Drug intelligence / Profile preview

BPI-7711 + itraconazole

Development stage
Phase 1
Lead developer
Beta Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

BPI-7711 + itraconazole is a **combination regimen** of rezivertinib (BPI-7711), a novel third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI), and itraconazole, an antifungal agent known to be a potent inhibitor of the cytochrome P450 enzyme CYP3A4. BPI-7711 (rezivertinib) selectively and irreversibly inhibits both sensitizing and T790M-resistant EGFR mutations and is indicated primarily for EGFR-mutated non-small cell lung cancer (NSCLC). Itraconazole may be used in combination for pharmacokinetic interaction studies, as it can increase blood levels of BPI-7711 by inhibiting its metabolism through CYP3A4 inhibition. This combination is used in clinical pharmacology studies to evaluate drug-drug interactions, but is not a therapeutic fixed-dose combination for any indication.

Brand names
rezivertinib
Other names
rezivertinib + itraconazole
02

Targets

EGFR (Epidermal growth factor receptor)CYP3A4 (Cytochrome P450 3A4)

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