Src is a non-receptor tyrosine kinase that is deregulated in many types of cancer. Decades of research have revealed the crucial role of Src in many aspects of tumor development, including proliferation, survival, adhesion, migration, invasion and, most importantly, metastasis, in multiple tumor types. Despite extensive preclinical evidence that warrants targeting Src as a promising therapeutic approach for cancer, Src inhibitor(s) showed only minimal therapeutic activity in various types of solid tumors when used as a single agent in recent early-phase clinical trials. In this review, we highlight the most recent advances from preclinical studies and clinical trials that shed light on potential clinical use of Src inhibitor-containing combinatorial regimens in overcoming resistance to current anticancer therapies and in preventing metastatic recurrence.
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