Drug intelligence / Profile preview

GDC-0623

Development stage
Phase 1
Lead developer
Genentech
Modality
Small Molecules
Administration
Oral
01

Overview

GDC-0623 is an orally active, selective small molecule inhibitor of mitogen-activated protein kinase kinase (MEK or MAP/ERK kinase), developed as a potential antineoplastic agent. It acts as a potent ATP non-competitive inhibitor of MEK1 (Ki = 0.13 nM), effectively blocking growth factor-mediated cell signaling and tumor cell proliferation by inhibiting the RAS/RAF/MEK/ERK pathway. This pathway is frequently dysregulated in cancers due to mutations in upstream components such as BRAF and KRAS. GDC-0623 has demonstrated efficacy against both mutant BRAF and mutant KRAS-driven tumors and has been investigated in clinical trials for the treatment of locally advanced or metastatic solid tumors[1][2][3][4][5].

Other names
1168091-68-6
02

Targets

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

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