Dasatinib is a second-generation, oral, multi-targeted tyrosine kinase inhibitor (TKI) used primarily in the treatment of Philadelphia chromosome-positive (Ph+) leukemias. It is a potent inhibitor of BCR-ABL, SRC family kinases, c-KIT, EPHA2, and PDGFR-β. In the Indian context, it is a critical therapy for chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL), especially in cases of resistance or intolerance to first-line imatinib therapy.
Adult: CML-CP & Ph+ ALL: 100 mg once daily. CML-AP/BP: 140 mg once daily. Dose adjustments are based on response and tolerability. The 50mg tablet allows for flexible dosing adjustments (e.g., 50mg twice daily, 70mg twice daily using combinations).
Note: Swallow tablet whole with a full glass of water. Can be taken with or without food, but avoid high-fat meals as they increase exposure. Should be taken at the same time each day. DO NOT crush, split, or chew the tablet. If a dose is missed, take the next scheduled dose at the regular time. Do not take two doses at the same time.
Dasatinib is a potent, ATP-competitive inhibitor of multiple tyrosine kinases. Its primary target is the BCR-ABL oncoprotein, the constitutively active tyrosine kinase responsible for Philadelphia chromosome-positive leukemias. It binds to both the active and inactive conformations of the ABL kinase domain.
Pregnancy: Category D: Dasatinib can cause fetal harm. It is embryotoxic and teratogenic in animal studies. Women of childbearing potential must use effective contraception during and for at least 30 days after therapy. If pregnancy occurs, patient should be apprised of the potential risk.
Driving: May cause dizziness, fatigue, or blurred vision. Patients should be cautioned about operating machinery or driving until they know how dasatinib affects them.
| Strong CYP3A4 Inhibitors (e.g., Ketoconazole, Itraconazole, Clarithromycin, Ritonavir) | Significantly increase dasatinib plasma concentration, increasing toxicity risk. | Major |
| Strong CYP3A4 Inducers (e.g., Rifampicin, Phenytoin, Carbamazepine, St. John's Wort) | Significantly decrease dasatinib plasma concentration, leading to potential therapeutic failure. | Major |
| Antacids, H2 Blockers (e.g., Famotidine), Proton Pump Inhibitors (e.g., Omeprazole) | Increase gastric pH, reducing dasatinib solubility and absorption. Avoid concomitant use. | Major |
| Anticoagulants/Antiplatelets (e.g., Warfarin, Clopidogrel) | Increased risk of hemorrhage due to dasatinib's effect on platelets. Use with caution; monitor INR closely. | Moderate |
| Simvastatin, Lovastatin | Increased risk of myopathy/rhabdomyolysis as both are CYP3A4 substrates. | Moderate |