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Table 1 PI3K, AKT, and mTOR inhibitors selected for preclinical and clinical development(main PI3K/AKT/mTOR inhibitors in clinical trials) [73,74,75,76,77,78,79,80,81]

From: RETRACTED ARTICLE: Roles of the PI3K/AKT/mTOR signalling pathways in neurodegenerative diseases and tumours

Inhibitor

Compound or drug

Targets

Tumor types currently under investigation

PI3K

LY294002

Pan-class I PI3K

Advanced solid tumors

Buparlisib (BKM120)

Pan-class I PI3K

Advanced solid tumors

SAR245408 (XL-147)

Pan-class I PI3K

Advanced solid tumors

Sonolisib (PX-866)

P110-Delta, gamma

Phase II and III trials in NHL and CLL are underway, both alone and in combination with hantiCD20 antibodies

Pictilisib (GDC-0941)

P110-alpha, Delta

Added alpha specificity may provide benefit in MCLandsome others versus delta-only inhibitors

Taselisib (GDC-0032)

P110-alpha, Delta

Advanced solid tumors and metastatic breast cancer (ERþ)

AKT

Pirifosine

AKT

Advanced solid tumors, multiple myeloma

Palomid529(P529)

AKT

Advanced solid tumors, breast cancer, cervical cancer, endometrial cancer, leukemias, melanoma, multiple myeloma

GSK2141795

AKT

Advanced solid tumors, breast cancer, cervical cancer, endometrial cancer, leukemias, melanoma, multiple myeloma

MK-2206

AKT

Advanced solid tumors, breast cancer, colorectal cancer, endometrial cancer, head & neck cancer, lung cancer, lymphomas, pancreatic cancer, prostate cancer

mTOR

Everolimus(RAD001)

mTORC1

Approved for the treatment of renal cell carcinoma, subependymal giant cell astrocytoma associated with tuberous sclerosis, pancreatic neuroendocrine tumors, and ERþ breast cancer

Temsirolimus

mTORC1

Approved for the treatment of renal cell carcinoma

Rapamycin

mTORC1

Advanced solid tumors, multiple myeloma

Dual

NVP-BEZ235 (BEZ-235)

P110, mTORC1/2

Advanced solid tumors, multiple myeloma

SAR245409(XL765)

PI3K/mTOR

Advanced solid tumors, CLL, indolent non-Hodgkin lymphoma, mantle cell lymphoma, ovarian cancer

GDC-0980

PI3K/mTOR

Solid cancers, non-Hodgkin lymphoma, breast cancer, prostate cancer