Dasatinib.
Article Details
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Lindauer M, Hochhaus A
Dasatinib.
Recent Results Cancer Res. 2010;184:83-102. doi: 10.1007/978-3-642-01222-8_7.
- PubMed ID
- 20072833 [ View in PubMed]
- Abstract
Dasatinib, (former BMS 354825), is an orally available small-molecule multikinase inhibitor. It potently inhibits BCR-ABL and SRC-family kinases (SRC, LCK, YES, FYN), but also c-KIT, PDGFR-alpha and beta, and ephrin receptor kinase.Dasatinib is about 300 times more potent than imatinib in cells expressing unmutated BCR-ABL in vitro. The drug has demonstrated activity against clinically relevant mutations, including those associated with poor prognosis during ongoing imatinib therapy.Dasatinib is approved for the treatment of patients with BCR-ABL-positive chronic myeloid leukemia (CML), resistant or intolerant to imatinib in chronic, accelerated, and blast phase. It also is approved for the treatment of Philadelphia Chromosome positive (Ph+) acute lymphoblastic leukemia (ALL) resistant or intolerant to imatinib.A single daily dose of 100 mg in chronic phase CML results in high hematologic and molecular remission rates and prolongation of survival. In accelerated and blastic phase as well as in ALL, 70 mg twice daily is recommended. Complete hematologic and cytogenetic remissions (CR) frequently occur even in this patient group with poor prognosis. Remissions however are very short.Side effects of dasatinib are frequent but mostly moderate and manageable and include cytopenias and pleural effusions. The role of dasatinib in other diseases, including solid tumors, has to be identified.
DrugBank Data that Cites this Article
- Drugs
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Dasatinib Ephrin type-A receptor 2 Protein Humans YesAntagonistDetails Dasatinib Platelet-derived growth factor receptor beta Protein Humans YesAntagonistDetails Dasatinib Tyrosine-protein kinase ABL2 Protein Humans UnknownMultitargetDetails Dasatinib Tyrosine-protein kinase Fyn Protein Humans YesInhibitorMultitargetDetails Dasatinib Tyrosine-protein kinase Lck Protein Humans YesInhibitorMultitargetDetails Dasatinib Tyrosine-protein kinase Yes Protein Humans YesInhibitorDetails - Drug Interactions
Drugs Interaction Integrate drug-drug
interactions in your softwareDasatinibPentobarbital The therapeutic efficacy of Dasatinib can be decreased when used in combination with Pentobarbital. DasatinibCarbamazepine The therapeutic efficacy of Dasatinib can be decreased when used in combination with Carbamazepine. DasatinibMitotane The therapeutic efficacy of Dasatinib can be decreased when used in combination with Mitotane. DasatinibPrimidone The therapeutic efficacy of Dasatinib can be decreased when used in combination with Primidone. DasatinibRifampicin The therapeutic efficacy of Dasatinib can be decreased when used in combination with Rifampicin.