dasatinib

Dasatinib is an oral small-molecule tyrosine kinase inhibitor used in the treatment of certain leukemias. It potently inhibits BCR-ABL1, the fusion oncoprotein driving chronic myeloid leukemia and some Philadelphia chromosome–positive acute lymphoblastic leukemia, and also targets Src family kinases, PDGFR-β, c-KIT and EPHA2. By suppressing BCR-ABL–mediated signaling, dasatinib reduces leukemic cell proliferation and promotes apoptosis.

Indications include Philadelphia chromosome–positive chronic myeloid leukemia in chronic, accelerated, and blast phases, and Philadelphia chromosome–positive ALL. It is used in patients with resistance or intolerance to prior therapies, including imatinib, and has been employed as first-line therapy in certain settings depending on regulatory approvals.

Dasatinib is administered orally, with dosing regimens varying by disease phase and tolerability. Typical starting doses include 100 mg once daily for chronic-phase CML, with higher doses or divided dosing used for advanced disease or ALL. Dose adjustments are made for cytopenias, adverse reactions, and drug interactions. The drug can be taken with or without food, but regimen-specific instructions should be followed.

Pharmacokinetics are influenced by hepatic metabolism, primarily via CYP3A4. Co-administration with strong CYP3A4 inhibitors raises dasatinib exposure, while inducers lower it. Strong CYP3A4 inhibitors and inducers require caution or adjustment; grapefruit-containing products should be avoided.

Common adverse effects include cytopenias (neutropenia, thrombocytopenia), edema and pleural effusion, diarrhea, rash, and fatigue. Serious risks include QT prolongation, hepatic injury, infections, bleeding, and pulmonary or cardiac toxicity. Monitoring of blood counts and liver function is recommended, with attention to signs of pleural effusion or cardiac symptoms.

The brand name Sprycel is associated with dasatinib. Resistance can occur with mutations such as T315I, which may necessitate alternative therapies.

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