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Description: Dasatinib is an oral dual BCR/ABL and Src family tyrosine kinases inhibitor approved for use in patients with chronic myelogenous leukemia (CML). The main targets of Dasatinib, are BCRABL, SRC, Ephrins and GFR.
Drug Type: Small Molecule; Approved; Investigational
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 sensitive and resistant disease. Dasatinib inhibited the growth of chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL) cell lines overexpressing BCR-ABL. Under the conditions of the assays, dasatinib was able to overcome imatinib resistance resulting from BCR-ABL kinase domain mutations, activation of alternate signaling pathways involving the SRC family kinases (LYN, HCK), and multi-drug resistance gene overexpression.
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.
Half Life: The overall mean terminal half-life of dasatinib is 3-5 hours.
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Data Correlations | 2 studies

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Genes category icon Genes
Score Help
MT1X 100 100
RHOB 93 93
LOXL2 92 92
MCM5 92 92
PTGS2 91 91
CAV1 91 91
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Biogroups category icon Biogroups
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Extrinsic Prothrombin Activation Pa… 100 100
FOSB Gene Expression and Drug Abuse 99 99
Intrinsic Prothrombin Activation Pa… 99 99
I8 - chymotrypsin/elastase inhibit… 99 99
I47 - latexin 98 98
I27 - Inhibitor family I27 (calpas… 98 98
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Individual Studies

  • Dasatinib resistance in breast cancer cell lines

    Homo sapiens Homo sapiens | RNA Expression   RNA Expression

    Transcriptional profiling was conducted on RNA from 23 breast cancer cell lines to identify genes whose expression level correlates with sensitivity of dasatinib.

    Authors: Huang F, Reeves K, Han X

    Organization: Bristol-Myers Squibb Co P.O. Box 5400/HW…
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Associated Researchers

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Thought leaders and organizations working on research involving Sprycel.

View All Author iconAuthors
  • Francis Y Lee
  • Jorge Cortes
  • Hagop Kantarjian
  • Andreas Hochhaus
  • Brian J Druker
View All Clinical trial sponsors icon Clinical Trials Sponsors
  • Bristol-Myers Squibb
  • M.D. Anderson Cancer Center
  • Weill Medical College of Cornell University
  • Duke University
  • University of Pittsburgh
View All Affiliations icon Organizations
  • University of Texas M. D. Anderson Cancer Center
  • M. D. Anderson Cancer Center
  • University of South Florida College of Medicine
  • Pharmaceutical Research Institute
  • Broad Institute of Harvard University and Massachusetts Institute of T…

Clinical Trials | 157 trials

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