Table 1 MDM2 inhibitors in development
From: Novel targeted therapeutics: inhibitors of MDM2, ALK and PARP
Chemical series | Therapeutics | Development stage |
|---|---|---|
Inhibitors of MDM2-p53 interaction by targeting to MDM2 | ||
Cis-imidazoline | RO5045337 (RG7112; Nutlin-3) | Phase I: Advanced solid tumors and hematological malignancy |
Benzodiazepinedione | TDP521252 & TDP665759 | Preclinical |
Spiro-oxindoles | MI-219, MI-319 & other MI compounds | Preclinical |
Isoquinolinone | PXN727 & PXN822 | Preclinical |
Inhibitor of MDM2-p53 interaction by targeting to p53 | ||
Thiophene | RITA (NSC 652287) | Preclinical |
E3 Ligase Inhibitors | ||
5-Deazaflavin | HLI98 compounds | Preclinical |
Tryptamine | JNJ-26854165 | Phase I: Advanced solid tumors |