Drug intelligence / Profile preview

GDC-0712

Development stage
Preclinical
Lead developer
Genentech
Modality
Small Molecules
Administration
Oral
01

Overview

GDC-0712 is a potent and selective small molecule inhibitor of the MET receptor tyrosine kinase (also known as hepatocyte growth factor receptor, HGFR). Developed by Genentech, it was primarily investigated in preclinical models for its ability to block MET phosphorylation and downstream oncogenic signaling pathways, including MAPK and PI3K. Research has demonstrated that GDC-0712 can suppress tumor growth in pancreatic cancer xenograft models, particularly when used in combination with other targeted agents such as MEK inhibitors (e.g., cobimetinib/GDC-0973) or EGFR inhibitors (e.g., erlotinib). By inhibiting MET, GDC-0712 disrupts the HGF-mediated signaling that drives tumor cell proliferation, survival, and invasive growth.

02

Targets

MET (Mesenchymal-epithelial transition factor receptor)

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