. Author manuscript; available in PMC: 2021 Nov 1.

Published in final edited form as: Drugs. 2020 Nov;80(16):1685–1697. doi: 10.1007/s40265-020-01394-w

Table 1:

Classes of PI3K Pathway Inhibitors

Class	Drug Target(s)	Drugs	Common Toxicities by Class
mTORC1 (mammalian target of rapamycin complex 1) inhibitors	mTORC1 kinase	Everolimus Temsirolimus Deforolimus	Stomatitis Rash Pneumonitis Hyperglycemia Immunosuppression
mTORC1/mTORC2 inhibitors	mTORC1/mTORC2 kinases	Sapanisertib (TAK-228) AZD2014	Hyperglycemia Rash Stomatitis Diarrhea
Pan-pi3k inhibitors	All class ia pi3kS	Buparlisib (BKM120) Pilaralisib (XL147) Pictilisib (GDC-0941) GDC-0084	Hyperglycemia Rash Neutropenia Neuropsychiatric effects (confusion, depression, anxiety) Hepatotoxicity Diarrhea
Pan-Akt inhibitors	Three isoforms of Akt (Akt1, 2, and 3)	Capivasertib (AZD5363) Ipatasertib (GDC0068) MK2206	Rash Hyperglycemia
Dual pi3k and mTOR inhibitors	p110 subunit of pi3k and mTOR	Dactolisib (BEZ235) Voxtalisib (XL765) Gedatolisib Bimiralisib (PQR309)	Stomatitis Hyperglycemia Immunosuppression
Isoform-specific pi3k inhibitors	pi3k p110α isoform	Alpelisib(BYL719) Taselisib (GDC-0032) Serabelisib (MLN1117) MEN1611 GDC-0077	Hyperglycemia Rash Diarrhea Pneumonitis
	pi3k p110δ isoform	Idelalisib (CAL-101) Duvelisib (IPI-145)	Hyperglycemia Rash Diarrhea Hypertension
	pi3k p110α and p110δ isoforms	Copanlisib	Hyperglycemia Hypertension Diarrhea Neutropenia