Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.

By Qing-jie Ding, Zhuming Zhang, Jin-jun Liu, Nan Jiang, Jing Zhang, T. M. Ross, Xin-jie Chu, D. Bartkovitz, F. Podlaski, C. Janson and 7 more. 2013

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Synthetic Lethality of Combined Bcl-2 Inhibition and p53 Activation in AML: Mechanisms and Superior Antileukemic Efficacy (2017, background): “The recently developed RG7388 (RG, idasanutlin) is a second-generation MDM2 inhibitor with greater potency, selectivity, and bioavailability compared with its predecessors Nutlin-3a and RG7112 and is able to effectively activate p53 (Ding et al., 2013).”
Cellular Senescence: Aging, Cancer, and Injury. (2019, unknown): “This has led to the discovery of RG7112 (RO5045337) (332), the first MDM2 inhibitor to be advanced into phase I human clinical trials (13, 332) and others such as RG7388 (99), MI-77301 (338), MI888 (364), AMG-232 (307), AM-7209, DS-3032b (18), Serdemetan (JNJ-26854165), and the Nutlin family members”
Small-molecule inhibitors of protein-protein interactions: progressing toward the reality. (2014, methodology): “Roche recently disclosed Ro8994, a 5 nM (95% bioavailable) analog based on a spiroindolinone scaffold that combines features of RG7388 andMI-888 (Zhang et al., 2014).”
Targeting p53 pathways: mechanisms, structures and advances in therapy (2023, background): “RG7388: The MDM2 inhibitor RG7388, which was subsequently designed and synthesized, is a class of pyrrolidine derivatives.(344) RG7388, Kd = 0.”