Cover Story: Pre-EMP-tive strike against GBM

Table 1. EMP2's downstream crowd. University of California, Los Angeles researchers have shown that in mouse models of glioblastoma multiforme (GBM) and breast cancer, epithelial membrane protein 2 (EMP2) activates the integrin avb3 (CD51/CD61)-focal adhesion kinase (FAK)-Src signaling pathway that drives cancer progression.1 At least 16 companies have therapies on the market or in the clinic that target 1 of the 3 downstream components on that signaling pathway to treat cancer.

Source: BCIQ: BioCentury Online Intelligence





Bristol-Myers Squibb Co. (NYSE:BMY)/Otsuka Pharmaceutical Co. Ltd.

Sprycel dasatinib

Small molecule inhibitor of BCR-ABL tyrosine kinase and Src kinase

Marketed for acute lymphoblastic leukemia (ALL) and chronic myelogenous leukemia (CML); Phase II for breast and pancreatic cancers; Phase I for relapsed or refractory leukemia

Pfizer Inc. (NYSE:PFE)/Avillion LLP

Bosulif bosutinib
(PF-05208763; SKI-606)

Dual inhibitor of BCR-ABL and Src kinases

Marketed for CML

Merck KGaA (Xetra:MRK)

Cilengitide (EMD 121974)

Inhibitor of CD51/CD61 and integrin avb5

Phase III for brain cancer; Phase II for head and neck cancer, non-small cell lung cancer (NSCLC) and melanoma

Bristol-Myers Squibb/Johnson & Johnson (NYSE:JNJ)

Intetumumab (BGB-101; CNTO-95)

Human mAb targeting CD51/CD61, integrin avb5, integrin avb6 and integrin avb1 (CD51/CD29)

Phase II for melanoma and castration-resistant prostate cancer (CRPC); Phase I for solid tumors

Kinex Pharmaceuticals LLC/Hanmi Pharmaceutical Co. Ltd. (KOSDAQ:128940)

KX01 (KX2-391)

Small molecule, non-ATP Src inhibitor

Phase II for prostate cancer; Phase
I/II for breast cancer, gastric cancer and solid tumors; Phase Ib for acute myelogenous leukemia (AML)

Pfizer/Verastem Inc. (NASDAQ:VSTM)

Defactinib (VS-6063; formerly PF-4554878)

Inhibitor of FAK targeting cancer stem cells

Phase II for mesothelioma and NSCLC; Phase I for ovarian cancer and solid tumors

Tactic Pharma LLC


Inhibitor of CD51/CD61 and integrin a5b1

Phase II for brain cancer; Phase I for head and neck cancer

BioAlliance Pharma S.A. (Euronext:BIO)

AMEP (BA-015)

Plasmid encoding a peptide targeting CD51/CD61 and integrin a5b1

Phase I/II for melanoma

Nippon Shinyaku Co. Ltd. (Tokyo:4516)


Inhibitor of Src and Janus kinase-2 (JAK-2)

Phase I/II for hematologic malignancies



Inhibitor of FAK targeting cancer stem cells

Phase I for solid tumors

AstraZeneca plc (LSE:AZN; NYSE:AZN)


Src inhibitor

Phase I for advanced solid tumors

GlaxoSmithKline plc (LSE:GSK; NYSE:GSK)


Small molecule FAK inhibitor

Phase I for solid tumors

Teva Pharmaceutical Industries Ltd. (NYSE:TEVA)


Inhibitor of FAK and anaplastic lymphoma kinase (ALK)

Phase I for solid tumors

ValiRx plc (LSE:VAL)


Src inhibitor

Phase I for CRPC and other cancers