Dasatinib

What it is and how it works

Mechanism of Action Dasatinib, at nanomolar concentrations, inhibits the following kinases: BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ. Based on modeling studies, dasatinib is predicted to bind to multiple conformations of the ABL kinase. In vitro , dasatinib was active in leukemic cell lines representing variants of imatinib mesylate‑-sensitive and resistant disease. Dasatinib inhibited the growth of chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL) cell lines overexpressing BCR-ABL.

Indications

Dasatinib tablets are indicated for the treatment of adult patients with newly diagnosed Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) in chronic phase. chronic, accelerated, or myeloid or lymphoid blast phase Ph+ CML with resistance or intolerance to prior therapy including imatinib. Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL) with resistance or intolerance to prior therapy. Dasatinib tablets are indicated for the treatment of pediatric patients 1 year of age and older with Ph+ CML in chronic phase. newly diagnosed Ph+ ALL in combination with chemotherapy. Dasatinib tablets are a kinase inhibitor indicated for the treatment of newly diagnosed adults with Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) in chronic phase. ( 1 , 14 ) adults with chronic, accelerated, or myeloid or lymphoid blast phase Ph+ CML with resistance or intolerance to prior therapy including imatinib.

Dosage and administration (summary)

Chronic phase CML in adults: 100 mg once daily. Accelerated phase CML, myeloid or lymphoid blast phase CML, or Ph+ ALL in adults: 140 mg once daily. Chronic phase CML and ALL in pediatrics: starting dose based on body weight. Administer orally, with or without a meal. Do not crush, cut, or chew tablets. Dosage of Dasatinib Tablets in Adult Patients The recommended starting dosage of dasatinib tablets for chronic phase CML in adults is 100 mg administered orally once daily. The recommended starting dosage of dasatinib tablets for accelerated phase CML, myeloid or lymphoid blast phase CML, or Ph+ ALL in adults is 140 mg administered orally once daily.

Contraindications

None. None.

Warnings and precautions

Myelosuppression and Bleeding Events: Severe thrombocytopenia, neutropenia, and anemia may occur. Use caution if used concomitantly with medications that inhibit platelet function or anticoagulants. Monitor complete blood counts regularly. Transfuse and interrupt dasatinib tablets when indicated. ( 2.5 , 5.1 , 5.2 ) Fluid Retention: Fluid retention, sometimes severe, including pleural effusions. Manage with supportive care measures and/or dose modification. ( 2.5 , 5.3 ) Cardiovascular Toxicity: Monitor patients for signs or symptoms and treat appropriately.

Pregnancy

Pregnancy Risk Summary Based on limited human data, dasatinib can cause fetal harm when administered to a pregnant woman. Adverse pharmacologic effects including hydrops fetalis, fetal leukopenia, and fetal thrombocytopenia have been reported with maternal exposure to dasatinib.

Storage and supply

How Supplied Dasatinib tablets are available as described in Table 21. Table 21: Dasatinib Tablets Trade Presentations NDC Number Strength Description Tablets per Bottle 68001-660-06 20 mg White to off-white, biconvex, round, film-coated tablet with “D8” debossed on one side and plain on the other side and free from physical defects.

Source: Dasatinib (Dasatinib) — US FDA prescribing information, 2026-03-05, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.