DDInter484 DDInter899
Dasatinib is an orally available multikinase inhibitor indicated for the treatment of Philadelphia chromosome (Ph)-positive leukemias.[A2224,L45171] 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.[A11377,A33432] 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
Ibrutinib is a small molecule that acts as an irreversible potent inhibitor of Burton's tyrosine kinase. It is designated as a targeted covalent drug and presented as a promising activity in B-cell malignancies in clinical trials. Ibrutinib was developed by Pharmacyclics Inc and was first approved by the FDA in November 2013 for the treatment of mantle cell lymphoma (MCL) under accelerated approval; however, in April 2023, the drug manufacturer withdrew the accelerated approvals for ibrutinib in the US. Ibrutinib was approved by the EMA in October 2014 and by Health Canada in November 2014. It is currently approved for the treatment of various conditions, such as chronic lymphocytic leukemia (CLL), Waldenström's Macroglobulinemia, and chronic graft versus host disease (cGVHD) in August 2017. Notably, ibrutinib became the first FDA-approved cGVHD treatment for children in August 2017.
Dasatinib {u} (Compound) treats {v} (Disease) hematologic cancer
Dasatinib {u} (Compound) binds {v} (Gene) SRC
Dasatinib {u} (Compound) upregulates {v} (Gene) SATB1
Dasatinib {u} (Compound) downregulates {v} (Gene) EBNA1BP2
Dasatinib {u} (Compound) causes {v} (Side Effect) Body temperature increased
Dasatinib {u} may cause a minor interaction that can limit clinical effects when taken with {v} Sulfamethoxazole
Dasatinib {u} may cause a minor interaction that can limit clinical effects when taken with {v} Doravirine
Dasatinib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Denosumab
Dasatinib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Granisetron
Dasatinib {u} may lead to a major life threatening interaction when taken with {v} Halofantrine
Dasatinib (Compound) treats hematologic cancer (Disease)
Dasatinib (Compound) binds SRC (Gene)
Dasatinib (Compound) upregulates SATB1 (Gene)
Dasatinib (Compound) downregulates EBNA1BP2 (Gene)
Dasatinib (Compound) causes Body temperature increased (Side Effect)
Dasatinib may cause a minor interaction that can limit clinical effects when taken with Sulfamethoxazole
Dasatinib may cause a minor interaction that can limit clinical effects when taken with Doravirine
Dasatinib may cause a moderate interaction that could exacerbate diseases when taken with Denosumab
Dasatinib may cause a moderate interaction that could exacerbate diseases when taken with Granisetron
Dasatinib may lead to a major life threatening interaction when taken with Halofantrine