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Discovery of NVP-CGM097 - a highly potent and selective MDM2 inhibitor undergoing phase 1 clinical trials in p53wt tumors

Holzer, Philipp and Masuya, Keiichi and Furet, Pascal and Kallen, Joerg and Valat, Therese-Marie and Ferretti, Stephane Raymond and Berghausen, Joerg and Bouisset-Leonard, Michele and Buschmann, Nicole and Pissot Soldermann, Carole and Rynn, Caroline and Ruetz, Stephan and Stutz, Stefan and Chene, Patrick and Jeay, Sebastien and Gessier, Francois (2015) Discovery of NVP-CGM097 - a highly potent and selective MDM2 inhibitor undergoing phase 1 clinical trials in p53wt tumors. Journal of Medicinal Chemistry, 58 (16). pp. 6348-6358.

Abstract

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.

Item Type: Article
Date Deposited: 13 Oct 2015 13:11
Last Modified: 13 Oct 2015 13:11
URI: https://oak.novartis.com/id/eprint/25927

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