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. Author manuscript; available in PMC: 2017 Feb 1.
Published in final edited form as: Pharmacol Ther. 2015 Dec 2;158:63–70. doi: 10.1016/j.pharmthera.2015.11.013

Table 1.

Inhibitors of the PI3K/AKT/mTOR pathway currently under clinical development for breast cancer. HR, hormone receptor; MBC, metastatic breast cancer; TNBC triple negative breast cancer; AR, androgen receptor. Information retrieved from clinicaltrials.gov.

Agent Activity Phase of clinical development
Everolimus mTORC1 allosteric inh. Approved
Temsirolimus mTORC1 allosteric inh. Approved
BEZ235 PI3K/mTOR Phase II in HER2+ patients failing to prior trastuzumab, and in HR+ in combination with endocrine treatment
GDC-0980 PI3K/mTOR Phase II in combination with endocrine therapy
Buparlisib (BKM120) Pan-class I PI3K Phase III in combination with endocrine treatment in HR+/HER2−; in combination with BYL719 in MBC; in TNBC; and in combination with neoadjuvant trastuzumab in HER2+ patients
Pictilisib (GDC-0941) Pan-class I PI3K Phase II in HR+ in combination with endocrine treatment
GDC-0032 PI3K p110α, δ, and γ inhibitor Phase I with anti-HER2 treatment in HER2+ patients; Ib/II with enzatulamide in AR+ TNBC patients; and III in combination with endocrine therapy in HR+/HER2− patients
BYL719 PI3K p110α Phase I in combination with T-DM1 in HER2+ patients progressing to trastuzumab; and II in monotherapy in patients harboring alterations on the PI3K pathway, or in combination with endocrine therapy
MK-2206 AKT Phase II in combination with endocrine therapy in HR+ patients
GDC-0068 AKT Phase II in TNBC
AZD5363 AKT Phase I/II in combination with endocrine therapy in HR+ patients