Dasatinib: a potent SRC inhibitor in clinical development for the treatment of solid tumors

Cancer Treat Rev. 2010 Oct;36(6):492-500. doi: 10.1016/j.ctrv.2010.02.015. Epub 2010 Mar 11.


SRC is a tyrosine kinase that plays a role in oncogenic, invasive and bone-metastatic processes. It has therefore been prioritized as a candidate therapeutic target in patients with solid tumors. Several SRC inhibitors are now in development, of which dasatinib has been most explored. Preclinical studies in a wide variety of solid tumor cell lines, including prostate, breast and glioma, have shown that that dasatinib acts as a cytostatic agent, inhibiting the processes of cell proliferation, invasion and metastasis. Dasatinib also inhibits the activity of osteoclasts, which have a major role in the development of metastatic bone lesions. Dasatinib has additive or synergistic activity in combination with a number of other agents, including cytotoxic agents and targeted therapies, providing a rationale for combination treatment in a clinical setting. Emerging clinical data with dasatinib support experimental observations, with preliminary phase 1 and 2 data demonstrating activity, both as a single agent and as combination therapy, in a range of solid tumors. Future clinical trials will further assess the clinical value of SRC inhibition with dasatinib.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Clinical Trials as Topic
  • Dasatinib
  • Humans
  • Neoplasms / drug therapy*
  • Protein Kinase Inhibitors / pharmacology
  • Pyrimidines / pharmacology*
  • Thiazoles / pharmacology*
  • src-Family Kinases / antagonists & inhibitors*
  • src-Family Kinases / drug effects


  • Antineoplastic Agents
  • Protein Kinase Inhibitors
  • Pyrimidines
  • Thiazoles
  • src-Family Kinases
  • Dasatinib