Drug intelligence / Profile preview

HLX208

Development stage
Phase 2
Lead developer
Henlius
Modality
Small Molecules
Administration
Oral
01

Overview

HLX208 is an orally bioavailable, small molecule inhibitor that selectively targets the BRAF protein with the V600E mutation. It features a proprietary novel chemical structure distinct from other marketed BRAF inhibitors, exhibiting high bioavailability and strong antitumor efficacy in preclinical studies. Developed by Shanghai Henlius Biotech and introduced from NeuPharma, HLX208 has shown promising safety and efficacy in early clinical trials for patients with cancers harboring the BRAF V600E mutation. The drug is currently being evaluated in phase 2 clinical trials for adult Langerhans cell histiocytosis (LCH), Erdheim-Chester disease (ECD), and advanced solid tumors with BRAF V600 mutations. Mechanistically, it inhibits mutant BRAF kinase activity within the RAS-RAF-MEK-ERK MAPK signaling pathway, thereby blocking downstream MEK/ERK activation to suppress tumor cell proliferation.

Other names
BRAF V600E inhibitor HLX208
02

Targets

BRAF V600E

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