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Therapy Name | Bosutinib |
Synonyms | |
Therapy Description |
Bosulif (bosutinib) inhibits SRC and ABL kinases, and has additional activity against other kinases including AXL, TNK2, BTK, resulting in decreased pathway activation and inhibition of tumor cell proliferation (PMID: 12543790, PMID: 19039322, PMID: 26555154). Bosulif (bosutinib) is FDA approved for use in patients with Ph+ (BCR-ABL) chronic myelogenous leukemia (FDA.gov). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
Bosutinib | Bosulif | SKI-606|PF-5208763 | ABL Inhibitor (pan) 8 AXL Inhibitor 27 BTK inhibitor 24 SRC Inhibitor 29 TNK2 Inhibitor 6 | Bosulif (bosutinib) inhibits SRC and ABL kinases, and has additional activity against other kinases including AXL, TNK2, BTK, resulting in decreased pathway activation and inhibition of tumor cell proliferation (PMID: 12543790, PMID: 19039322, PMID: 26555154). Bosulif (bosutinib) is FDA approved for use in patients with Ph+ (BCR-ABL) chronic myelogenous leukemia (FDA.gov). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
SRC positive | biliary tract cancer | sensitive | Bosutinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Bosulif (bosutinib) inhibited Src signaling, resulted in cell cycle arrest and decreased invasion of biliary tract cancer cell lines in culture, and delayed tumor growth in cell line xenograft models (PMID: 27196758). | 27196758 |
ABL1 rearrange | myeloid neoplasm | sensitive | Bosutinib | Guideline | Actionable | Bosulif (bosutinib) is included in guidelines for patients with a myeloid/lymphoid neoplasm with eosinophilia harboring an ABL1 rearrangement (NCCN.org). | detail... |
SRC positive | Advanced Solid Tumor | predicted - sensitive | Bosutinib | Preclinical - Cell culture | Actionable | In a preclinical study, Bosulif (bosutinib) inhibited invasion and migration of Src-positive cells in culture (PMID: 18483306). | 18483306 |
Unknown unknown | Advanced Solid Tumor | not applicable | Bosutinib | Phase I | Actionable | In a Phase I trial, Bosulif (bosutinib) demonstrated safety and limited efficacy in patients with advanced solid tumors (PMID: 22179664). | 22179664 |
Unknown unknown | chronic myeloid leukemia | not applicable | Bosutinib | Clinical Study | Actionable | In a meta-analysis, Bosulif (bosutinib) treatment was associated with increased rate of major molecular response compared with Gleevec (imatinib) (Odds Ratio (OR): 1.86 [1.29-2.70]), but not improved overall survival (OR: 2.38 [0.82-6.89]), and was associated with a trend toward increased risk of vascular occlusive events in chronic myeloid leukemia patients (PMID: 26847662). | 26847662 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
---|---|---|---|---|---|---|
NCT04258943 | Phase Ib/II | Bosutinib | Bosutinib in Pediatric Patients With Newly Diagnosed Chronic Phase or Resistant/Intolerant Ph + Chronic Myeloid Leukemia", | Recruiting | USA | 0 |
NCT01331291 | Phase II | Bosutinib | Bosutinib in Adult Patients With Recurrent Glioblastoma | Completed | USA | 0 |
NCT03106779 | Phase III | Bosutinib Asciminib | Study of Efficacy of CML-CP Patients Treated With ABL001 Versus Bosutinib, Previously Treated With 2 or More TKIs | Active, not recruiting | USA | CAN | 23 |
NCT03297606 | Phase II | Bosutinib Palbociclib Vismodegib Ipilimumab + Nivolumab Cobimetinib + Vemurafenib Temsirolimus Olaparib Erlotinib Crizotinib Sunitinib Afatinib Dasatinib Pertuzumab + Trastuzumab Axitinib | Canadian Profiling and Targeted Agent Utilization Trial (CAPTUR) (CAPTUR) | Recruiting | CAN | 0 |
NCT02130557 | Phase III | Bosutinib Imatinib | A Multicenter Phase 3, Open-Label Study of Bosutinib Versus Imatinib in Adult Patients With Newly Diagnosed Chronic Phase Chronic Myelogenous Leukemia | Completed | USA | CAN | 24 |
NCT01903733 | Phase I | Bosutinib | Bosutinib Treatment Extension Study Only For Subjects With Chronic Myeloid Leukemia (CML) Who Have Previously Participated In Bosutinib Studies B1871006 Or B1871008 | Active, not recruiting | USA | CAN | 27 |
NCT03654768 | Phase II | Bosutinib Dasatinib Nilotinib Dasatinib + Ruxolitinib Bosutinib + Ruxolitinib Nilotinib + Ruxolitinib | Testing the Addition of Ruxolitinib to the Usual Treatment (Tyrosine Kinase Inhibitors) for Chronic Myeloid Leukemia | Recruiting | USA | 0 |
NCT02906696 | Phase II | Bosutinib | Bosutinib Dose-Optimization Study in Chronic Myeloid Leukemia (CML) | Terminated | USA | 0 |
NCT02551718 | Phase I | Bosutinib Irinotecan Romidepsin Busulfan Melphalan Nilotinib Crizotinib Cytarabine Mitoxantrone Dasatinib Pazopanib Paclitaxel Clofarabine Hydroxyurea Tretinoin Carfilzomib Nelarabine Bexarotene Pentostatin Everolimus Cabozantinib Mercaptopurine Methotrexate Cladribine Thioguanine Daunorubicin Ponatinib Etoposide Afatinib Gefitinib Gemcitabine Regorafenib Arsenic trioxide Trametinib Imatinib Erlotinib Dabrafenib Decitabine Axitinib Azacitidine Ruxolitinib Fludarabine Lapatinib Ceritinib Sirolimus Sorafenib Lomustine Sunitinib Cabazitaxel Temsirolimus Topotecan Bortezomib Pralatrexate | High Throughput Drug Sensitivity Assay and Genomics- Guided Treatment of Patients With Relapsed or Refractory Acute Leukemia | Active, not recruiting | USA | 0 |
NCT02228382 | FDA approved | Bosutinib | Safety And Efficacy Study Of Bosutinib In Patients With Philadelphia Chromosome Positive Chronic Myeloid Leukemia Previously Treated With One Or More Tyrosine Kinase Inhibitors | Completed | USA | 7 |