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. 2021 Dec 16;6:425. doi: 10.1038/s41392-021-00828-5

Table 2.

Novel agents targeting PI3K signaling in cancer

Class Inhibitor Phase Toxic effects Reference
Pan‑PI3K inhibitors GDC-0941 I Neutropenia、Neuropsychiatric effects (confusion, depression, anxiety)、Hepatotoxicity、Diarrhea 254
BKM-120 II Hyperglycemia 255
BAY-80-6946 Approved

Nausea

High blood sugar

256
XL-147 I Rash 257
PX-866 II

Diarrhea

ALT/AST elevation

258
Isoform-selective PI3K inhibitors BYL-719 I Hyperglycemia 259
GDC-0032 I Rash、Diarrhea、Pneumonitis 206
IPI-145 Approved Hyperglycemia、Rash、Diarrhea、Hypertension 260
SAR-260301 Preclinical Nausea、Vomiting、Diarrhea 261
MLN-1117 I Nausea 262
Dual pan‑PI3K and mTOR inhibitors BEZ-235 I/II Fatigue/asthenia、Thrombocytopenia 263
SF-1126 I/II Hyperglycemia 264
GDC-0980 I

Maculopapular rash

Symptomatic hyperglycemia

265
PF-04691502 II

Fatigue

Loss of appetite、Nausea、High blood sugar、Rash、Vomiting

266
XL-765 I Stomatitis 267
GSK-2126458 I Diarrhea 268
PF-05212384 II Fatigue 266
GSK-1059615 Preclinical Immunosuppression 269
BGT-226 I/II

Diarrhea

Nausea

Loss of appetite

Vomiting

Fatigue

270