Discovery of AMG 232, a potent, selective, and orally bioavailable MDM2-p53 inhibitor in clinical development.

By Daqing Sun, Zhihong Li, Y. Rew, Michael W. Gribble, M. Bartberger, Hilary P. Beck, J. Canon, Ada Chen, Xiaoqi Chen, D. Chow and 40 more. 2014

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Molecular Docking and Structure-Based Drug Design Strategies (2015, background): “…strategy in drug design has been challenged by recent successful cases, such as the development AMG-232, a MDM2-p53 inhibitor, currently in Phase II clinical trials for cancer therapy [117]; and maraviroc (Selzentry ® ), a commercially available CCR5-gp120 inhibitor used in AIDS treatment [118].”
Targeting p53 pathways: mechanisms, structures and advances in therapy (2023, background): “Meanwhile, the imidazole group of His96 formed π-π stacking interactions with the C5 aryl group and formed hydrogen bonds with carboxylate.(342) In addition, the isopropyl group extends into the “cleft” of Gly58, forming CH·O-type interactions with Gly58 and enhancing contacts with nearby hydrophobi”
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”
Genomic Classification of Cutaneous Melanoma (2015, background): “Such agents may also be beneficial for patients with wild-type TP53 across the genetic subtypes (Frederick et al., 2014; Ji et al., 2013; Sun et al., 2014).”