1313365-95-5Relevant articles and documents
Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors
Holzer, Philipp,Masuya, Keiichi,Furet, Pascal,Kallen, Joerg,Valat-Stachyra, Therese,Ferretti, Stéphane,Berghausen, Joerg,Bouisset-Leonard, Michèle,Buschmann, Nicole,Pissot-Soldermann, Carole,Rynn, Caroline,Ruetz, Stephan,Stutz, Stefan,Chène, Patrick,Jeay, Sébastien,Gessier, Francois
supporting information, p. 6348 - 6358 (2015/09/07)
(Figure Presented). As a result of our efforts to discover novel p53:MDM2 protein-protein interaction inhibitors useful for treating cancer, the potent and selective MDM2 inhibitor NVP-CGM097 (1) with an excellent in vivo profile was selected as a clinical candidate and is currently in phase 1 clinical development. This article provides an overview of the discovery of this new clinical p53:MDM2 inhibitor. The following aspects are addressed: mechanism of action, scientific rationale, binding mode, medicinal chemistry, pharmacokinetic and pharmacodynamic properties, and in vivo pharmacology/toxicology in preclinical species.