Clinical development of Src tyrosine kinase inhibitors in lung cancer

Src tyrosine kinases regulate a large number of. important mechanisms in normal and cancerous cells, are overexpressed in a broad range or tumors including lung cancer, and thus represent a potential target for cancer therapy. Preclinical experiments indicate that small-molecule inhibitors of Src block tumor growth, metastasis, and angiogenesis. Phase I data from healthy volunteers also suggest that inhibitors of Src prevent bone resorption. Several phase 11 trials with small-molecule inhibitors of Src are under way or have been initiated in lung cancer and in other malignancies, as discussed herein.