Drug intelligence / Profile preview

HLX208 + rifampicin

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

Overview

HLX208 + rifampicin is a combination of HLX208, a small molecule inhibitor specifically targeting BRAF V600E mutations, and rifampicin, a broad-spectrum antibiotic primarily used against mycobacterial infections. HLX208 demonstrates antitumor activity by inhibiting the constitutively active serine/threonine kinase BRAF V600E—a mutation that drives pathogenesis in several cancers, including Langerhans cell histiocytosis (LCH) and Erdheim-Chester disease (ECD)[1][3][5][7]. HLX208 exhibits high bioavailability and a novel chemical structure, differing from marketed BRAF inhibitors, and has shown efficacy and safety in phase 2 trials for LCH, ECD, and several solid tumors[1][3][5][7]. Rifampicin inhibits bacterial DNA-dependent RNA polymerase, thereby preventing transcription and bacterial replication; as an inducer of hepatic enzymes, it can significantly interact with drugs metabolized by the liver, including small molecule inhibitors. The combination of HLX208 with rifampicin would be expected to require close monitoring due to enzymatic interaction potential but no clinical studies of this exact combination have been reported. HLX208 is developed by Shanghai Henlius Biotech and was introduced from NeuPharma[3][5].

02

Targets

RNAP (Bacterial dna-dependent RNA polymerase)BRAF V600ECYP3A4 (Cytochrome P450 3A4)

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