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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). 

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.  

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.


Tumour shrinkage clinic.png

Treatment of MET exon 14 skipping mutant NSCLC patient with DO-1 resulted in significant tumour volume reduction and clinical benefit

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