Table 3 Summary of clinical activity of phosphatidylinositol 3-kinase (PI3K) inhibitors in phase I clinical trials

Pan-isoform PI3K inhibitors

SAR245408 (XL147)

75

No

NSCLC

No alteration

[6]

BKM120

66

No (expansion only)

TN breast

KRAS mutation

[7]

ER+ HER2- breast

PIK3CA mutation

Parotid cancer

PIK3CA mutation

GDC-0941

Once a day

42

No

Melanoma

BRAF V600E mutation

[8]

Once a day or twice a day

97

No

ER+, HER2- breast

Unknown

[9]

Endocervical adenocarcinoma

PIK3CA mutation

BAY 80-9646

Dose escalation

17

No

None

-

[10]

Expansion: solid

30

No

ER+ HER2- Breast

No alteration

[11]

ER+ HER2+ Breast

HER2 amplification

Expansion: NHL

5

No

Follicular lymphoma (5 patients)

No alteration (0 of 5 patients)

[11]

CH5132799

31

No

None

-^a

[12]

PX-866

84^b

No

None

-

[13]

Pan-isoform PI3K-mTOR inhibitors

SAR245409 (XL765)

Solid tumors

83

No

None

-

[14]

Lymphoma

16

No

Mantle cell lymphoma

Unknown

[15]

Transformed lymphoma

Unknown

Diffuse large B-cell lymphoma

Unknown

BEZ235

Once a day

59^c

No (expansion only)

ER+ HER2- breast

Unknown

[16]

NSCLC

PTEN mutation (Cowden)

Twice a day

16

No

None

-

[17]

GSK2126458

129

No (expansion only)

Renal

No alteration

[18]

Renal

PTEN loss

Bladder

PIK3CA mutation

Bladder

Unknown

GDC-0980

42

No

Adrenal cortical

Unknown

[19]

32

No

None

-

[20]

SF-1126

39

No

None

-

[21]

PF-04691502

33

No

None

-

[22]

PF-05212384

53

No (expansion only)

Ovarian cancer

No alteration

[23]

NSCLC

EGFR mutation

BGT-226

57

No

None

-

[24]

PI3Kα-specific inhibitors

BYL719

35

Yes

ER+ breast

PIK3CA mutation

[25]

Cervix

PIK3CA mutation

Colon

PIK3CA and KRAS mutations

PI3Kδ-specific inhibitors

GS-1101

CLL

54

No

26% RR according to IWCLL

Unknown

[26]

Non-Hodgkin's lymphoma

49

No

Indolent NHL (15 PR out of 24); mantle cell lymphoma (10 PR out of 16)

Unknown

[27]