer, Endometrial Cancer, Leukemia, Lymphoma, Ovarian Cancer | Phase II—NCT04324879, NCT04355520, NCT04398953, NCT04610970, NCT04615468, NCT04808570, NCT04836663 | Active | |
| PI3Kα inhibitor | alpelisib | Breast Cancer | — | Marketed |
| CYH-33 (HHCYH-33) | Solid Tumor | Phase I—NCT04586335, NCT04856371 | Active | |
| inavolisib (GDC-0077) | Breast Cancer | Phase III—NCT04191499 | Active | |
| serabelisib (INK-1117) | Solid Tumor | Phase II—NCT04073680 | Active | |
| taselisib | Lymphoma, Myeloma, Solid Tumor | Phase II—NCT02465060 | Active | |
| PI3Kβ inhibitor | GSK2636771 | Lymphoma, Myeloma, Solid Tumor | Phase II—NCT02465060 | Active |
| PI3Kγ inhibitor | eganelisib (IPI-549) | Breast Cancer, Kidney Cancer | Phase II—NCT03961698 | Active |
| PI3Kδ inhibitor | amdizalisib (HMPL-689) | Lymphoma | Phase II—NCT04849351 | Active |
| idelalisib | Leukemia, Lymphoma | — | Marketed | |
| IOA-244 | Lymphoma, Melanoma, Solid Tumor | Phase I—NCT04328844 | Active | |
| linperlisib (YY-20394) | Lymphoma | Phase II—NCT04370405, NCT04379167, NCT04500561, NCT04705090, NCT04948788 | Active | |
| parsaclisib (INCB50465) | Lymphoma, Myelofibrosis | Phase III—NCT04551053, NCT04551066, NCT04796922, NCT04849715 | Active | |
| SHC014748 (SH-748) | Lymphoma | Phase II—NCT04431089, NCT04470141 | Active | |
| umbralisib | Lymphoma | - | Marketed | |
| zandelisib (PWT-143) | Lymphoma | Phase III—NCT04745832 | Active | |
| Various targets | AMG319 (ACP-319), apitolisib, AZD-8835, bimiralisib (PQR309), dactolisib, dezapelisib (NCB-040093), nemiralisib (GSK2269557), pictilisib (GDC-0941), pilaralisib, SAR260301, seletalisib (UCB-5857), SF1126, sonolisib, voxtalisib, ZSTK-474etc. | Inactive/Discontinued | ||
| mTOR inhibitors | ||||
| Allosteric mTOR inhibitor | everolimus | Breast Cancer, Central Nervous System Tumor, Endocrine Tumor, Kidney Cancer | — | Marketed |
| sirolimus | Lymphangioleiomyomatosis | — | Marketed | |
| temsirolimus | Kidney Cancer | — | Marketed | |
| mTOR-kinase inhibitor (inhibits both mTORC1 and mTORC2) | CC-115 | Central Nervous System Tumor | Phase II—NCT02977780 | Active |
| onatasertib (ATG-008) | Solid Tumor | Phase II—NCT03591965, NCT04337463, NCT04518137, NCT04998760 | Active | |
| sapanisertib (MLN0128) | Lymphoma, Myeloma, Solid Tumor | Phase II—NCT02465060 | Active | |
| vistusertib | Lung Cancer | Phase II—NCT02664935, NCT03334617 | Active | |
| Various targets | apitolisib, AZD8055, bimiralisib (PQR309), dactolisib, ridaforolimus (Deforolimus, MK-8669), SF1126, voxtalisibetc. | Inactive/Discontinued | ||
| Akt inhibitors | ||||
| Pan-Akt | afuresertib | Ovarian Cancer, Prostate Cancer | Phase II—NCT04060394, NCT04374630 | Active |
| capivasertib | Breast Cancer, Prostate Cancer | Phase III—NCT03997123, NCT04305496, NCT04493853, NCT04862663 | Active | |
| ipatasertib | Breast Cancer, Prostate Cancer | Phase III—NCT03072238, NCT03337724, NCT04060862, NCT04177108, NCT04650581 | Active | |
| MK-2206 | Breast Cancer, Lung Cancer, Thymoma | Phase II—NCT01042379, NCT01306045 | Active | |
| TAS-117 | Solid Tumor | Phase II—NCT04770246 | Active | |
| triciribine (PTX-200) | Leukemia | Phase II—NCT02930109 | Active | |
| uprosertib | Myeloma, Solid Tumor | Phase II—NCT01902173, NCT01989598 | Active | |
| Various targets | COTI-2, LY-2503029, perifosineetc. | Inactive/Discontinued | ||
| Dual inhibitors | ||||
| PI3K, mTOR dual inhibitor | gedatolisib | Breast Cancer | Phase II—NCT03698383, NCT03911973 | Active |
| paxalisib | Central Nervous System Tumor | Phase III—NCT03970447 | Active | |
| samotolisib | Lymphoma, Solid Tumor | Phase II—NCT03155620, NCT03213678 | Active | |