Table 3.

Investigational dual PI3K/mTOR inhibitors.

Inhibitor Name	Company	Stage of development	Approved indications	References
BEZ-235	Novartis	Phase I, II; discontinued	Leukemia, lymphoma, multiple myeloma, adrenocortical, bladder, breast, colon, cholangiocarcinoma, endometrial, gastric, hepatocellular, lung, nasopharyngeal, ovarian, pancreatic, prostate, renal, thyroid cancer, gliomas, melanoma, non-functioning pituitary adenomas, osteosarcoma, rhabdomyosarcoma	Maira et al., 2008; Schnell et al., 2008; Serra et al., 2008; Brachmann et al., 2009; Cao et al., 2009; Liu et al., 2009; Marone et al., 2009; McMillin et al., 2009; Cho et al., 2010; Benjamin et al., 2011; Wander et al., 2011; Zhang et al., 2011; Hong et al., 2014; Bendell et al., 2015b; Salazar et al., 2015; Seront et al., 2016
BGT-226	Novartis	Phase I, II	Leukemia, lymphoma, multiple myeloma, breast, head and neck, hepatocellular, pancreatic cancer	Benjamin et al., 2011; Wander et al., 2011; Zhang et al., 2011; Markman et al., 2012
GDC-0980 (Apitolisib)	Genentech	Phase I, II	Non-Hodgkin's lymphoma, breast, endometrial, hepatocellular, lung, pancreatic, prostate, renal cancer, malignant pleural mesothelioma	Dolly et al., 2010; Benjamin et al., 2011; Wagner et al., 2011; Wallin et al., 2011; Wander et al., 2011; Zhang et al., 2011; Makker et al., 2014; Powles et al., 2014
GSK-2126458 (Omipalisib)	GlaxoSmithKline	Phase I	Lymphoma, breast nasopharyngeal, prostate cancer	Knight et al., 2010; Benjamin et al., 2011; Wander et al., 2011; Zhang et al., 2011; Liu et al., 2015; Munster et al., 2016
PF-04691502	Wyeth/Pfizer	Phase I, II	Leukemia, non-Hodgkin's lymphoma, bladder, breast, colon, endometrial, head and neck, hepatocellular, nasopharyngeal, ovarian cancer	Benjamin et al., 2011; Wander et al., 2011; Yuan et al., 2011; Wang F.-Z. et al., 2013; Britten et al., 2014; Chen et al., 2016
PI-103	Merck	Preclinical	Leukemia, hepatocellular, lung cancer, astrocytoma, chordomas, glioblastomia, melanoma, neuroblastoma, peripheral nerve sheath tumor	Park et al., 2008
PKI-587 (PF-05212384, Gedatolisib)	Wyeth/Pfizer	Phase I, II	Leukemia, breast, colon, head and neck, hepatocellular, lung, nasopharyngeal cancer, glioma	Benjamin et al., 2011; Mallon et al., 2011; Wander et al., 2011; Liu et al., 2015
XL-765 (SAR245409, Voxtalisib)	Exelixis Inc.	Phase I, II	Leukemia, lymphoma, breast, pancreatic, prostate cancer, gliomas, neuroblastoma, peripheral nerve sheath tumor, pituitary adenoma	Benjamin et al., 2011; Wander et al., 2011; Zhang et al., 2011; Papadopoulos et al., 2014; Yu et al., 2014; Papadopoulos et al., 2015; Gravina et al., 2016; Thijssen et al., 2016
VS-5584 (SB-2343)	Verastem Inc.	Phase I, II	Leukemia, lymphoma, breast, colon, gastric, ovarian, prostate cancer, melanoma, mesothelioma	Hart et al., 2013
WJD-008	–	Preclinical	Breast, colon, lung, prostate cancer, glioblastoma	Li et al., 2010; Zhou and Huang, 2012
SF-1126	Semafore	Phase I, II	Multiple myeloma, breast, prostate, neck, renal cancer, glioblastoma, neuroblastoma	Benjamin et al., 2011; Zhang et al., 2011; Mahadevan et al., 2012