Drug reference

Dasatinib

Tyrosine Kinase Inhibitor · Antineoplastic

Also known as Sprycel

Tyrosine Kinase InhibitorAntineoplastic

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

FDA category + note

Top interactionssee all 12 →

AbciximabSevereDatabaseDDInter
AcalabrutinibSevereDatabaseDDInter
AdalimumabSevereDatabaseDDInter
AlteplaseSevereDatabaseDDInter

Mechanism

Dasatinib is a protein tyrosine kinase inhibitor. It works by inhibiting the activity of various kinases, including BCR-ABL. This inhibition leads to the suppression of cell proliferation and induction of apoptosis in leukemic cells expressing the BCR-ABL fusion protein, making it effective in chronic myeloid leukemia and acute lymphoblastic leukemia.

Indications

Chronic phase chronic myeloid leukaemia (initiated by a specialist)Accelerated and blast phase chronic myeloid leukaemia [resistant or intolerant to prior therapy] (initiated by a specialist)Acute lymphoblastic leukaemia [resistant or intolerant to prior therapy] (initiated by a specialist)CML with resistance to or intolerance of imatinib (in both chronic and advanced phases)Ph+ ALL (in combination with cytotoxic chemotherapy) who are resistant or intolerant to prior therapiesAll phases of CML

Dosing

Adult: Chronic phase chronic myeloid leukaemia (BY MOUTH USING TABLETS): Initially 100 mg once daily, then increased if necessary up to 140 mg once daily. Chronic phase chronic myeloid leukaemia (BY MOUTH USING ORAL SUSPENSION): Adult (body-weight 30–44 kg): 105 mg once daily; adjust dose based on changes in body-weight every 3 months or more often if necessary.…
Max dose: 180 mg once daily

Pharmacokinetics

Half-life

3 to 5 h (plasma)

Bioavailability

well absorbed (oral); significantly reduced at neutral gastric pH

Metabolism

CYP3A4 (primarily), FMO3 (minor), UGT (minor)

Side effects

Common

Alopeciaanaemiaappetite abnormalarrhythmiasarthralgiaastheniabone marrow depressioncardiac disordercardiomyopathychest painchillsconstipationcoughdepressiondiarrhoeadizzinessdrowsinessdry eyedyspnoeaeye in ammationfacial swellingfeveru id imbalanceu shinggastrointestinal discomfortgastrointestinal disordersgenital abnormalitieshaemorrhageheadacheheart failurehypertensionhyperuricaemiaincreased risk of infectioninsomniamiliamucositismuscle complaintsmuscle weaknessmusculoskeletal stiffnessmyocardial dysfunctionnauseanerve disordersneutropeniaoedemaoral disordersGI symptoms (diarrhea, nausea, vomiting)fluid retentionedemaperiorbital swellingmyelosuppression (20–30%)thrombocytopeniapleural effusions (10–25%)pericardial effusions (≤5%)

Serious

Hepatitis B virus reactivation
Cardiac dysfunction
QT-interval prolongation
myelosuppression
hepatotoxicity
pleural effusions
pulmonary hypertension
QT interval prolongation
pulmonary hypertension (<5%)
recurrent pleural effusions
vasospastic or vaso-occlusive events
immune-mediated events (pneumonitis, myocarditis, pericarditis, hepatitis, nephritis)