Drug intelligence / Profile preview

HLX208 + cetuximab

Development stage
Phase 2
Lead developer
Henlius
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

HLX208 + cetuximab is an investigational combination therapy comprising **HLX208**, a novel small-molecule inhibitor of BRAF V600E, and **cetuximab**, an anti-EGFR monoclonal antibody. HLX208 is developed by Shanghai Henlius Biotech and is designed to selectively inhibit the mutated BRAF V600E protein, a serine/threonine kinase implicated in multiple cancers through the MAPK/ERK pathway. Cetuximab, developed by Merck KGaA and Bristol Myers Squibb, inhibits the epidermal growth factor receptor (EGFR), used in several solid tumors, especially colorectal and head and neck cancers. The combination aims to suppress two key oncogenic drivers—BRAF V600E and EGFR—to provide a synergistic therapeutic effect in tumors harboring BRAF V600E mutations, especially solid tumors where resistance to BRAF monotherapy is commonly mediated by EGFR activation. HLX208 shows promising efficacy and a manageable safety profile in early trials for BRAF V600E-mutant Langerhans cell histiocytosis, Erdheim-Chester disease, and advanced solid tumors, with ongoing investigations in combination regimens, including with anti-EGFR antibodies, to address additional resistance mechanisms[1][2][3].

02

Targets

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