Pyrotinib + fluconazole

Pyrotinib + fluconazole refers to the coadministration of two pharmaceutical agents: pyrotinib, an oral irreversible pan-ErbB receptor tyrosine kinase inhibitor primarily used in the treatment of HER2-positive breast cancer, and fluconazole, a triazole antifungal agent used to treat and prevent a variety of fungal infections. Pyrotinib acts by inhibiting epidermal growth factor receptor (EGFR/HER1), HER2, and HER4 signaling pathways, thereby blocking tumor cell proliferation. Fluconazole works by inhibiting lanosterol 14-alpha-demethylase in fungi, disrupting ergosterol synthesis and compromising fungal cell membrane integrity. When administered together, fluconazole—a moderate CYP3A4 inhibitor—significantly increases systemic exposure to pyrotinib by reducing its metabolism via CYP3A4 inhibition[1][3]. This combination may require dose adjustments or increased monitoring due to elevated risk of adverse effects from higher pyrotinib plasma concentrations.

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