alisertib
Small moleculeexperimental
Alisertib (MLN8237) is an orally available, investigational, reversible, ATP-competitive, selective aurora A kinase inhibitor developed by Takeda. Inhibition of aurora A kinase A leads to disruption of mitotic spindle apparatus assembly, disruption of chromosome segregation, and inhibition of cell proliferation. — Wikipedia
Clinical trial activity
63 trials · 31 clinical orgs · 0 marketing orgs
Phase 1
41
Phase 2
27
Phase 3
1
Phase 4
0
Earliest trial started May 1, 2007 (NCT00500903)
Timeline
Indications
Studied for
- Adenocarcinoma · Phase 1
- Astrocytoma · Phase 1
- Brain Neoplasms · Phase 1
- Breast Neoplasms · Phase 2
- Burkitt Lymphoma · Phase 2
- Carcinoma, Non-Small-Cell Lung · Phase 1/Phase 2
- Carcinoma, Transitional Cell · Phase 2
- Colonic Neoplasms · Phase 1
- Colorectal Neoplasms · Phase 1
- Digestive System Neoplasms · Phase 1
- Enteropathy-Associated T-Cell Lymphoma · Phase 1
- Ependymoma · Phase 1
- Esophageal Neoplasms · Phase 1/Phase 2
- Fallopian Tube Neoplasms · Phase 2
- Fibrosarcoma · Phase 2
- Glioblastoma · Phase 1
- Glioma · Phase 1
- Gliosarcoma · Phase 1
- Hamartoma · Phase 2
- Head and Neck Neoplasms · Phase 1
- Hepatoblastoma · Phase 2
- Hodgkin Disease · Phase 1
- Intestinal Neoplasms · Phase 1
- Intraocular Lymphoma · Phase 1
- Kidney Neoplasms · Phase 2
- Leiomyosarcoma · Phase 2
- Leukemia, Hairy Cell · Phase 1
- Leukemia, Large Granular Lymphocytic · Phase 1
- Leukemia, Lymphocytic, Chronic, B-Cell · Phase 1
- Leukemia-Lymphoma, Adult T-Cell · Phase 2
- Leukemia, Myeloid, Acute · Phase 2
- Liposarcoma · Phase 2
- Lung Neoplasms · Phase 2
- Lymphoma · Phase 1
- Lymphoma, B-Cell · Phase 1
- Lymphoma, B-Cell, Marginal Zone · Phase 2
- Lymphoma, Follicular · Phase 2
- Lymphoma, Large B-Cell, Diffuse · Phase 2
- Lymphoma, Large-Cell, Anaplastic · Phase 2
- Lymphoma, Large-Cell, Immunoblastic · Phase 2
- Lymphoma, Mantle-Cell · Phase 2
- Lymphoma, Non-Hodgkin · Phase 2
- Lymphoma, Primary Cutaneous Anaplastic Large Cell · Phase 1
- Lymphoma, T-Cell · Phase 3
- Lymphomatoid Granulomatosis · Phase 1
- Melanoma · Phase 1
- Mesothelioma · Phase 2
- Multiple Myeloma · Phase 1/Phase 2
- Mutation · Phase 1
- Myelodysplastic Syndromes · Phase 2
- Neoplasm Metastasis · Phase 1
- Neoplasms · Phase 1/Phase 2
- Neoplasms, Germ Cell and Embryonal · Phase 2
- Nerve Sheath Neoplasms · Phase 2
- Neuroblastoma · Phase 2
- N-Myc Proto-Oncogene Protein · Phase 1
- Oligodendroglioma · Phase 1
- Osteosarcoma · Phase 2
- Ovarian Neoplasms · Phase 2
- Pancreatic Neoplasms · Phase 1
- Postmenopause · Phase 2
- Precursor B-Cell Lymphoblastic Leukemia-Lymphoma · Phase 1
- Precursor Cell Lymphoblastic Leukemia-Lymphoma · Phase 2
- Prostatic Neoplasms · Phase 2
- Rhabdoid Tumor · Phase 2
- Rhabdomyosarcoma · Phase 2
- Sarcoma · Phase 2
- Sarcoma, Ewing · Phase 2
- Sezary Syndrome · Phase 1
- Small Cell Lung Carcinoma · Phase 2
- Squamous Cell Carcinoma of Head and Neck · Phase 1/Phase 2
- Testicular Neoplasms · Phase 1
- Urinary Bladder Neoplasms · Phase 2
- Waldenstrom Macroglobulinemia · Phase 2
Mechanism of action
AURKA inhibitor
Chemistry & pharmacology
Loading structure…
SMILES
COc1cc(Nc2ncc3c(n2)-c2ccc(Cl)cc2C(c2c(F)cccc2OC)=NC3)ccc1C(=O)O- Mol. weight
- 518.93 g/mol
- Lipinski Ro5
- 2 violation(s)
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaAlisertib ↗
- ChEMBLCHEMBL483158 ↗
Also known as
- alisertib
- alisertib
- alisertib
- alisertib
- alisertib
- alsertib
- mln8237
- mln8237
- mln8237
- mln 8237
- mln-8237
- mln-8237
- mln-8237
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06369285 | Phase 2 | Dec 31, 2024 | Puma Biotechnology, Inc. |
| NCT06095505 | Phase 2 | Dec 31, 2023 | Puma Biotechnology, Inc. |
| NCT04555837 | Phase 1/Phase 2 (Phase 2) | Sep 15, 2020 | National Cancer Institute (NCI), University of Texas at Houston |
| NCT04479306 | Phase 1 | Jun 18, 2020 | University of Texas at Houston |
| NCT04085315 | Phase 1 | Aug 23, 2019 | Takeda, University of California, San Francisco |
| NCT02860000 | Phase 2 | Jul 28, 2017 | Mayo Clinic, National Cancer Institute (NCI) |
| NCT03005262 | N/A | Dec 22, 2016 | University of Texas, San Antonio |
| NCT02700022 | Phase 1 | Oct 1, 2016 | Millennium Pharmaceuticals, University of North Carolina at Chapel Hill |
| NCT02780011 | Phase 1 | Sep 1, 2016 | Methodist Cancer Center, Houston, Texas, Millennium Pharmaceuticals |
| NCT02812056 | Phase 1 | Sep 1, 2016 | Millennium Pharmaceuticals, University of Texas at Houston |
| NCT02719691 | Phase 1 | May 13, 2016 | University of Colorado, Denver |
| NCT02560025 | Phase 2 | Dec 1, 2015 | Harvard University, Takeda |
| NCT02530619 | N/A | Oct 1, 2015 | Millennium Pharmaceuticals, National Cancer Institute (NCI), Northwestern University, The Leukemia and Lymphoma Society |
| NCT02551055 | Phase 1 | Sep 1, 2015 | Millennium Pharmaceuticals, Takeda |
| NCT02319018 | Phase 1 | Aug 27, 2015 | National Cancer Institute (NCI), Yale University |
| NCT02293005 | Phase 2 | May 20, 2015 | Millennium Pharmaceuticals, University of Texas at Houston |
| NCT02367352 | Phase 1 | Mar 25, 2015 | Millennium Pharmaceuticals |
| NCT02327169 | Phase 1 | Feb 2, 2015 | Millennium Pharmaceuticals, Takeda |
| NCT02187991 | Phase 2 | Feb 1, 2015 | Millennium Pharmaceuticals, US Oncology |
| NCT02186509 | Phase 1 | Jan 1, 2015 | Millennium Pharmaceuticals, Thomas Jefferson University |
Showing 20 of 63 trials
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Organizations
Research & Development (31)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Millennium Pharmaceuticals | For profit | 36 | 23 | 4 | 2007 |
| National Cancer Institute (NCI) | Government | 16 | 10 | 3 | 2008 |
| Takeda | For profit | 6 | 0 | 2 | 2013 |
| University of Texas at Houston | Academic/Hospital | 5 | 4 | 2 | 2013 |
| Harvard University | Academic/Hospital | 3 | 2 | 2 | 2012 |
| Mayo Clinic | Academic/Hospital | 3 | 3 | 2 | 2010 |
| Puma Biotechnology, Inc. | For profit | 2 | 2 | 1 | 2023 |
| Thomas Jefferson University | Academic/Hospital | 2 | 2 | 2 | 2013 |
| University of California, Davis | Academic/Hospital | 2 | 2 | 1 | 2013 |
| City of Hope National Medical Center | Academic/Hospital | 1 | 0 | 1 | 2012 |
| Cornell University | Academic/Hospital | 1 | 1 | 1 | 2013 |
| Emory University | Academic/Hospital | 1 | 1 | 1 | 2013 |
| Methodist Cancer Center, Houston, Texas | Academic/Hospital | 1 | 1 | 1 | 2016 |
| Northwestern University | Academic/Hospital | 1 | 1 | 1 | 2015 |
| NRG Oncology | Academic/Hospital | 1 | 0 | 1 | 2012 |
| Ohio State University | Academic/Hospital | 1 | 0 | 1 | 2013 |
| Southwest Oncology Group | Academic/Hospital | 1 | 0 | 1 | 2011 |
| St. Jude Children's Hospital | Academic/Hospital | 1 | 1 | 1 | 2014 |
| Temple University | Academic/Hospital | 1 | 1 | 1 | 2011 |
| The Leukemia and Lymphoma Society | Academic/Hospital | 1 | 0 | 1 | 2015 |
31 organizations
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