This week in therapeutics

Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Cancer

Sarcoma

Focal adhesion kinase (FAK)

Cell culture and mouse studies suggest inhibiting FAK could help treat Ewing's sarcoma. In Ewing's sarcoma cell lines, a small molecule FAK inhibitor blocked cell viability with an average IC50 value of 2.4 mM. In a mouse model for Ewing's sarcoma, small hairpin RNA or a small molecule inhibitor against FAK decreased tumor growth compared with control shRNA or vehicle. Next steps include testing FAK inhibitors in combination with other therapies and examining the role of FAK in metastasis.
CureFAKtor Pharmaceuticals LLC's CFAK-C4, a FAK and VEGF receptor 3 (FLT4; VEGFR-3) inhibitor, is in preclinical development for pancreatic cancer.
Verastem Inc.'s VS-6063, a FAK inhibitor in-licensed from Pfizer Inc., is in Phase I testing to treat ovarian cancer. Verastem's VS-4718, a FAK inhibitor in-licensed from Poniard Pharmaceuticals Inc., is in preclinical development to treat cancer.

SciBX 6(14); doi:10.1038/scibx.2013.337
Published online April 11, 2013

Unpatented; licensing status not applicable

Crompton, B.D. et al. Cancer Res.; published online March 27, 2013;
doi:10.1158/0008-5472.CAN-12-1944
Contact: Kimberly Stegmaier, Dana-Farber Cancer Institute, Boston, Mass.
e-mail:
kimberly_stegmaier@dfci.harvard.edu