JNJ-38877618 (OMO-1) is a potent, highly selective, orally bioavailable Met (c-Met) kinase inhibitor with binding affinity (Kd) of 1.4 nM and enzyme inhibitory activity against wt and M1268T mutant Met (c-Met) (2 and 3 nM IC50).
In vivo, OMO-1 induces complete inhibition of tumor growth in 3 models: the SNU5 MET amp gastric, U87-MG HGF autocrine glioblastoma and Hs746T MET exon 14 skipping mutant gastric cancer. Combination treatments are well tolerated and improve EGFR targeted therapy. Although single agent OMO-1 has no effect on NSCLC HCC827 EGFR, combination with Erlotinib leads to delayed onset of tumor recurrence[1].
[1] Marion Libouban, et al. AACR Cancer Res. 2018, 78(13 Suppl):Abstract nr 4791.