Synonyms: MLN 4924 | MLN-4924 | MLN4924 | TAK-924 | TAK924
Compound class:
Synthetic organic
Comment: Pevonedistat (MLN4924) is an inhibitor of the NEDD8 activating enzyme (NAE) [1], which is a heterodimer of NAE1 (NAE1; Q13564) and UBA3 subunits. Pevonedistat is structurally similar to the NAE reaction product adenosine 5′-monophosphate (AMP), and interacts with nucleotide-binding site of NAE. NAE is essential for the NEDD8 conjugation pathway which controls the activity of the cullin-RING ubiquitin E3 ligases. NAE inhibitors are proposed to disrupt cullin-RING ligase-mediated protein turnover and to promote apoptosis in human tumour cells.
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No information available. |
Summary of Clinical Use |
Pevonedistat (MLN4924) has progressed to clinical evaluation in solid and liquid tumours. |
Clinical Trials | |||||
Clinical Trial ID | Title | Type | Source | Comment | References |
NCT03268954 | Pevonedistat Plus Azacitidine Versus Single-Agent Azacitidine as First-Line Treatment for Participants With Higher-Risk Myelodysplastic Syndromes (HR MDS), Chronic Myelomonocytic Leukemia (CMML), or Low-Blast Acute Myelogenous Leukemia (AML) | Phase 3 Interventional | Takeda | ||
NCT03330821 | Pevonedistat, Cytarabine, and Idarubicin in Treating Patients With Acute Myeloid Leukemia | Phase 1/Phase 2 Interventional | University of Southern California | ||
NCT03965689 | Testing the Combination of MLN4924 (Pevonedistat), Carboplatin, and Paclitaxel in Patients With Advanced Non-small Cell Lung Cancer (NSCLC) Who Have Previously Been Treated With Immunotherapy | Phase 2 Interventional | National Cancer Institute (NCI) | ||
NCT03486314 | A Study to Evaluate the Effects of Rifampin on Pharmacokinetics (PK) of Pevonedistat in Participants With Advanced Solid Tumors | Phase 1 Interventional | Takeda | 2 |