Products
Dasatinib is commercially available in the form of film-coated tablets (Sprycel). It has been approved in many countries since 2007. Generic versions were registered in 2020.
Structure and properties
Dasatinib (C22H26ClN7O2S, Mr = 488.0 g/mol) exists as a white powder that is insoluble in water. It is an aminopyrimidine derivative.
Effects
Dasatinib (ATC L01XE06) is antiproliferative and selectively cytostatic. It binds competitively to the ATP-binding site of BCR-ABL kinase in chronic myeloid leukemia, inhibiting cell proliferation. Dasatinib also inhibits other tyrosine kinases, namely those of c-Kit, EPH and PDGFβ. Dasatinib is also partially active in patients who are resistant or intolerant to imatinib, for example, because of BCR-ABL muation.
Indications
For the treatment of chronic myeloid leukemia (Ph+CML) and acute lymphoblastic leukemia (Ph+ALL).
Dosage
According to the SmPC. Tablets are taken once daily, independent of meals. Hands should be washed well after contact with the tablets. Caution should be exercised when handling the tablets because it is a cytostatic drug (see the Instructions for Use).
Contraindications
- Hypersensitivity
- Pregnancy and lactation
Full precautions can be found in the drug label.
Interactions
Dasatinib is a substrate of CYP3A4 and P-glycoprotein and an inhibitor of CYP3A4 and CYP2C8. Corresponding drug-drug interactions are possible and should be considered.
Adverse effects
The most common potential adverse effects include digestive symptoms such as diarrhea, nausea, vomiting, abdominal pain, rash, bleeding, hypophosphatemia, infectious disease, headache, muscle pain, bone pain, fatigue, edema, fever, pleural effusion, respiratory insufficiency, and blood count changes.