Drug intelligence / Profile preview

DBPR728

Development stage
Preclinical
Lead developer
Institute of Biotechnology and Pharmaceutical Research
Modality
Small Molecules
Administration
Oral
01

Overview

DBPR728 is a small molecule prodrug of the dual MYCN/AURKA inhibitor 6K465, developed by the National Health Research Institutes (NHRI) in Taiwan. It is designed to treat high-risk pediatric cancers, specifically neuroblastoma and Ewing's sarcoma, which are characterized by the co-overexpression of MYCN and Aurora Kinase A (AURKA). In these tumors, AURKA interacts with and stabilizes the MYCN protein, preventing its degradation and driving malignancy. DBPR728 disrupts this interaction, leading to MYCN degradation and tumor growth inhibition. In preclinical SK-N-BE(2) neuroblastoma xenograft models, DBPR728 demonstrated superior and more durable tumor suppression compared to the selective AURKA inhibitor alisertib.

02

Targets

AURKA (Aurora kinase A)AURKB (Aurora kinase B)

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