DO-1 is a highly selective small molecule inhibitor of the MET kinase that was found to inhibit the organic cation transporter-2 (OCT-2). 

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DO-1 (formerly JNJ-38877618 or OMO-1) was initially  tested in a healthy volunteer study where initial data on pharmacokinetics, food effect and safety were obtained by JNJ where it originated.   

The formation of a MET inactive metabolite that remained in circulation was noted in this study, but associated adverse events were not observed.

 

A phase 1/1b patient study carried out by OCTIMET, who licensed OMO-1 from JNJ,  led to the identification of a recommended Phase 2 Dose (250mg BID).  Promising signs of clinical activity were observed in MET exon 14 skipping patients as well tumour shrinkage in combination with an EGFR inhibitor (gefitinib) in a gefitinib resistant patient.  

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Preclinical data generated at DeuterOncology have shown that, in addition to MET target inhibition, DO-1 is able to induce vascular normalisation, reduce tumour acidification and increase DNA adduct formation in combination with chemotherapeutics such as gemcitabine and cisplatin.