Dasatinib is an oral targeted medicine used to treat chronic myeloid leukaemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukaemia (Ph+ ALL). It belongs to a class of medicines called second-generation BCR-ABL tyrosine kinase inhibitors, generally more potent than imatinib and used both as first-line treatment and after imatinib resistance or intolerance. It is a prescription-only medicine.

• Therapeutic Class: Anti-cancer (oncology) targeted therapy.

• Pharmacological Class: BCR-ABL tyrosine kinase inhibitor, second-generation (also inhibits SRC family kinases, KIT, PDGFR).

• Drug Family: Second-generation small-molecule tyrosine kinase inhibitors.

• ATC Classification: L01EA02 (Dasatinib).

Approved: Newly diagnosed Philadelphia chromosome-positive (Ph+) chronic-phase CML in adults and children; chronic-, accelerated-, or myeloid/lymphoid blast-phase CML with resistance or intolerance to prior therapy including imatinib; and Ph+ acute lymphoblastic leukaemia with resistance or intolerance to prior therapy.

Commonly used for: Patients starting first-line CML treatment where a more potent option is preferred, and patients whose CML has stopped responding to or who cannot tolerate imatinib.

Off-label use (only under medical guidance): Being studied in other BCR-ABL- or SRC-family-kinase-driven conditions in clinical trials; not routine outside its approved indications.

• Oral tablets: 20 mg, 50 mg, 70 mg, 80 mg, 100 mg, and 140 mg.

Like imatinib, dasatinib blocks the abnormal BCR-ABL protein that drives CML, but it does so roughly 300-fold more potently in laboratory studies and also blocks additional proteins (SRC family kinases, KIT, PDGFR), which may explain its effectiveness in some patients whose leukaemia has developed resistance to imatinib. This more thorough blockade of the abnormal growth signal helps control or reduce the leukaemia cell population.

• Standard dose (chronic-phase CML): 100 mg orally once daily, whether used first-line or after imatinib resistance/intolerance (a lower starting dose than the original approval, based on later dosing studies).

• Condition-wise dose (accelerated/blast-phase CML or Ph+ ALL): 140 mg orally once daily.

• Route: Oral, once daily, at approximately the same time each day, with or without food; tablets should be swallowed whole and not crushed or split.

• Missed dose: If more than 12 hours have passed since the missed dose was due, skip it and take the next dose at the regular scheduled time; don't double up.

• Overdose: May worsen known side effects such as fluid retention, bleeding, or low blood counts; requires medical attention.

• Common: Fluid retention (including pleural effusion, a build-up of fluid around the lungs, more specifically associated with dasatinib than with imatinib), headache, diarrhoea, fatigue, muscle/joint pain, and low blood counts.

• Serious: Significant pleural effusion, pulmonary arterial hypertension (a serious lung blood pressure condition, potentially not fully reversible), significant bleeding events, QT interval prolongation, and cardiac effects (including, rarely, heart failure).

• Emergency symptoms: Significant shortness of breath or chest pain (possible pleural effusion or heart-related issue), unusual bleeding, or a fainting episode.

• Recovery advice: Because pleural effusion is a distinctive risk with dasatinib, new or worsening breathlessness should always be reported promptly; regular blood counts and clinical review help catch other effects early.

• Pregnancy: Can cause fetal harm; effective contraception is recommended during treatment.

• Breastfeeding: Not recommended during treatment.

• Liver disease: Used with caution and monitoring.

• Kidney disease: Used with caution; dose adjustment may be needed in significant impairment.

• Elderly: Used with routine monitoring; fluid-related and cardiac side effects may warrant closer observation.

• Children: Approved for pediatric Ph+ CML, with body-surface-area-based dosing.

• Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin): can significantly increase dasatinib levels; avoided or requires dose adjustment.

• Strong CYP3A4 inducers (e.g., rifampin): can significantly reduce dasatinib levels and effectiveness.

• Acid-reducing medicines (proton pump inhibitors, H2 blockers, antacids): reduce dasatinib absorption, since it requires an acidic stomach environment; proton pump inhibitors are generally avoided, and antacids should be separated by several hours.

• Other QT-prolonging medicines or anticoagulants/antiplatelet drugs: increase the risk of heart rhythm effects or bleeding when combined with dasatinib.

• Complete blood counts every 2 weeks for the first 12 weeks, then periodically thereafter.

• Chest examination and imaging if pleural effusion is suspected, given new or worsening breathing symptoms.

• Cardiac assessment (ECG, and echocardiogram if pulmonary hypertension is suspected) at baseline and as clinically indicated.

• BCR-ABL molecular monitoring to track CML treatment response over time.

Imatinib, Nilotinib, Bosutinib, Asciminib (other BCR-ABL tyrosine kinase inhibitors, used first-line or after resistance/intolerance to a specific agent).

Used as monotherapy in CML settings; sometimes combined with chemotherapy in Ph+ ALL treatment protocols, under specialist hematology-oncology guidance.

• Chronic Myeloid Leukaemia (CML) Medicines

• Philadelphia Chromosome-Positive ALL Treatments

• BCR-ABL Tyrosine Kinase Inhibitors

1. Skin Rashes And Leukemia

2. Leukemia And Its Risk In Children Having Down Syndrome

• https://www.cancernetwork.com/view/fda-approves-lower-starting-dose-dasatinib-cml

• https://pmc.ncbi.nlm.nih.gov/articles/PMC5901015/

The information on this page is for educational purposes only and is not a substitute for medical advice. Please consult your oncologist to know if this treatment is appropriate for your condition.