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. 2022 Jan 14;40(4):989–1033. doi: 10.1007/s10555-021-10006-2

Table 2.

The application of PI3K/Akt/mTOR inhibitors in different cancers

Target Drug name Tumor type ID number and the highest developmental stage Status
PI3K inhibitors
PI3K pan-inhibitor Copanlisib Lymphoma Marketed
Buparlisib (NVP-BKM120) Head and neck cancer Phase III — NCT04338399 Active
PI3Kα Alpelisib Breast cancer Marketed
Inavolisib (GDC-0077) Breast cancer Phase III — NCT04191499 Active
Serabelisib (INK-1117) Solid tumor Phase II — NCT04073680 Active
MEN1611 (CH5132799) Colorectal cancer Phase II — NCT04495621 Active
CYH-33 (HHCYH-33) Solid tumor Phase I — NCT04586335, NCT04856371 Active
PI3Kβ AZD8186 Solid tumor Phase II — NCT04001569 Active
GSK2636771 Lymphoma, myeloma, solid tumor Phase II — NCT02465060 Active
PI3Kγ Eganelisib (IPI-549) Breast cancer, kidney cancer Phase II — NCT03961698 Active
PI3Kδ Idelalisib Lymphoma, leukemia Marketed
Umbralisib Lymphoma Marketed
Parsaclisib (INCB50465) Myelofibrosis, lymphoma Phase III — NCT04551066, NCT04551053, NCT04796922, NCT04849715 Active
Zandelisib (PWT-143) Lymphoma Phase III — NCT04745832 Active
SHC014748 (SH-748) Lymphoma Phase II — NCT04470141, NCT04431089 Active
Linperlisib (YY-20394) Lymphoma Phase II — NCT04500561, NCT04705090, NCT04370405, NCT04379167, NCT04948788 Active
IOA-244 Lymphoma, melanoma, solid tumor Phase I — NCT04328844 Active
PI3Kδ, PI3Kγ Duvelisib Lymphoma, leukemia Marketed
PI3Kδ, PI3Kγ Tenalisib (RP6530) Breast cancer Phase II — NCT05021900 Active
PI3Kα, PI3Kδ, PI3Kγ Taselisib Solid tumor, lymphoma, myeloma Phase II — NCT02465060 Active
Undisclosed PI3K isoform inhibitor TQ-B-3525 Lymphoma, leukemia, endometrial cancer, ovarian cancer, breast cancer Phase II — NCT04615468, NCT04610970, NCT04398953, NCT04324879, NCT04836663, NCT04808570, NCT04355520 Active
HMPL-689 Lymphoma Phase II — NCT04849351 Active
PI3K, mTOR dual inhibitor Paxalisib CNS cancer Phase III — NCT03970447 Active
Samotolisib Solid tumor, lymphoma Phase II — NCT03213678, NCT03155620 Active
Gedatolisib Breast cancer Phase II — NCT03698383, NCT03911973 Active
Various targets Pictilisib (GDC-0941), Pilaralisib, ZSTK-474, Sonolisib, SAR260301, Seletalisib (UCB-5857), AMG319 (ACP-319), Nemiralisib (GSK2269557), Dezapelisib (NCB-040093), AZD-8835, Dactolisib, Apitolisib, SF1126, Bimiralisib (PQR309), Voxtalisib, etc Inactive/discontinued
mTOR inhibitors
Allosteric mTOR inhibitor Everolimus Breast cancer, kidney cancer, endocrine tumor, CNS cancer Marketed
Sirolimus Lymphangioleiomyomatosis (LAM) Marketed
Temsirolimus Kidney cancer Marketed
mTOR kinase inhibitor Sapanisertib (MLN0128) Solid tumor, lymphoma, myeloma Phase II — NCT02465060 Active
Vistusertib Lung cancer Phase II — NCT02664935, NCT03334617 Active
CC-115 CNS cancer Phase II — NCT02977780 Active
Onatasertib (ATG-008) Solid tumor Phase II — NCT04518137, NCT03591965, NCT04998760, NCT04337463 Active
PI3K, mTOR dual inhibitor Paxalisib CNS cancer Phase III — NCT03970447 Active
Samotolisib Solid tumor, lymphoma Phase II — NCT03213678, NCT03155620 Active
Gedatolisib Breast cancer Phase II — NCT03698383, NCT03911973 Active
Various targets Dactolisib, Apitolisib, SF1126, Bimiralisib (PQR309), Voxtalisib, Ridaforolimus (Deforolimus, MK-8669), AZD8055 Inactive/discontinued
Akt inhibitors
Pan-Akt Ipatasertib Prostate cancer, breast cancer Phase III — NCT04650581, NCT04177108, NCT04060862, NCT03337724, NCT03072238 Active
Capivasertib Breast cancer, prostate cancer Phase III — NCT03997123, NCT04493853, NCT04862663, NCT04305496 Active
Triciribine (PTX-200) Leukemia Phase II — NCT02930109 Active
TAS-117 Solid tumor Phase II — NCT04770246 Active
Afuresertib Ovarian cancer, prostate cancer Phase II — NCT04060394, NCT04374630 Active
MK-2206 Lung cancer, thymoma, breast cancer Phase II — NCT01042379, NCT01306045 Active
Uprosertib Myeloma, solid tumor Phase II — NCT01989598, NCT01902173 Active
Various targets COTI-2, Perifosine, LY-2503029 Inactive/discontinued