Dasatinib
- Atc Codes:L01XE06
- CAS Codes:863127-77-9
- PHARMGKB ID:863127-77-9
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Sprycel; Belgium: Sprycel; Bulgaria: Sprycel; Czech Republic: Sprycel; Denmark: Sprycel; Estonia: Sprycel; Finland: Sprycel; France: Sprycel; Germany: Sprycel; Greece: Sprycel; Hungary: Sprycel; Ireland: Sprycel; Italy: Sprycel; Latvia: Sprycel; Lithuania: Sprycel; Luxembourg: Sprycel; Malta: Sprycel; Netherlands: Sprycel; Poland: Sprycel; Portugal: Sprycel; Romania: Sprycel; Slovakia: Sprycel; Slovenia: Sprycel; Spain: Sprycel; Sweden: Sprycel; UK: Sprycel.
North America
Canada: Sprycel; USA: Sprycel.
Latin America
Argentina: Sprycel.
Drug combinations
Chemistry
Dasatinib: C~22~H~26~ClN~7~O~2~S H~2~O. Mw: 506.00. (1) 5-Thiazolecarboxamide-N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-, monohydrate; (2) N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl]amino]thiazole-5-carboxamide hydrate. CAS-863127-77-9 (2005).
Pharmacologic Category
Other Antineoplastic Agents; Protein Kinase Inhibitors. Tyrosine Kinase Inhibitor. (ATC-Code: L01XE06).
Mechanism of action
BCR-ABL tyrosine kinase inhibitor, targets most imatinib-resistant BCR-ABL mutations (except the T315I and F317V mutants) by distinctly binding to ABL-kinase. Kinase inhibition halts proliferation of leukemia cells. Also inhibits SRC family (including SRC, LKC, YES, FYN), c-KIT, EPHA2 and platelet-derived growth factor receptor (PDGFRβ).
Therapeutic use
Treatment of chronic myelogenous leukemia (CML) in chronic, accelerated or blast (myeloid or lymphoid) phase, resistant or intolerant to prior therapy. Treatment of Philadelphia chromosome-positive (Ph+) acute lymphoblastic leukemia (ALL) resistant or intolerant to prior therapy.
Pregnancy and lactiation implications
May cause fetal harm if administered to a pregnant woman. Not recommended during pregnancy or lactation.
Unlabeled use
Contraindications
Hypersensitivity to dasatinib or any other component of the formulation.
Warnings and precautions
Bone marrow suppression (neutropenia, anemia, or thrombocytopenia) reported, mainly in advanced CML and Ph+ ALL. May cause fluid retention (i.e. pleural effusion, pericardial effusion, pulmonary edema, ascites, generalized edema). Severe hemorrhage (CNS, GI, other cases) reported. Caution should be used in patients receiving anticoagulants or drugs which inhibit platelet function. May prolong QT interval (should be used with caution in patients who have or may develop prolongation of the QT interval). Caution in hepatic impairment (hepatic metabolism), and in patients taking anticoagulants or therapy which alters CYP3A4 activity. Tablets contain lactose monohydrate (caution in lactose-intolerant patients).