Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Cancer

Melanoma

BRAF; neuroblastoma Ras viral (v-Ras) oncogene (NRAS)

In vitro and mouse studies have identified a pan-Raf kinase inhibitor that could help treat BRAF- or NRAS-mutant melanoma. In binding studies, the inhibitor TAK-632 bound BRAF with an IC50 of about 2.4 nM and with 67-fold selectivity over VEGF receptor 2 (KDR/Flk-1; VEGFR-2). In two mouse xenograft models of melanoma, TAK-632 decreased tumor volume compared with vehicle. Next steps include studying the compound in additional mutant NRAS cell lines to help determine the optimal indication for clinical testing.

SciBX 6(38); doi:10.1038/scibx.2013.1061
Published online Oct. 3, 2013

Patent filed by Takeda Pharmaceutical Co. Ltd.; licensing status undisclosed

Okaniwa, M. et al. J. Med. Chem.; published online Aug. 1, 2013;
doi:10.1021/jm400778d
Contact: Tomoyasu Ishikawa, Takeda Pharmaceutical Co. Ltd., Kanagawa, Japan
e-mail:
tomoyasu.ishikawa@takeda.com

Contact: Masaaki Hirose, same affiliation as above
e-mail:
masaaki.hirose@takeda.com

Contact: Masanori Okaniwa, same affiliation as above
e-mail:
masanori.okaniwa@takeda.com