Drug intelligence / Profile preview

nemtabrutinib + itraconazole

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

Overview

**Nemtabrutinib + itraconazole** is a combination of two pharmaceutical drugs administered together. Nemtabrutinib (formerly known as ARQ-531) is a small molecule inhibitor of Bruton tyrosine kinase (BTK), developed as a targeted therapy mainly for hematological malignancies. Itraconazole is a broad-spectrum triazole antifungal that inhibits fungal cytochrome P450-dependent enzyme lanosterol 14\u03b1-demethylase, impairing ergosterol synthesis and disrupting fungal cell membrane formation. This specific combination is under investigation for *drug-drug interaction studies*: Itraconazole is used to observe its effect as a strong CYP3A4 inhibitor on the pharmacokinetics of nemtabrutinib, as nemtabrutinib is likely metabolized by the CYP3A4 pathway. Itraconazole is sometimes combined with other drugs to manage fungal infections, but there is no clinical evidence or approval for the combined use of nemtabrutinib and itraconazole as a therapeutic regimen for any specific disease. The combination is not a fixed-dose product or marketed formulation.

02

Targets

CYP3A4 (Cytochrome P450 3A4)BTK (Bruton tyrosine kinase)CYP51A1 (Sterol 14α-demethylase)

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