Drug reference

Bosutinib

Tyrosine Kinase Inhibitor · Antineoplastic

Tyrosine Kinase InhibitorAntineoplastic

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

FDA category + note

Top interactionssee all 12 →

AdalimumabSevereDatabaseDDInter
AmiodaroneSevereDatabaseDDInter
AmisulprideSevereDatabaseDDInter
AmprenavirSevereDatabaseDDInter

Mechanism

Bosutinib inhibits Bcr-Abl tyrosine kinase and retains activity against imatinib-resistant Bcr-Abl mutations, with the exception of T315I and V299L mutations. It also inhibits Src family tyrosine kinases. This dual inhibition targets key pathways involved in the proliferation of chronic myeloid leukemia cells.

Indications

Previously treated chronic, accelerated and blast phase Philadelphia chromosome-positive chronic myeloid leukaemia (specialist use only)Newly-diagnosed chronic phase Philadelphia chromosome-positive chronic myeloid leukaemia (specialist use only)chronic, accelerated, or blast-phase Ph+ CML with resistance or intolerance to prior therapyAll phases of CML

Dosing

Adult: Previously treated chronic, accelerated and blast phase Philadelphia chromosome-positive chronic myeloid leukaemia: 500 mg once daily, consult product literature for dose adjustment due to side-effects, or incomplete haematologic response by week 8, or incomplete cytogenetic response by week 12.…

Contraindications

Hepatitis B infection (risk of reactivation, status should be established before treatment initiation)

Side effects

Common

Nausea and vomitingDiarrheadiarrhea (>20%)nausea (>20%)thrombocytopenia (>20%)vomiting (>20%)abdominal pain (>20%)rash (>20%)anemia (>20%)pyrexia (>20%)fatigue (>20%)liver toxicityrenal dysfunctionearly and self-limited gastrointestinal adverse events (diarrhea, nausea, vomiting)

Serious

Fluid retention
Myelosuppression
Skin rash
Hepatotoxicity
Hepatitis B virus reactivation
QT prolongation
Pancreatitis (if lipase elevated and abdominal symptoms occur)
Visual disturbances
Increased blood pressure
Elevated creatine kinase and creatinine levels
severe colitis
renal dysfunction
renal failure
arterio-occlusive events (lower incidence compared to ponatinib, nilotinib, dasatinib)