Name: | dasatinib |
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PubChem Compound ID: | 11540687 |
Molecular formula: | C22H28ClN7O3S |
Molecular weight: | 506.022 g/mol |
Name: | dasatinib |
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Name (isomeric): | DB01254 |
Drug Type: | small molecule |
Synonyms: |
BMS-354825
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Brand: | Sprycel |
Category: | Protein Kinase Inhibitors |
CAS number: | 302962-49-8 |
Indication: | For the treatment of adults with chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia with resistance or intolerance to prior therapy. Also indicated for the treatment of adults with Philadelphia chromosome-positive acute lymphoblastic leukemia with resistance or intolerance to prior therapy. |
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Pharmacology: | Dasatinib is an oral dual BCR/ABL and Src family tyrosine kinase inhibitor |
Mechanism of Action: |
Dasatinib, at nanomolar concentrations, inhibits the following kinases: BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ. Based on modeling studies, dasatinib is predicted to bind to multiple conformations of the ABL kinase. In vitro, dasatinib was active in leukemic cell lines representing variants of imatinib mesylate sensi...
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Protein binding: | 96% |
Biotransformation: | Dasatinib is extensively metabolized in humans, primarily by the cytochrome P450 enzyme 3A4 |
Route of elimination: | Dasatinib is extensively metabolized in humans, primarily by the cytochrome P450 enzyme 3A4. Elimination is primarily via the feces. |
Half Life: | The overall mean terminal half-life of dasatinib is 3-5 hours. |
Toxicity: | Acute overdose in animals was associated with cardiotoxicity. |
Affected organisms: | Humans and other mammals |
Drug interaction: |
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