Drug intelligence / Profile preview

erlotinib + CB-839

Development stage
Unknown
Lead developer
Calithera Biosciences, Inc
Modality
Small Molecules
Administration
Oral
01

Overview

A combination of **erlotinib**, an **epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor**, and **CB-839 (Telaglenastat)**, a **small-molecule inhibitor of glutaminase 1 (GLS-1)**. This combination is being investigated as a metabolic-targeted therapy, particularly in **non-small cell lung cancer (NSCLC)** with EGFR mutations. Erlotinib inhibits EGFR signaling, decreasing glucose uptake and glycolysis, while CB-839 limits glutamine metabolism and impairs glutathione and ATP production. Dual inhibition produces **energetic stress** leading to cell death and tumor regression in preclinical EGFR mutant lung cancer models. The approach seeks to exploit the metabolic dependency of cancer cells on both glucose and glutamine for their survival and proliferation[1][3][5].

Brand names
Tarceva (for erlotinib)Telaglenastat (for CB-839)
Other names
erlotinib and CB-839erlotinib plus CB-839
02

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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