Table 1.

PI3K inhibitors tested in preclinical and clinical models, genetic determinants of response, and open clinical trials described for each compound.

Group	Selectivity	Compound	Cancer type	Genetic determinant of response	Clinical trial status
I Pan-class I	Class I PI3K	GDC-0941 (Roche/Genentech)	Breast	HER-2 amplification PIK3CA mutations	I-II in breast, non-Hodgkin’s lymphoma, NSCLC
			Melanomas, MM, non-Hodgkin’s lymphoma, NSCLC, ovarian	–
		BKM120 (Novartis)	Breast	PIK3CA mutations	I-II in breast CRC, endometrial, GIST, GBM, leukemia, melanoma, NSCLC, pancreatic, renal cell, SCCHN, TCC
			CRC, endometrial, GIST, GBM, leukemia, melanoma, NSCLC, pancreatic prostate	–
		PX866 (Oncothyreon)	Breast, CRC, MM, NSCLC, pancreatic prostate, ovarian	PIK3CA mutation, PTEN loss	I-II in CRC, GBM, NSCLC, SCCHN
		BAY 80-6946 (Bayer)	Advanced solid cancers	PIK3CA mutations	I-II in advanced solid cancers
II Isoform specific	PI3Kα	GDC-0032 (Roche/Genentech)	Solid cancers	–	I-II in solid cancers
	PI3Kβ	GSK2636771 (GlaxoSmithKline)	Advanced solid cancers	–	I-IIa in advanced solid cancers with PTEN deficiency
	PI3Kγ and PI3Kδ	IPI-145 (Infinity)	Hematological malignancies	–	I-IIa in advanced hematological malignancies
	PI3Kδ	CAL-101 (Gilead Sciences)	AML, CLL, Hodgkin’s and non-Hodgkin’s lymphoma, MCL	–	I-II-III in AML, CLL, Hodgkin’s and non-Hodgkin’s lymphoma, MCL, MM
III Dual PI3K/mTOR	PI3K and mTOR	BEZ235 (Novartis)	Breast	PIK3C2a mutation, HER-2 amplification, PTEN loss	I-II in breast, renal cell
			Ovarian	PIK3C2a mutation, PTEN loss