DP226

DP226 is a highly potent, orally bioavailable small molecule inhibitor of Polo-like kinase 1 (PLK1), developed by DP Technology. It was discovered and optimized using the RiDYMO platform, which enabled significant improvements in activity and pharmacokinetic properties over earlier compounds in its class. In preclinical studies, DP226 demonstrated an in vitro PLK1 inhibitory activity of 0.19 nM—nearly 300-fold more potent than its predecessor DP101—and showed superior oral bioavailability (76.8%) compared to PCM075 (24%). At low doses, it exhibited stronger anti-tumor effects than PCM075 and induced tumor regression when combined with bevacizumab, suggesting potential as a candidate for further development as an anti-cancer agent[2][1].