Drug intelligence / Profile preview

EGF816 + LXH254

Development stage
Unknown
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

EGF816 + LXH254 is an investigational **combination therapy** of two oral small molecule inhibitors developed for the treatment of advanced non-small cell lung cancer (NSCLC) with EGFR mutations. **EGF816 (nazartinib)** is a third-generation, mutant-selective, irreversible inhibitor of the epidermal growth factor receptor (EGFR), targeting mutations such as exon 19 deletion, L858R, and T790M. **LXH254 (naporafenib)** is an oral, selective **pan-RAF inhibitor** that targets RAF kinases in the RAS/RAF/MEK/ERK pathway, including BRAF and CRAF, and is under investigation for tumors with MAPK pathway alterations. This combination aims to address resistance mechanisms in NSCLC by concurrently inhibiting critical drivers of tumor growth. The combination is being developed and studied by Novartis in Phase 1 clinical trials for patients with advanced EGFR-mutant NSCLC[1][3][5][7][9].

Other names
EGF816 + LXH254nazartinib + naporafenib
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)RAF1 (c-Raf-1 (Y340D/Y341D))BRAF (B-Raf proto-oncogene, serine/threonine kinase)

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