pevonedistat
Small moleculeexperimental
Pevonedistat (MLN4924) is a selective NEDD8 inhibitor. It is being investigated as a cancer treatment, e.g. for mantle cell lymphoma (MCL). — Wikipedia
Clinical trial activity
42 trials · 21 clinical orgs · 0 marketing orgs
Phase 1
27
Phase 2
19
Phase 3
4
Phase 4
0
Earliest trial started Apr 1, 2008 (NCT00677170)
Timeline
Indications
Studied for
- Carcinoma, Hepatocellular · Phase 2
- Carcinoma, Non-Small-Cell Lung · Phase 2
- Cholangiocarcinoma · Phase 2
- Hematologic Neoplasms · Phase 1
- Hodgkin Disease · Phase 1
- Hypercholesterolemia · Phase 3
- Leukemia, Eosinophilic, Acute · Phase 1/Phase 2
- Leukemia, Lymphocytic, Chronic, B-Cell · Phase 1
- Leukemia, Myeloid · Phase 1/Phase 2
- Leukemia, Myeloid, Acute · Phase 3
- Leukemia, Myeloid, Chronic, Atypical, BCR-ABL Negative · Phase 1/Phase 2
- Leukemia, Myelomonocytic, Chronic · Phase 3
- Leukemia, Neutrophilic, Chronic · Phase 1/Phase 2
- Leukemia, Prolymphocytic, B-Cell · Phase 1
- Liver Diseases · Phase 1
- Lung Neoplasms · Phase 2
- Lymphoma · Phase 1
- Lymphoma, B-Cell, Marginal Zone · Phase 1
- Lymphoma, Follicular · Phase 1
- Lymphoma, Large B-Cell, Diffuse · Phase 1/Phase 2
- Lymphoma, Mantle-Cell · Phase 1
- Lymphoma, Non-Hodgkin · Phase 1
- Lymphoma, Primary Cutaneous Anaplastic Large Cell · Phase 1
- Melanoma · Phase 1
- Mesothelioma · Phase 1/Phase 2
- Multiple Myeloma · Phase 1
- Myelodysplastic Syndromes · Phase 3
- Myeloproliferative Disorders · Phase 2
- Neoplasm Metastasis · Phase 2
- Neoplasm, Residual · Phase 2
- Neoplasms · Phase 1/Phase 2
- Polycythemia Vera · Phase 1/Phase 2
- Precursor B-Cell Lymphoblastic Leukemia-Lymphoma · Phase 1
- Precursor Cell Lymphoblastic Leukemia-Lymphoma · Phase 1
- Primary Myelofibrosis · Phase 1/Phase 2
- Renal Insufficiency · Phase 1
- Thrombocythemia, Essential · Phase 1/Phase 2
Mechanism of action
- NEDD8 activating enzymeINHIBITOR
NEDD8 activating enzyme inhibitor
Potent inhibitor of NEDD8 activating enzyme (NAE) (IC50 = 0.004uM).
Chemistry & pharmacology
Loading structure…
SMILES
NS(=O)(=O)OC[C@@H]1C[C@@H](n2ccc3c(N[C@H]4CCc5ccccc54)ncnc32)C[C@@H]1O- Mol. weight
- 443.53 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaPevonedistat ↗
- ChEMBLCHEMBL1231160 ↗
Also known as
- ((1s,2s,4r)-4-(4-((1s)-2,3-dihydro-1h-inden-1-ylamino)-7h-pyrrolo(2,3-d)pyrimidin-7-yl)-2-hydroxycyclopentyl)methyl sulfamate
- ((1s,2s,4r)-4-(4-((1s)-2,3-dihydro-1h-inden-1-ylamino)-7h-pyrrolo(2,3-d)pyrimidin-7-yl)-2-hydroxycyclopentyl)methyl sulphamate
- 4-(4-((1s)-2,3-dihydro-1h-inden-1-ylamino)-7h-pyrrolo(2,3-d)pyrimidin-7-yl)-2-hydroxycyclopentyl methyl sulfamidate
- mln4924
- mln4924
- mln4924
- mln-4924
- mln-4924
- pevonedistat
- pevonedistat
- pevonedistat
- pevonedistat
- pevonedistat
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT04985656 | Phase 2 | Oct 1, 2021 | Takeda |
| NCT04800627 | Phase 1/Phase 2 (Phase 2) | Mar 29, 2021 | University of Texas at Houston |
| NCT04712942 | Phase 2 | Jan 1, 2021 | Millennium Pharmaceuticals, University of Leipzig |
| NCT04266795 | Phase 2 | Mar 31, 2020 | Takeda |
| NCT04289649 | Phase 3 | Mar 12, 2020 | Kowa |
| NCT04289662 | Phase 3 | Mar 6, 2020 | Kowa |
| NCT04175912 | Phase 2 | Jan 31, 2020 | ECOG-ACRIN Cancer Research Group, National Cancer Institute (NCI) |
| NCT04172844 | Phase 1 | Dec 1, 2019 | Medical College of Wisconsin |
| NCT03965689 | Phase 2 | Aug 16, 2019 | Johns Hopkins University, National Cancer Institute (NCI) |
| NCT04090736 | Phase 3 | Aug 13, 2019 | Dynamic Science S.L., Millennium Pharmaceuticals, PETHEMA Foundation |
| NCT03814005 | Phase 1 | Jul 31, 2019 | Millennium Pharmaceuticals |
| NCT03770260 | Phase 1 | Jun 7, 2019 | Emory University, National Cancer Institute (NCI) |
| NCT03745352 | Phase 2 | May 31, 2019 | City of Hope National Medical Center, National Cancer Institute (NCI) |
| NCT03813147 | Phase 1 | May 1, 2019 | National Cancer Institute (NCI) |
| NCT03772925 | Phase 1 | Feb 28, 2019 | National Cancer Institute (NCI), University of Toronto |
| NCT03862157 | Phase 1/Phase 2 (Phase 2) | Feb 27, 2019 | National Cancer Institute (NCI), University of Texas at Houston |
| NCT03349281 | Phase 1 | Sep 30, 2018 | Takeda, University of Miami |
| NCT03486314 | Phase 1 | Aug 13, 2018 | Millennium Pharmaceuticals |
| NCT03709576 | Phase 2 | Jul 18, 2018 | Millennium Pharmaceuticals, Pennsylvania State University, Takeda |
| NCT03459859 | Phase 1 | May 21, 2018 | Takeda, University of Miami |
Showing 20 of 42 trials
Page 1 / 3
Organizations
Research & Development (21)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Millennium Pharmaceuticals | For profit | 18 | 15 | 4 | 2008 |
| National Cancer Institute (NCI) | Government | 13 | 8 | 2 | 2011 |
| Takeda | For profit | 8 | 2 | 3 | 2016 |
| City of Hope National Medical Center | Academic/Hospital | 3 | 2 | 2 | 2017 |
| University of Texas at Houston | Academic/Hospital | 3 | 2 | 1 | 2017 |
| Kowa | For profit | 2 | 2 | 1 | 2020 |
| University of Miami | Academic/Hospital | 2 | 2 | 1 | 2018 |
| Dynamic Science S.L. | For profit | 1 | 0 | 1 | 2019 |
| ECOG-ACRIN Cancer Research Group | Academic/Hospital | 1 | 0 | 1 | 2020 |
| Emory University | Academic/Hospital | 1 | 0 | 1 | 2019 |
| Johns Hopkins University | Academic/Hospital | 1 | 0 | 1 | 2019 |
| Medical College of Wisconsin | Academic/Hospital | 1 | 1 | 1 | 2019 |
| Memorial Sloan-Kettering Cancer Center | Academic/Hospital | 1 | 1 | 1 | 2017 |
| Pennsylvania State University | Academic/Hospital | 1 | 1 | 1 | 2018 |
| PETHEMA Foundation | Academic/Hospital | 1 | 1 | 1 | 2019 |
| University of Leipzig | Academic/Hospital | 1 | 1 | 1 | 2021 |
| University of Michigan | Academic/Hospital | 1 | 1 | 1 | 2018 |
| University of Southern California | Academic/Hospital | 1 | 1 | 1 | 2018 |
| University of Toronto | Academic/Hospital | 1 | 0 | 1 | 2019 |
| Vanderbilt University | Academic/Hospital | 1 | 1 | 1 | 2017 |
21 organizations
Page 1 / 2