Drug intelligence / Profile preview

ziftomenib + itraconazole

Development stage
Unknown
Lead developer
Kura Oncology
Modality
Small Molecules
Administration
Oral
01

Overview

Ziftomenib + itraconazole refers to the combined use of ziftomenib, a selective small molecule menin-MLL (KMT2A) inhibitor developed for the treatment of acute myeloid leukemia, especially with NPM1 or KMT2A mutations, and itraconazole, a triazole antifungal agent commonly used to treat fungal infections. This combination has been investigated in clinical studies to assess the effects of itraconazole—a strong CYP3A4 inhibitor—on the pharmacokinetics (PK) of ziftomenib, given potential drug-drug interactions important for dosing and safety in leukemia settings. Itraconazole may increase ziftomenib exposure by inhibiting its metabolism. There is no evidence that this combination serves as an approved therapeutic regimen; its use together is for pharmacokinetic interaction studies in clinical trials.

02

Targets

CYP51A1 (Sterol 14α-demethylase)MEN1 (Menin)

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