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docetaxel + pevonedistat
- Development stage
- Unknown
- Lead developer
- Millennium Pharmaceuticals
- Modality
- Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
- Administration
- Intravenous
01
Overview
Docetaxel + pevonedistat is an investigational combination therapy consisting of docetaxel, a microtubule inhibitor chemotherapy agent, and pevonedistat (MLN4924), a first-in-class small molecule inhibitor of the NEDD8-activating enzyme (NAE). Docetaxel disrupts microtubule function leading to cell cycle arrest and apoptosis in cancer cells. Pevonedistat inhibits neddylation by blocking NAE, which prevents activation of cullin-RING ligases (CRLs) involved in protein degradation pathways critical for tumor growth and survival. The combination has been studied primarily in patients with relapsed or refractory advanced non-small cell lung cancer (NSCLC), where it demonstrated safety and preliminary antitumor activity. Development of pevonedistat was discontinued by the sponsor during clinical trials[1][2][5].
- Brand names
- None specific to the combinationDocetaxel is marketed as Taxotere
- Other names
- pevonedistat and docetaxel combinationMLN4924 + docetaxelTAK-924 + docetaxel
02
Targets
NAE (NEDD8-activating enzyme)TUBB (Tubulin (alpha and beta subunits))
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