DBPR728 is an acyl prodrug of 6K465 that carries fewer drogen bond donors. 6K465 acts as an Aurora kinase inhibitor that destabilizes MYC family cancer proteins and has antitumor efficacy. DBPR728 has the potential to inhibit cancers that overexpress C-MYC and N-MYC, with a 10-fold increase in oral bioavailability compared to 6K465.
References:
[1]. Chang C P, et al. Discovery of a long half-life AURKA inhibitor to treat MYC-amplified solid tumors as a monotherapy and in combination with everolimus[J]. Molecular Cancer Therapeutics, 2024: OF1-OF14.