MLN4924 + fluconazole

MLN4924 + fluconazole refers to the combination of **MLN4924 (pevonedistat)**, a first-in-class small molecule inhibitor of the NEDD8-activating enzyme (NAE), with **fluconazole**, a moderate CYP3A inhibitor and antifungal agent. MLN4924 blocks NEDD8 activation, thereby inhibiting cullin-RING E3 ubiquitin ligase activity, causing protein accumulation, cell cycle arrest, apoptosis, autophagy, senescence, and antiangiogenic effects in cancer cells[2][3][5]. Fluconazole is co-administered in some clinical studies to examine pharmacokinetic interactions, as it can inhibit the CYP3A-mediated metabolism of MLN4924[1][4]. The combination is not itself a marketed fixed-drug product, but rather an investigational regimen used to assess drug-drug interactions and safety in clinical studies.

Other names

TAK924 + fluconazole