. 2015 May 27;11(10):1711–1728. doi: 10.1080/15548627.2015.1043076

Table 3.

Examples of PtdIns3K and PI3K inhibitors, their status in clinical development and effects on autophagy

Selectivity	Name of the inhibitor	Molecular targets	Effects on on autophagy	Status in clinical trials	References
Pan-class	Wortmannin	PtdIns3K and PI3K enzymes, as well as PI3K-related kinases	Inhibition	Failed to enter clinical trial	^{26,72,175,177,178,181,190-192}
	LY294002	PtdIns3K and PI3K enzymes, as well as PI3K-related kinases	Dual effect: activation and inhibition	Failed to enter clinical trial	^{26,72,175,177}
	SF1126	PtdIns3K and PI3K enzymes, as well as PI3K-related kinases	Unknown	Phase I	^177,194-201
Class I-specific	PX-866	PIK3CA, PIK3CB, PIK3CD, PIK3CG	Activation	Phase I/II	National Cancer Institute (USA) http://www.cancer.gov/clinicaltrials/^24,202-211
	XL147	PIK3CA, PIK3CB, PIK3CD, PIK3CG	Activation	Phase I/II	^24,212-219
	BKM120	PIK3CA, PIK3CB, PIK3CD, PIK3CG	Activation	Phase I/ II/III	National Cancer Institute (USA) http://www.cancer.gov/clinicaltrials/^{24,26,220-224}
	BAY80–6946	PIK3CA, PIK3CB	Unknown	Phase I/ II	National Cancer Institute (USA) http://www.cancer.gov/clinicaltrials/^24,26,225
Dual PI3K and MTOR	NVP-BGT226	PIK3CA, PIK3CB, PIK3CD, PIK3CG, MTOR	Activation	Phase I/ II	^{24,173,182,226,227}
	BEZ235	PIK3CA, PIK3CB, PIK3CD, PIK3CG, MTOR	Activation	Phase I/ II	National Cancer Institute (USA) http://www.cancer.gov/clinicaltrials/^24,228-233
	XL765	PIK3CA, PIK3CB, PIK3CD, PIK3CG, MTOR	Activation	Phase I/ II	National Cancer Institute (USA) http://www.cancer.gov/clinicaltrials/^24,234-238
Class I-Isoform specific	BYL719	PIK3CA	Unknown	Phase I/ II	National Cancer Institute (USA) http://www.cancer.gov/clinicaltrials/
	INK1117	PIK3CA	Unknown	Phase I	National Cancer Institute (USA) http://www.cancer.gov/clinicaltrials/
	GSK2636771	PIK3CB	Unknown	Phase I/II	National Cancer Institute (USA) http://www.cancer.gov/clinicaltrials/
	SAR260301	PIK3CB	Unknown	Phase I	¹⁷³
	IPI-145	PIK3CG, PIK3CD	Unknown	Phase I/ II/ III	National Cancer Institute (USA) http://www.cancer.gov/clinicaltrials/²³⁹
	GDC-0941	PIK3CA, PIK3CD	Activation	Phase I/ II	National Cancer Institute (USA) http://www.cancer.gov/clinicaltrials/^{175,219,240-244}
	GS-1101	PIK3CD	Unknown	Phase I/ II/ III	National Cancer Institute (USA) http://www.cancer.gov/clinicaltrials/^245–251
Class III-specific	Compound 31((2S)8-[(3R)3-Methylmorpholin-4-yl]-1-(3-methyl-2-oxobutyl)-2-(trifluoromethyl)-3,4-dihydro2H-pyrimido[1,2α]pyrimidin-6-one)	PIK3C3	Unknown	NA	¹⁸⁶
	PIK-III	PIK3C3	Inhibition	NA	¹⁸⁵
	SAR405	PIK3C3	Inhibition	NA	¹⁸³
	VPS34-IN1	PIK3C3	Unknown	NA	¹⁸⁴

NA: Not available.