Format

Send to

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

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

Author information

1
Genitourinary Center, M.D. Anderson Cancer Centre, Houston, TX 77030, USA. johna@mdanderson.org

Abstract

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.

PMID:
20226597
PMCID:
PMC3940067
DOI:
10.1016/j.ctrv.2010.02.015
[Indexed for MEDLINE]
Free PMC Article

Supplemental Content

Full text links

Icon for Elsevier Science Icon for PubMed Central
Loading ...
Support Center