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Bosulif (Bosutinib Monohydrate)
Bosulif blocks the abnormal tyrosine kinase activity in cancer cells, inhibiting their growth and proliferation.
Bosulif (Bosutinib Monohydrate) is a small molecule kinase inhibitor originally developed by Wyeth Pharms Inc and currently owned by Pf Prism Cv. It targets the Tyrosine-protein kinase ABL1 and is FDA approved for the treatment of Blastic phase chronic myeloid leukemia and Chronic Myelocytic Leukemia Accelerated Phase. Bosulif works by blocking the abnormal tyrosine kinase activity in cancer cells, thereby inhibiting their growth and proliferation. The commercial status of Bosulif is patented, with a single generic manufacturer available. Key safety considerations include potential side effects such as diarrhea, nausea, and fatigue.
At a glance
| Generic name | Bosutinib Monohydrate |
|---|---|
| Sponsor | Pfizer |
| Drug class | Kinase Inhibitor |
| Target | Tyrosine-protein kinase ABL1 |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
| First approval | 2012 |
| Annual revenue | 611 |
Mechanism of action
Bosutinib is tyrosine kinase inhibitor. Bosutinib inhibits the Bcr-Abl kinase that promotes CML; it is also an inhibitor of Src-family kinases including Src, Lyn, and Hck. Bosutinib inhibited 16 of 18 imatinib-resistant forms of Bcr-Abl expressed in murine myeloid cell lines. Bosutinib did not inhibit the T315I and V299L mutant cells. In mice, treatment with bosutinib reduced the size of CML tumors relative to controls and inhibited growth of murine myeloid tumors expressing several imatinib-resistant forms of Bcr-Abl.
Approved indications
- Blastic phase chronic myeloid leukemia
- Chronic Myelocytic Leukemia Accelerated Phase
Common side effects
- Diarrhea
- Hepatic dysfunction
- Rash
- Nausea
- Abdominal pain
- Vomiting
- Fatigue
- Respiratory tract infection
- Pyrexia
- Headache
- Creatinine increased
- Hemoglobin decreased
Drug interactions
- P-glycoprotein Substrates
- amprenavir
- aprepitant
- atazanavir
- boceprevir
- bosentan
- carbamazepine
- ciclosporin
- cimetidine
- ciprofloxacin
- clarithromycin
- conivaptan
Key clinical trials
- Canadian Profiling and Targeted Agent Utilization Trial (CAPTUR) (PHASE2)
- A Study of Oral Asciminib Versus Other TKIs in Adult Patients With Newly Diagnosed Ph+ CML-CP (PHASE3)
- Asciminib Roll-over Study (PHASE4)
- Treatment Free Remission After Combination Therapy With Ruxolitinib Plus Tyrosine Kinase Inhibitors (PHASE2)
- Safety And Efficacy Of TKI Cessation For CML Patients With Stable Molecular Response In A Real World Population (PHASE2)
- Testing the Addition of Ruxolitinib to the Usual Treatment (Tyrosine Kinase Inhibitors) for Chronic Myeloid Leukemia (PHASE2)
- A Study to Learn About the Study Medicine Bosulif in Adult Patients With Chronic Myeloid Leukemia(CML).
- Treatment Patterns and Outcomes Among Patients With Chronic Myeloid Leukemia (CML) in All Lines of Treatment
Patents
| Patent | Expiry | Type |
|---|---|---|
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |
| SEC EDGAR | Revenue + earnings |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Bosulif CI brief — competitive landscape report
- Bosulif updates RSS · CI watch RSS
- Pfizer portfolio CI