Drug intelligence / Profile preview

CZ0775

Development stage
Preclinical
Lead developer
Chemizon
Modality
Small Molecules
01

Overview

CZ0775 is a small molecule inhibitor targeting MEK1 and MEK2, key kinases in the MAPK/ERK signaling pathway. It was developed by Chemizon for potential use in oncology, particularly for non-small cell lung cancer (NSCLC) with EGFR mutations. Preclinical studies demonstrated that while monotherapy with CZ0775 showed limited cytotoxicity in certain NSCLC cell lines, its combination with EGFR inhibitors such as lapatinib resulted in synergistic anti-proliferative and pro-apoptotic effects. The mechanism involves inhibition of ERK phosphorylation and upregulation of the pro-apoptotic protein BIM, leading to caspase-3-dependent apoptosis. This suggests potential utility for overcoming resistance to EGFR tyrosine kinase inhibitors in lung cancer[1][2][4].

Other names
CZ-0775CZ0775CZ 0775
02

Targets

MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)

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