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erlotinib + momelotinib
- Development stage
- Discontinued
- Lead developer
- GSK
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
A combination therapy consisting of erlotinib, an EGFR tyrosine kinase inhibitor, and momelotinib, a JAK1/2 and TBK1 inhibitor. This combination was investigated in clinical trials for EGFR-mutated non-small cell lung cancer (NSCLC) based on preclinical evidence suggesting the interleukin-6/JAK/STAT3 cytokine loop plays a role in EGFR TKI resistance.
02
Targets
ACVR1 (Activin receptor type I)EGFR (Epidermal growth factor receptor)JAK1 (Janus kinase 1)JAK2 (Janus kinase 2)TBK1 (TANK binding kinase 1)
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