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MLN4924 + itraconazole
- Development stage
- Unknown
- Lead developer
- Takeda
- Modality
- Small Molecules
- Administration
- Intravenous, Oral
01
Overview
MLN4924 + itraconazole is an investigational combination used in clinical pharmacokinetic studies to evaluate drug-drug interactions. MLN4924 (also known as pevonedistat or TAK-924) is a **small molecule inhibitor of the NEDD8-activating enzyme (NAE)**, which suppresses cullin-RING ligase (CRL) activity and disrupts proteasomal protein degradation in malignant cells, leading to cell cycle arrest and apoptosis. *Itraconazole* is an antifungal agent and a strong inhibitor of CYP3A and P-glycoprotein (P-gp), used in the combination to assess its impact on MLN4924 metabolism. The combination is not a marketed therapy but was studied for drug-drug interactions and safety in patients with advanced solid tumors[1][2][3][5].
- Other names
- pevonedistat + itraconazole
02
Targets
NAE (NEDD8-activating enzyme)CYP3A (CYP3A family)ABCB1 (P-glycoprotein)
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