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TDP665759 is an inhibitor of the Hdm2:p53 complex. It acts by suppressing human tumor cell proliferation in vitro and sensitizing tumors to doxorubicin in vivo.

TDP-665759 is an inhibitor for HDm2:p53 complex, and thus activates p53, inhibits STAT3 signaling pathway (EC50 of 5.90 μM) and the cell viability of p53 expressing A549R (IC50 of 7.02 μM). TDP-665759 induces apoptosis in HepG2. TDP-665759 exhibits antitumor efficacy in mouse models[1].

[1] Koblish HK, et al. Benzodiazepinedione inhibitors of the Hdm2:p53 complex suppress human tumor cell proliferation in vitro and sensitize tumors to doxorubicin in vivo. Mol Cancer Ther. 2006 Jan;5(1):160-9. DOI:10.1158/1535-7163.MCT-05-0199