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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
  1. RITA, reactivation of p53 and induction of tumor cell apoptosis
  2. Reference; [23, 36, 37, 130132, 134139]