HMN-214 (IVX-214) is a potent inhibitor of Polo-like kinase (Plk)1 with IC50 of 118 nM. The in vitro data may be similar to that of HMN-176, which is active metabolite of HMN-214.
In vivo
HMN-214 has a potent antitumor activity in mouse xenograft models. When administered p.o., HMN-214 suppressed the expression of MDR1 mRNA in a mouse xenograft model implanted with KB-A.1, an Adriamycin-resistant cell line. HMN-214 is an oral prodrug because of the poor oral absorption of HMN-176 itself. The antitumor activity of HMN-214 against human tumor xenografts was equal or superior to that of clinically available agents, including cis-platinum, adriamycin, vincristine, and UFT without severe toxicity such as neurotoxicity. The maximum tolerated dose of HMN-214 when administered is 8 mg/m2/d.