Drug intelligence / Profile preview

hlx208 + itraconazole

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

Overview

HLX208 + itraconazole is a combination regimen comprising HLX208, a small-molecule inhibitor targeting the BRAF V600E mutation, and itraconazole, an antifungal agent that is sometimes studied for its effect on drug metabolism and, in some settings, as a potential anticancer repurposing candidate due to its impact on the Hedgehog pathway and other mechanisms. HLX208 is developed for the treatment of adult patients with conditions such as Langerhans cell histiocytosis (LCH) and Erdheim-Chester disease (ECD) harboring the BRAF V600E mutation. HLX208 acts by inhibiting the constitutive activation of the MAPK/ERK signaling pathway driven by this mutation, and is administered orally. Itraconazole is not an anticancer agent but may be used in combination to affect HLX208’s pharmacokinetics and bioavailability by inhibiting CYP3A4-mediated metabolism. There is no evidence of a unique commercial formulation under the name "HLX208 + itraconazole"; this is a regimen of two existing drugs, not a fixed-combination product.

02

Targets

CYP3A4 (Cytochrome P450 3A4)BRAF V600E

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