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Synonyms: MLN-2238 | MLN2238 | Ninlaro®
ixazomib is an approved drug (FDA (2015), EMA (2016))
Compound class: Synthetic organic
Comment: Ixazomib is the first approved oral proteasome inhibitor. Ixazomib reversibly inhibits 20S proteasome activity. Like bortezomib, ixazomib primarily inhibits the chymotrypsin-like (β5) proteolytic site within the 20S proteasome, but its pharmacokinetics, pharmacodynamics, and antitumor activity are superior to those of bortezomib .
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Bonvini P, Zorzi E, Basso G, Rosolen A. (2007)
Bortezomib-mediated 26S proteasome inhibition causes cell-cycle arrest and induces apoptosis in CD-30+ anaplastic large cell lymphoma.
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2. Ciechanover A. (2005)
Intracellular protein degradation: from a vague idea, through the lysosome and the ubiquitin-proteasome system, and onto human diseases and drug targeting (Nobel lecture).
Angew Chem Int Ed Engl, 44 (37): 5944-67. [PMID:16142822]
3. Kupperman E, Lee EC, Cao Y, Bannerman B, Fitzgerald M, Berger A, Yu J, Yang Y, Hales P, Bruzzese F et al.. (2010)
Evaluation of the proteasome inhibitor MLN9708 in preclinical models of human cancer.
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4. Richardson PG, Moreau P, Laubach JP, Gupta N, Hui AM, Anderson KC, San Miguel JF, Kumar S. (2015)
The investigational proteasome inhibitor ixazomib for the treatment of multiple myeloma.
Future Oncol, 11 (8): 1153-68. [PMID:25832873]