1.Phase I and pharmacological study of the broad-spectrum tyrosine kinase inhibitor JNJ-26483327 in patients with advanced solid tumours.
Konings IR1, de Jonge MJ, Burger H, van der Gaast A, van Beijsterveldt LE, Winkler H, Verweij J, Yuan Z, Hellemans P, Eskens FA. Br J Cancer. 2010 Sep 28;103(7):987-92. doi: 10.1038/sj.bjc.6605867. Epub 2010 Sep 7.
BACKGROUND: JNJ-26483327 is an oral, potent, multi-targeted tyrosine kinase inhibitor, inhibiting kinases of epidermal growth factor receptor (EGFR)-1, -2 and -4, rearranged during transfection (RET) receptor, vascular endothelial growth factor receptor (VEGFR)-3 and Src family (Lyn, Fyn, Yes) at low nanomolar concentrations. This phase I, accelerated titration study assessed maximum tolerated dose, safety, pharmacokinetics and pharmacodynamic effects of JNJ-26483327.