From: Phosphatidylinositol 3-kinase (PI3K) inhibitors as cancer therapeutics
Drug | Target(s) | Tumors | Toxicities | Clinical trials | References |
---|---|---|---|---|---|
Idelalisib (CAL-101) | p110-δ | CLL/SLL, iNHL, MCL | Pyrexia, nausea, decrease appetite, fatigue | III | |
Buparlisib (BKM-120) | p110-α,-β, -δ,-γ | Breast, GBM, NSCLC | Rash, hyperglycemia diarrhea, anorexia | IB/II | |
GDC-0941 | p110-α,-β, -δ,-γ | Breast, NSCLC, melanoma endometrial, pancreatic | Nausea, diarrhea, rash vomiting, anorexia | IB/II | |
PX-866 | p110-α,-β, -δ,-γ | Ovarian, prostate, GBM NSCLC | Fatigue, diarrhea thromboembolism | II | |
GDC-0032 | p110-α, -δ,-γ | Breast, NSCLC | Diarrhea, hyperglycemia fatigue, nausea, decreased appetite | I | [132] |
BAY 80-6946 | p110-α,-β | NHL, esophageal, sarcoma pancreatic | Alopecia, dysgeusia anemia, mucositis | I | |
IPI-145 | p110-δ,-γ | CLL/SLL, iNHL, MCL | Cytopenias liver enzyme elevations | I | |
BEZ-235 | p110-α,-β, -δ,-γ/mTOR | Breast, GBM | Mucositis | IB/II | |
BYL-719 | p110-α | Breast, cervical, endometrial ovarian, H&N | Nausea, diarrhea hyperglycemia, vomiting | IB/II | |
BGT-226 | p110-α,-β, -δ,-γ/mTOR | Solid tumors, breast | Nausea, vomiting diarrhea | I/II | [156] |
PF-04691502 | p110-α,-β, -δ,-γ/mTOR | Endometrial | Fatigue, nausea, vomiting decreased appetite, rash | II | [162] |
GDC-0980 | p110-α,-β, -δ,-γ/mTOR | Prostate | Hyperglycemia, rash mucositis | IB/II | |
GSK-2126458 | p110-α,-β, -δ,-γ/mTOR | RCC, bladder | Nausea, vomiting diarrhea | I | |
PF-05212384 | p110-α,-γ/mTOR | Solid tumor, CRC | Rash, mucositis transaminitis, hyperglycemia | II | [172] |
XL-765 | p110-α,-β, -δ,-γ/mTOR | NSCLC, gliomas | Nausea, diarrhea elevated liver enzymes | IB/II | |
XL-147 | p110-α,-β, -δ,-γ | Solid tumor, GBM | Nausea, vomiting diarrhea | I/II |