Src tyrosine kinase inhibitors in the treatment of lung cancer: rationale and clinical data

Author(s): Sacha I Rothschild,Oliver Gautschi

Src-family kinases have an important role in many oncologic functions in human cancers, including proliferation, motility, migration, survival and angiogenesis. Several Src inhibitors have been developed, of which dasatinib has been most explored in the clinic. Preclinical studies in a wide variety of solid tumor cell lines have shown that dasatinib acts as a cytostatic agent, inhibiting the processes of cell proliferation, invasion and metastasis. In particular, in preclinical studies, an interaction between Src-family kinases inhibition and cell survival has been noted in EGFR-dependent non-small-cell lung cancer cell lines. Src tyrosine kinase inhibitors in clinical trials have shown a favorable safety profile and moderate anticancer activity in unselected patient populations. Future trials will continue to explore the contribution of Src inhibition in combination with chemotherapy and other targeted agents.