Discovery of Potent and Selective p53-MDM2 Protein–Protein Interaction Inhibitors as Anticancer Drugs

Authors

  • Philipp Holzer Novartis Institutes for BioMedical Research CH-4002 Basel, Switzerland. Philipp.Holzer@novartis.com

DOI:

https://doi.org/10.2533/chimia.2017.716

Keywords:

Clinical trial, Hdm2, Inhibitor, Mdm2, Nvp-cgm097, Nvp-hdm201, P53, Protein–protein interaction, Ppi

Abstract

As a result of our persistent efforts to discover novel inhibitors of the p53-MDM2 protein–protein interaction useful for the treatment of cancer, the potent and selective MDM2 inhibitors NVP-CGM097 and NVP-HDM201 with excellent in vitro and in vivo profile were selected as clinical candidates and are currently in phase 1 clinical development. This short review article provides a summary of the program history, the applied pharmacophore model and the discovery story of these novel p53-MDM2 inhibitor investigational drugs.

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Published

2017-10-25

How to Cite

[1]
P. Holzer, Chimia 2017, 71, 716, DOI: 10.2533/chimia.2017.716.

Issue

Section

Scientific Articles