bosutinib
Trade name: bosulif
Approved
Sep 4, 2012
Bosutinib (trade name Bosulif) originally synthesized by Wyeth, it is being developed by Pfizer. Bosutinib received US FDA and EU European Medicines Agency approval on September 4, 2012 and 27 March 2013 respectively for the treatment of adult patients with Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia (CML) with resistance, or intolerance to prior therapy. Bosutinib is a synthetic quinolone derivative and dual kinase inhibitor that targets both Abl and Src kinases with potential antineoplastic activity. Unlike imatinib, bosutinib inhibits the autophosphorylation of both Abl and Src kinases, resulting in inhibition of cell growth and apoptosis. Because of the dual mechanism of action, this agent may have activity in resistant CML disease, other myeloid malignancies and solid tumors. Abl kinase is upregulated in the presence of the abnormal Bcr-abl fusion protein which is commonly associated with chronic myeloid leukemia (CML). Overexpression of specific Src kinases is also associated with the imatinib-resistant CML phenotype. — NCATS
Clinical trial activity
65 trials · 72 clinical orgs · 5 marketing orgs
Earliest trial started Oct 1, 2004 (NCT00195260)
Timeline
2000s
2010s
2020s
- Aug 25, 2023
Sun Pharmaceuticals — Marketing Organization
- May 23, 2025
Alembic — Marketing Organization
- May 28, 2025
MSN Laboratories — Marketing Organization
Indications
Approved for
Studied for
- Acute Kidney Injury · Phase 1
- Amyotrophic Lateral Sclerosis · Phase 1
- Antigens, CD · Phase 1/Phase 2
- Bone Marrow Cells · Phase 2
- Breast Neoplasms · Phase 2
- Bronchiectasis · Phase 2
- Carcinoma, Non-Small-Cell Lung · Phase 2
- Cholangiocarcinoma · Phase 1/Phase 2
- Cognitive Dysfunction · Phase 1
- Colorectal Neoplasms · Phase 1/Phase 2
- Dementia · Phase 1
- Fusion Proteins, bcr-abl · Phase 2
- Glioblastoma · Phase 2
- Hamartoma · Phase 1
- Healthy Volunteers · Phase 1
- Kidney Failure, Chronic · Phase 1
- Leukemia · Phase 2
- Leukemia, Lymphocytic, Chronic, B-Cell · Phase 1/Phase 2
- Leukemia, Myeloid, Acute · Phase 1
- Leukemia, Myeloid, Chronic, Atypical, BCR-ABL Negative · Phase 2
- Leukemia, Myeloid, Chronic-Phase · Phase 3
- Lewy Body Disease · Phase 2
- Lymphoma, Non-Hodgkin · Phase 2
- Mesothelioma · Phase 1
- Multiple Myeloma · Phase 2
- Mutation · Phase 2
- Myeloproliferative Disorders · Phase 2
- Neoplasm Metastasis · Phase 2
- Ovarian Neoplasms · Phase 1
- Pancreatic Neoplasms · Phase 1/Phase 2
- Polycystic Kidney, Autosomal Dominant · Phase 2
- Precursor B-Cell Lymphoblastic Leukemia-Lymphoma · Phase 1/Phase 2
- Renal Insufficiency, Chronic · Phase 1
- Thymoma · Phase 1
- Thymus Neoplasms · Phase 1
- Urinary Bladder Neoplasms · Phase 1
- Uterine Cervical Neoplasms · Phase 1
Mechanism of action
- Bcr/Abl fusion proteinINHIBITOR
Bcr/Abl fusion protein
- Tyrosine-protein kinase ABLINHIBITOR
ABL1 inhibitor
- Tyrosine-protein kinase LynINHIBITOR
LYN inhibitor
- Tyrosine-protein kinase SRCINHIBITOR
SRC inhibitor
- Tyrosine-protein kinase HCKINHIBITOR
HCK inhibitor
Approval history
- approvedSep 4, 2012
Chemistry & pharmacology
SMILES
COC1=CC(NC2=C(C=NC3=CC(OCCCN4CCN(C)CC4)=C(OC)C=C23)C#N)=C(Cl)C=C1Cl- Mol. weight
- 530.446 g/mol
- Lipinski Ro5
- 2 violation(s)
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- WikipediaBosutinib ↗
- NCATS5018V4AEZ0 ↗
- ChEMBLCHEMBL288441 ↗
- ChEMBLCHEMBL2095206 ↗
Also known as
- 4-((2,4-dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methyl-1-piperazinyl)propoxy)-3-quinolinecarbonitrile
- 4-((2,4-dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methyl-1-piperazinyl)propoxy)-3-quinolinecarbonitrile
- 4-((2,4-dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methyl-1-piperazinyl)propoxy)-3-quinolinecarbonitrile
- bosulif
- bosulif
- bosulif
- bosulif
- bosulif
- bosulif®
- bosulif®
- bosutinib
- bosutinib
- bosutinib
- bosutinib
- bosutinib
- bosutinib
- bosutinib
- bosutinib
- bosutinib
- bosutinib (as monohydrate)
- bosutinib hydrate
- bosutinib monohydrate
- bosutinib monohydrate
- bosutinib monohydrate
- bosutinib monohydrate
- bosutinib monohydrate
- lumacaftor / ivacaftor
- ski606
- ski 606
- ski 606
- ski 606
- ski-606
- ski-606
- ski-606
- ski-606
- ski-606
- tezacaftor/ivacaftor
- uglysycpd2
- way-173606
- way-173606
- way-173606
- way-173606
- way-173606
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07153770 | Phase 2 | Sep 20, 2025 | Huazhong University of Science and Technology |
| NCT06423911 | Phase 3 | Feb 5, 2024 | Ascentage Pharma Group Inc. |
| NCT04877522 | Phase 3 | May 16, 2022 | Novartis |
| NCT05032690 | Phase 1 | Jan 19, 2022 | Pfizer |
| NCT04971226 | Phase 3 | Oct 6, 2021 | Novartis |
| NCT04916769 | Phase 1 | Aug 13, 2021 | Pfizer |
| NCT04793399 | Phase 1/Phase 2 (Phase 2) | Feb 24, 2021 | Fundacion Espanola para la Curacion de la Leucemia Mieloide Cronica, Pfizer, Roche |
| NCT04655391 | Phase 1 | Dec 15, 2020 | City of Hope National Medical Center, National Cancer Institute (NCI) |
| NCT04626024 | Phase 2 | Nov 15, 2020 | Baylor University |
| NCT04549480 | Phase 1 | Sep 15, 2020 | Pfizer |
| NCT04258943 | Phase 1/Phase 2 (Phase 2) | Mar 20, 2020 | Dutch Childhood Oncology Group, Erasmus University Rotterdam, Innovative Therapies For Children with Cancer Consortium, National Cancer Institute (NCI), Pfizer |
| NCT04578847 | Phase 2 | Jan 15, 2020 | Russian Academy of Medical Sciences |
| NCT03888222 | Phase 2 | Apr 23, 2019 | Alzheimer's Association, Georgetown University |
| NCT03854903 | Phase 1 | Apr 1, 2019 | Georgetown University, Pfizer |
| NCT03831776 | Phase 2 | Mar 25, 2019 | CHU Henri Mondor, Hôpital Mignot, Versailles Paris, Hopital Rene Huguenin_Intitut Curie_Paris, Norwegian University of Science and Technology, University Hospital of North Norway, University of Bergen, University of Oslo, University of Southern Denmark, University of Stavanger, Uppsala University |
| NCT04744532 | Phase 1 | Mar 19, 2019 | Kitasato University, Kyoto University, Pfizer, Tokushima University, Tottori University |
| NCT03747679 | Phase 1 | Nov 22, 2018 | Pfizer |
| NCT03610971 | Phase 2 | Oct 31, 2018 | Cure CML Consortium, Incyte, University of South Florida |
| NCT03297606 | Phase 2 | Oct 6, 2017 | AstraZeneca, Bristol-Myers Squibb, British Columbia Cancer Agency, Canadian Cancer Trials Group, Pfizer, Roche, Seattle Genetics, University of Toronto |
| NCT03106779 | Phase 3 | Aug 15, 2017 | Novartis |
Organizations
Research & Development (72)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Pfizer | For profit | 46 | 34 | 5 | 2004 |
| Wyeth | For profit | 12 | 0 | 2 | 2006 |
| Novartis | For profit | 3 | 3 | 1 | 2017 |
| University of Texas at Houston | Academic/Hospital | 3 | 3 | 1 | 2015 |
| AstraZeneca | For profit | 2 | 0 | 1 | 2016 |
| Bristol-Myers Squibb | For profit | 2 | 0 | 1 | 2016 |
| Georgetown University | Academic/Hospital | 2 | 2 | 2 | 2019 |
| Harvard University | Academic/Hospital | 2 | 1 | 1 | 2011 |
| National Cancer Institute (NCI) | Government | 2 | 1 | 2 | 2020 |
| Roche | For profit | 2 | 0 | 1 | 2017 |
| University of California, San Francisco | Academic/Hospital | 2 | 1 | 2 | 2010 |
| University of South Florida | Academic/Hospital | 2 | 1 | 1 | 2014 |
| University of Utah | Academic/Hospital | 2 | 0 | 2 | 2010 |
| Alzheimer's Association | Academic/Hospital | 1 | 0 | 1 | 2019 |
| American Society of Clinical Oncology | Academic/Hospital | 1 | 1 | 1 | 2016 |
| Ascentage Pharma Group Inc. | For profit | 1 | 1 | 1 | 2024 |
| Augusta University | Academic/Hospital | 1 | 1 | 1 | 2017 |
| Avillion | For profit | 1 | 1 | 1 | 2014 |
| Bayer | For profit | 1 | 0 | 1 | 2016 |
| Baylor University | Academic/Hospital | 1 | 1 | 1 | 2020 |
Marketing (5)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Alembic | For profit | MKTG | May 23, 2025 |
| MSN Laboratories | For profit | MKTG | May 28, 2025 |
| Pfizer | For profit | NDA2 | Sep 4, 2012 |
| Sun Pharmaceuticals | For profit | MKTG | Aug 25, 2023 |
| Wyeth | For profit | NDA | Sep 4, 2012 |