Drug intelligence / Profile preview

milademetan + itraconazole

Development stage
Unknown
Lead developer
Daiichi Sankyo
Modality
Small Molecules
Administration
Oral
01

Overview

Milademetan + itraconazole is a combination of **milademetan**, a small molecule inhibitor of murine double minute 2 (MDM2), and **itraconazole**, a potent antifungal agent and strong inhibitor of CYP3A and P-glycoprotein. This combination has been investigated in clinical pharmacokinetic studies to assess drug–drug interaction effects, primarily focused on how itraconazole alters the exposure of milademetan. Milademetan is being developed for the treatment of advanced solid tumors and hematological cancers, including liposarcoma and acute myeloid leukemia. When administered together, itraconazole significantly increases milademetan plasma exposure (AUC) without notably affecting its absorption rate. The primary impact is through inhibition of CYP3A-mediated metabolism of milademetan, leading to higher systemic levels and necessitating dose reduction of milademetan when combined with itraconazole. There is no unique proprietary brand or product for this combination; currently, it is of research/clinical pharmacology interest[1][3][4].

Other names
milademetanDS-3032DS3032DS 3032itraconazole
02

Targets

MDM2 (Mouse double minute 2 homolog)CYP3A4 (Cytochrome P450 3A4)ABCB1 (P-glycoprotein)

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