Dasatinib

Generic Name
Dasatinib
Brand Names
Sprycel
Drug Type
Small Molecule
Chemical Formula
C22H26ClN7O2S
CAS Number
302962-49-8
Unique Ingredient Identifier
X78UG0A0RN
Background

Dasatinib is an orally available multikinase inhibitor indicated for the treatment of Philadelphia chromosome (Ph)-positive leukemias. Ph is a chromosomal abnormality found in patients with chronic myelogenous leukemia (CML) and acute lymphocytic leukemia (ALL), where the ABL tyrosine kinase and the breakpoint cluster region (BCR) gene transcribe the chimeric protein BCR-ABL. BCR-ABL is associated with the uncontrolled activity of the ABL tyrosine kinase and is involved in the pathogenesis of CML and 15-30% of ALL cases. Dasatinib also inhibits a spectrum of kinases involved in cancer, including several SRC-family kinases.

Unlike imatinib, another tyrosine kinase used for the treatment of CML and Ph-positive ALL, dasatinib inhibits the active and inactive conformations of the ABL kinase domain. Also, mutations in the kinase domain of BCR-ABL may lead to relapse during imatinib treatment. Since dasatinib does not interact with some of the residues involved in those mutations, the use of this drug represents a therapeutic alternative for patients with cancers that have developed imatinib-resistance. The use of dasatinib was first approved by the FDA in 2006.

Indication

Dasatinib is indicated for the treatment of newly diagnosed adults with Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) in chronic phase, as well as adults with chronic, accelerated, or myeloid or lymphoid blast phase Ph+ CML with resistance or intolerance to prior therapy including imatinib, and adults with Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL) with resistance or intolerance to prior therapy. Dasatinib is also indicated for the treatment of pediatric patients 1 year of age and older with Ph+ CML in chronic phase or newly diagnosed Ph+ ALL in combination with chemotherapy.

Associated Conditions
Accelerated Phase Chronic Myelogenous Leukemia (CML), Acute Lymphoblastic Leukaemias (ALL), Chronic Phase Chronic Myeloid Leukemia, Blast phase Chronic myeloid leukemia
Associated Therapies
-

Long-term Safety of Dasatinib in Patients With Chronic Myelogenous Leukemia or Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia

Phase 2
Completed
Conditions
Interventions
First Posted Date
2009-09-23
Last Posted Date
2016-01-22
Lead Sponsor
Bristol-Myers Squibb
Target Recruit Count
238
Registration Number
NCT00982488
Locations
🇺🇸

Pacific Cancer Medical Center Inc, Anaheim, California, United States

🇺🇸

Ucla Department Of Medicine, Los Angeles, California, United States

🇺🇸

John Theurer Cancer Center, Hackensack, New Jersey, United States

and more 15 locations

Evaluation of Response of Dasatinib to Treat Mastocytosis

Phase 2
Conditions
Interventions
First Posted Date
2009-09-17
Last Posted Date
2009-09-18
Lead Sponsor
Federico II University
Target Recruit Count
30
Registration Number
NCT00979160
Locations
🇮🇹

Divisione di Ematologia Ospedale Niguarda Ca' Grande, Milano, Italy

🇮🇹

Istituto di ematologia "L e A Seragnoli" - Policlinico universitario Sant'Orsola-Malpighi, Bologna, Italy

🇮🇹

Istituto di Ematologia Università degli Studi di Pavia - Policlinico S. Matteo IRCCS, Pavia, Italy

and more 9 locations

Chronic Myelogenous Leukemia or Philadelphia Chromosome Positive Acute Lymphoblastic Leukemic Study

Phase 1
Completed
Conditions
Interventions
First Posted Date
2009-09-17
Last Posted Date
2011-04-28
Lead Sponsor
Bristol-Myers Squibb
Target Recruit Count
46
Registration Number
NCT00978731

Study of CCNU (Lomustine) Plus Dasatinib in Recurrent Glioblastoma (GBM)

Phase 1
Terminated
Conditions
Interventions
First Posted Date
2009-07-29
Last Posted Date
2012-08-31
Lead Sponsor
Bristol-Myers Squibb
Target Recruit Count
28
Registration Number
NCT00948389
Locations
🇨🇭

Local Institution, Lausanne, Switzerland

Trial of Dasatinib Plus Ixabepilone in 2nd or 3rd Line Metastatic Breast Cancer

Phase 1
Completed
Conditions
Interventions
First Posted Date
2009-06-18
Last Posted Date
2014-10-13
Lead Sponsor
Accelerated Community Oncology Research Network
Target Recruit Count
56
Registration Number
NCT00924352
Locations
🇺🇸

Oncology Hematology Specialists, P.A., Denville, New Jersey, United States

🇺🇸

Hematology Oncology PC, Stamford, Connecticut, United States

🇺🇸

Northwest Georgia Oncology Centers, Marietta, Georgia, United States

and more 10 locations

XAD - Xelox (Capecitabine + Oxaliplatin) + Bevacizumab + Dasatinib

First Posted Date
2009-06-15
Last Posted Date
2016-02-03
Lead Sponsor
Herbert Hurwitz, MD
Target Recruit Count
22
Registration Number
NCT00920868
Locations
🇺🇸

Rocky Mountain Cancer Center, Denver, Colorado, United States

🇺🇸

Duke Univeristy Medical Center, Durham, North Carolina, United States

A Study to Evaluate the Safety and Efficacy of Dasatinib (Sprycel) in Subjects With Relapsed or Refractory Diffuse Large B-Cell Lymphoma (DLBCL)

Phase 2
Terminated
Conditions
Interventions
First Posted Date
2009-06-11
Last Posted Date
2018-08-31
Lead Sponsor
Weill Medical College of Cornell University
Target Recruit Count
2
Registration Number
NCT00918463
Locations
🇺🇸

Weill Cornell Medical College, New York, New York, United States

Genomic Guided Therapy With Dasatinib or Nilutamide in Metastatic Castration-Resistant Prostate Cancer

Phase 2
Terminated
Conditions
Interventions
First Posted Date
2009-06-11
Last Posted Date
2014-10-29
Lead Sponsor
Duke University
Target Recruit Count
57
Registration Number
NCT00918385
Locations
🇺🇸

Oregon Health and Science University, Portland, Oregon, United States

🇺🇸

University of Washington/Seattle Cancer Care Alliance, Seattle, Washington, United States

🇺🇸

Duke University Medical Center, Durham, North Carolina, United States

Trial of Fulvestrant, MK-0646, and Dasatinib for Metastatic Hormone Receptor-Positive HER2-Negative Breast Cancer

Phase 1
Terminated
Conditions
Interventions
First Posted Date
2009-05-15
Last Posted Date
2015-02-02
Lead Sponsor
M.D. Anderson Cancer Center
Target Recruit Count
11
Registration Number
NCT00903006
Locations
🇺🇸

UT MD Anderson Cancer Center, Houston, Texas, United States

Dasatinib Plus Radiation Therapy/Temozolomide in Newly-Diagnosed Glioblastoma

First Posted Date
2009-05-11
Last Posted Date
2018-11-08
Lead Sponsor
M.D. Anderson Cancer Center
Target Recruit Count
16
Registration Number
NCT00895960
Locations
🇺🇸

UT MD Anderson Cancer Center, Houston, Texas, United States

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