Definition

An orally bioavailable inhibitor of deoxycytidine kinase (dCK), with potential antineoplastic activity. Upon oral administration, dCK inhibitor TRE-515 targets, binds to and inhibits the activity of dCK, an enzyme that catalyzes the rate-limiting reaction in the deoxyribonucleoside salvage pathway in cancer cells. By inhibiting dCK, TRE-515 halts nucleotide synthesis and prevents the metabolism of DNA precursors in tumor cells. This inhibits DNA replication in and proliferation of cancer cells. dCK predominantly phosphorylates the deoxyribonucleoside deoxycytidine (dC) and converts dC into deoxycytidine monophosphate. It is upregulated in multiple tumor cell types in response to increased DNA synthesis needed for rapid cancer cell proliferation.