Table 2 PI3K inhibitors in clinical trials

Idelalisib (CAL-101)

p110-δ

CLL/SLL, iNHL, MCL

Pyrexia, nausea, decrease appetite, fatigue

III

[76, 77, 80, 83, 86, 88–90]

Buparlisib (BKM-120)

p110-α,-β, -δ,-γ

Breast, GBM, NSCLC

Rash, hyperglycemia diarrhea, anorexia

IB/II

[103–109]

GDC-0941

p110-α,-β, -δ,-γ

Breast, NSCLC, melanoma endometrial, pancreatic

Nausea, diarrhea, rash vomiting, anorexia

IB/II

[117–123]

PX-866

p110-α,-β, -δ,-γ

Ovarian, prostate, GBM NSCLC

Fatigue, diarrhea thromboembolism

II

[126–129]

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

[135–137]

IPI-145

p110-δ,-γ

CLL/SLL, iNHL, MCL

Cytopenias liver enzyme elevations

I

[138, 139]

BEZ-235

p110-α,-β, -δ,-γ/mTOR

Breast, GBM

Mucositis

IB/II

[149–152]

BYL-719

p110-α

Breast, cervical, endometrial ovarian, H&N

Nausea, diarrhea hyperglycemia, vomiting

IB/II

[153–155]

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

[167, 168]

GSK-2126458

p110-α,-β, -δ,-γ/mTOR

RCC, bladder

Nausea, vomiting diarrhea

I

[169, 170]

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

[176–178]

XL-147

p110-α,-β, -δ,-γ

Solid tumor, GBM

Nausea, vomiting diarrhea

I/II

[180–183]