Dasatinib

Plasma peak time: 0.5 to 6 hours
Plasma peak concentration: 82.2 ng/ml (with a daily dose of 100 mg)
AUC: 397 ng/ml per hour (with a daily dose of 100 mg)
A high-fat meal increased the mean AUC following a 100 mg dose by 14%
Protein binding: 96% (dasatinib); 93% (active metabolite)
Distribution volume: 2505 liters
Metabolism: Mainly metabolized by CYP3A4
Inhibited enzymes: CYP3A4 (weak)
Dasatinib is a P-gp substrate
Half-life: 3 to 5 hours
Clearance: 363.8 liters per hour
Excretion: feces (85%); Urine (4%)

Therapeutic Fields​

Dosage Form

Tablet 20,50,70,80,100 mg

Mechanism of action

Dasatinib is a BCR-ABL tyrosine kinase inhibitor that targets most imatinib-resistant BCR-ABL mutations (except T315I and F317V mutations) by distinctly binding to active and inactive ABL-kinase. Kinase inhibition stops the proliferation of leukemia cells. It also inhibits the SRC family (including SRC, LKC, YES, FYN) and c-KIT, EPHA2, and platelet-derived growth factor receptor (PDGFRβ).

Uses of Dasatinib

Acute lymphoblastic leukemia, chronic myelogenous leukemia
Chronic myeloid leukemia
– Acute lymphoblastic leukemia

Method of Use

Chronic myeloid leukemia
1- Newly diagnosed:
Start with 100 mg once a day (morning or evening)
In case of insufficient response, it may be increased to 140 mg/day
2- Advanced
It is used for the treatment of chronic and severe and explosive myeloid and lymphoid phase in Ph + CML with resistance or intolerance to previous treatments including imatinib.
Start with 140 mg daily
If there is no adequate response, it may be increased to 180 mg per day
– Acute lymphoblastic leukemia
It is used for acute lymphoblastic leukemia (ALL) with positive Philadelphia chromosome with resistance or intolerance to previous treatment.
Start with 140 mg daily
In case of insufficient response, it may be increased to 180 mg/day