DO-2 is a deuterated small molecule kinase inhibitor.
Deuteration is well known to modulate the metabolic characteristics of small molecule drugs. The primary human metabolic path of the non deuterated parent molecule results in the formation of an inactive metabolite.
Deuteration results in an alternative metabolic path for DO-2 that results in an active metabolite that has additional activity on a kinase that is downstream of RAS.
We have observed increased parent drug, and this active metabolite, exposures resulting in DO-2 demonstrating highly potent in vivo activity, with very low doses causing tumour regression.
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