Active Pharmaceutical Ingredients

Catalog ID80071716

CAS NO.380843-75-4

Purity 99%

MDL NumberMFCD07367846

Molecular FormulaC26H29Cl2N5O3

Molecular Weight530.453

Melting point: 116-120 °C

Item	Information
Mechanism of Action	Bosutinib is a dual tyrosine kinase inhibitor targeting both BCR-ABL1 and SRC-family kinases (e.g., SRC, Lyn, Hck). It inhibits BCR-ABL1 at concentrations of 25–50 nM, preventing tyrosine phosphorylation and demonstrating anti-proliferative activity against chronic myeloid leukemia (CML) cells. It also inhibits SRC with an IC₅₀ of 1.2 nM, blocking pathways involved in cell proliferation, angiogenesis, and metastasis.
Indications	– Treatment of chronic phase (CP) Philadelphia chromosome-positive chronic myelogenous leukemia (Ph⁺ CML) in adults and pediatric patients aged 1 year and older, whether newly diagnosed or resistant/intolerant to prior therapy.<br>- Treatment of accelerated phase (AP) or blast phase (BP) Ph⁺ CML in adults with resistance or intolerance to prior therapy.
Dosing Considerations	– Newly-diagnosed CP Ph⁺ CML (Adults): 400 mg orally once daily with food.<br>- Resistant/Intolerant CP, AP, or BP Ph⁺ CML (Adults): 500 mg orally once daily with food.<br>- Pediatric Patients: Doses range from 150 mg to 500 mg based on body surface area (BSA), with specific dosing tables available.<br>- Missed Dose: If a dose is missed beyond 12 hours, skip the missed dose and take the next scheduled dose.<br>- Dose Adjustments: Lower starting doses (200–300 mg) may be used in patients with comorbidities or prior intolerance, with gradual escalation to standard doses.
Pharmacokinetics	– Absorption: Oral administration with food.<br>- Peak Concentration (Tmax): 4–6 hours.<br>- Half-life: 22.5 hours.<br>- Metabolism: Primarily via CYP3A4.<br>- Excretion: Mostly in feces, with only 1% excreted in urine.
Special Precautions	– Avoid concurrent use with strong or moderate CYP3A inhibitors or inducers.<br>- Monitor for gastrointestinal toxicity, vascular toxicity, fluid retention, and renal toxicity.<br>- Use with caution in patients with hepatic or renal impairment.<br>- Regular monitoring of blood counts and liver function is recommended.
Patient Education	– Take with food to enhance absorption.<br>- Do not cut, crush, or chew tablets.<br>- Report any persistent side effects or signs of infection.

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