Promising proof of concept for small molecule modality to treat non-small cell lung cancer

Ichiro Kadawa et al., from the Department of Medicine of the University of Chicago, have published an article on a study into a new small molecule modality to treat non-small cell lung cancer (NSCLC). The findings, acquired with the Pamstation12, offer a robust preclinical proof of concept for dual targeting of the MET and RON kinases.

Lung cancer is a heterogeneous disease encompassing a wide array of genetic abnormalities. The kinase MET is altered in many lung cancers, especially non-small cell lung cancer (NSCLC). Clinical trials of MET inhibitors that are underway, show cases of resistance. There is evidence that the RON kinase can also be overexpressed in NSCLC. Therefore the researchers studied the effects of the dual inhibitor LY2801653, which targets both MET and RON.

Using the PamGene platform, the researchers found that inhibition of MET and RON was associated with decreased phosphorylation of three others kinases. LY2801653 decreased tumor growth in mouse xenograft models of lung cancer, dramatically inhibiting mitotic events and angiogenesis. Taken together, the results argued that specific targeting of the­ MET/RON kinases could provide robust inhibition of cell proliferation and tumor outgrowth in multiple in vitro and in vivo models of NSCLC.

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Dramatic antitumor effects of the MET/TON small-molecule inhibitor LY2801653 in non-small cell lung cancer

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