Skip to main content
. Author manuscript; available in PMC: 2011 Jul 24.
Published in final edited form as: Nat Rev Drug Discov. 2009 Aug;8(8):627–644. doi: 10.1038/nrd2926

Table 2. Summary of drugs targeting the PI3K pathway in clinical trials for cancer treatment*.

Cateogory Agent Target Sponsor Phase Cancer Type/Condition Chemical structure
PI3K Inhibitors BEZ235 Class I PI3K/mTOR Novartis Phase I/II Advanced solid tumors
Advanced Breast cancer		 graphic file with name nihms212276t1.jpg
BGT226 Class I PI3K/mTOR Novartis Phase I/II Solid tumors
Advanced breast cancer
Cowden syndrome		 ND
BKM120 Class I PI3K Novartis Phase I
(1st Qtr 2009)		 Solid tumors ND
XL765 Class I PI3K/mTOR Exelixis Phase I Solid tumors
Non-Small Cell Lung Cance
Malignant Gliomas		 graphic file with name nihms212276t2.jpg
XL147 Class I PI3K Exelixis Phase I Advanced solid tumors
Endometrial Carcinoma
Ovarian Carcinoma
Non-Small Cell Lung Cance		 graphic file with name nihms212276t3.jpg
GDC0941 Class I PI3K Genentech Phase I Advanced solid tumors
Non-Hodgkin's lymphoma		 graphic file with name nihms212276t4.jpg
SF1126 pan-PI3K/mTOR Semafore Phase 1 Advanced solid tumors graphic file with name nihms212276t5.jpg
GSK1059615 pan-PI3K GlaxoSmithKline Phase I Advanced solid tumors
Metastatic breast cancer
Endometrial cancer
Lymphoma		 ND
PX-866 PI3K (α, δ, and γ) Oncothyreon Phase 1 Advanced solid tumors graphic file with name nihms212276t6.jpg
CAL-101 PI3K (δ) Calistoga Phase I Chronic lymphocytic leukemia (CLL)
Acute myeloid leukemia (AML)
Non-Hodgkin's lymphoma		 ND
Akt Inhibitors Perifosine
(KRX-0401)		 AKT Keryx Phase I/II Advanced solid tumors
Multiple myeloma
Ovarian cancer
Soft Tissue sarcoma
Malignant melanoma		 graphic file with name nihms212276t7.jpg
MK2206 AKT Merck Phase I Advanced solid tumors graphic file with name nihms212276t8.jpg
VQD-002
(API-2/TCN)		 AKT VioQuest Phase I Hematologic malignancies
Leukemia
Non-small cell lung cancer		 graphic file with name nihms212276t9.jpg
XL418 AKT/ S6K Exelixis Phase I** Solid Tumors ND
mTOR Inhibitors Rapamycin
(Sirolimus, Rapamune®)		 mTORC1 Wyeth Phase I/II Advanced solid tumors
Metastatic breast cancer
Myeloid leukemia		 graphic file with name nihms212276t10.jpg
Approved Advanced renal cell carcinoma (RCC) graphic file with name nihms212276t11.jpg
CCI-779
(Temsirolimus,Torisel®)		 mTORC1 Wyeth Phase I/II/III Advanced solid tumors
Multiple myeloma
Ovarian cancer
Endometrial Cancer
Mantle cell lymphoma
Brain tumors
Non-small cell lung cancer
Malignant melanoma
Approved Advanced renal cell carcinoma (RCC) graphic file with name nihms212276t12a.jpg
graphic file with name nihms212276t12b.jpg
RAD001
(Everolimus, Afinitor®)		 mTORC1 Novartis Phase I/II/III Advanced solid tumors
Advanced Hepatocellular Carcinoma
Bladder Cancer
Head and Neck Cancer
Glioma/Astrocytoma
Advanced Prostate Cancer
Brain tumors
Advanced Gastric Cance
Metastatic Breast Cancer
Metastatic Pancreatic Cancer
Approved Soft-tisse and bone sarcomas graphic file with name nihms212276t13.jpg
AP23573
(Deforolimus,MK-8669)		 mTORC1 Merck/Ariad Phase I/II/III Advanced malignancies
Relapsed Hematologic Malignancies
Progressive Glioma
Endometrial Cancer
Metastatic Breast Cancer
Brain tumors
Non-small cell lung cancer
Prostate Cancer
AZD8055 mTORC1/mTORC2 AstraZeneca Phase I/II Advanced solid tumors
Endometrial Carcinoma
Lymphoma		 ND
OSI-027 mTORC1/mTORC2 OSI Phase I Solid tumor
Lymphoma		 ND
*

Information presented is compiled from company websites and from www.clinicaltrials.gov and www.fda.gov

**

The trial has been suspended due to low drug exposure.

ND, not disclosed