Table 1.
MDM2 inhibitors in development
| 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 |