Discovery of a
Dihydroisoquinolinone Derivative (NVP-CGM097):
A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical
Trials in p53wt Tumors
Posted on 2015-08-27 - 00:00
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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Holzer, Philipp; Masuya, Keiichi; Furet, Pascal; Kallen, Joerg; Valat-Stachyra, Therese; Ferretti, Stéphane; et al. (2016). Discovery of a
Dihydroisoquinolinone Derivative (NVP-CGM097):
A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical
Trials in p53wt Tumors. ACS Publications. Collection. https://doi.org/10.1021/acs.jmedchem.5b00810
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AUTHORS (16)
PH
Philipp Holzer
KM
Keiichi Masuya
PF
Pascal Furet
JK
Joerg Kallen
TV
Therese Valat-Stachyra
SF
Stéphane Ferretti
JB
Joerg Berghausen
MB
Michèle Bouisset-Leonard
NB
Nicole Buschmann
CP
Carole Pissot-Soldermann
CR
Caroline Rynn
SR
Stephan Ruetz
SS
Stefan Stutz
PC
Patrick Chène
SJ
Sébastien Jeay
FG
Francois Gessier