2. Academic Validation
  3. Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors

Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors

  • J Med Chem. 2015 Aug 27;58(16):6348-58. doi: 10.1021/acs.jmedchem.5b00810.
Philipp Holzer 1,  Keiichi Masuya 1,  Pascal Furet 1,  Joerg Kallen 1,  Therese Valat-Stachyra 1,  Stéphane Ferretti 1,  Joerg Berghausen 1,  Michèle Bouisset-Leonard 1,  Nicole Buschmann 1,  Carole Pissot-Soldermann 1,  Caroline Rynn 1,  Stephan Ruetz 1,  Stefan Stutz 1,  Patrick Chène 1,  Sébastien Jeay 1,  Francois Gessier 1
Affiliations

Affiliation

  • 1 Novartis Institutes for BioMedical Research , 4002 Basel, Switzerland.
PMID: 26181851 DOI: 10.1021/acs.jmedchem.5b00810
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.

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