Drug intelligence / Profile preview

zongertinib + itraconazole

Development stage
Unknown
Lead developer
Boehringer Ingelheim
Modality
Small Molecules
Administration
Oral
01

Overview

This is a **combination regimen** comprising *zongertinib* and *itraconazole*. - **Zongertinib** is a small molecule kinase inhibitor targeting **human epidermal growth factor receptor 2 (HER2)**, used for the treatment of adults with unresectable or metastatic non-squamous non-small cell lung cancer (NSCLC) harboring HER2 tyrosine kinase domain activating mutations, as detected by an FDA-approved test, typically in patients who have received prior systemic therapy[1][3][4]. It acts by inhibiting phosphorylation of HER2 and downstream pathways (e.g., ERK), suppressing proliferation of cancer cells with HER2 mutations[4]. - **Itraconazole** is a triazole antifungal agent that inhibits fungal **lanosterol 14α-demethylase** (CYP51A1), affecting ergosterol biosynthesis. It also modulates human drug-metabolizing enzymes, including inhibition of **CYP3A4**, and is sometimes investigated for off-label anticancer effects due to effects on signaling pathways such as **hedgehog pathway** and angiogenesis. No unique brand name or code name exists for this combination itself. The **combination may be considered for drug-drug interaction studies** since itraconazole is a known CYP3A4 inhibitor and zongertinib is partially metabolized by CYP3A4/5[4].

02

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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