Improving Response Rates to EGFR-Targeted Therapies for Head and Neck Squamous Cell Carcinoma: Candidate Predictive Biomarkers and Combination Treatment with Src Inhibitors

Table 3

Src-targeting agents in clinical development.

Agent		Sponsor	Target(s)	SFKs targeted (IC50)	Target site	Irreversible	Solid cancers in phase II or III clinical study*	FDA approval (Date)	SCCHN clinical trial phase
Dasatinib	BMS-354825	Bristol-Myers Squibb	Src; Abl; c-Kit; PDGFR; others		ATP-binding	No	SCLC, NSCLC, breast, colorectal, head and neck, liver, melanoma, ovarian, pancreatic, sarcoma	Chronic myeloid leukemia (June 2006)	II
AZD0530		AstraZeneca	Src; Abl		ATP-binding	No	SCLC, NSCLC, breast, colorectal, head and neck, melanoma, osteosarcoma, ovarian, pancreatic, prostate	—	II
Bosutinib	SKI-606	Wyeth	Src; Abl		ATP-binding	No	Breast	—	—
KX01	KX2-391	Kinex	Src		Peptide-binding	No	(phase I)	—	—
XL999		Exelixis	Src, VEGFR, PDGFR, FGFR, FLT-3, others		ATP-binding	No	NSCLC, colorectal, kidney, ovarian	—	—

* ClinicalTrials.gov solid tumors.