Products
Bosutinib is commercially available in the form of film-coated tablets (Bosulif). The drug was approved in many countries in 2014.
Structure and properties
Bosutinib (C26H29Cl2N5O3, Mr = 530.4 g/mol) is a quinoline and piperazine derivative. It is present in drugs as bosutinib monohydrate, a white to yellowish powder that is sparingly soluble in water.
Effects
Bosutinib (ATC L01XE14) has antiproliferative and selective cytostatic properties. It binds to BCR-ABL kinase in chronic myeloid leukemia, inhibiting cell proliferation. It is also effective against imatinib-resistant forms of BCR-ABL kinase and against Src, Lyn and Hck kinases. It has a long half-life of approximately 33 hours.
Indications
As a second-line agent for the treatment of chronic myeloid leukemia (Ph+CML).
Dosage
According to the SmPC. Tablets are usually taken once daily with a meal.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Bosutinib is metabolized predominantly by CYP3A4 and is a substrate of P-glycoprotein. Corresponding drug-drug interactions with CYP or P-gp inhibitors and CYP inducers are possible. Proton pump inhibitors may decrease concentrations of bosutinib and should not be administered concomitantly.
Adverse Effects
The most common possible adverse effects include diarrhea, nausea and vomiting, abdominal pain, pain, rash, thrombocytopenia, anemia, fever, and fatigue.
