DDInter484 DDInter1628
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
Ruxolitinib, formerly known as INCB018424 or INC424, is an anticancer drug and a Janus kinase (JAK) inhibitor. It is a potent and selective inhibitor of JAK1 and JAK2, which are tyrosine kinases involved in cytokine signalling and hematopoiesis. Myeloproliferative neoplasms, such as myelofibrosis and polycythemia vera, are often characterized by aberrant activation of the JAK-STAT pathway, leading to abnormal blood cell counts and thrombotic complications. By inhibiting JAK1 and JAK2, ruxolitinib works to block the dysregulated cell signalling pathways and prevents abnormal blood cell proliferation. Due to a large number of patients with myeloproliferative neoplasms who have JAK2 mutations, ruxolitinib was the first ATP-competitive inhibitor of JAK1 and JAK2 ever developed. Ruxolitinib was first approved for the treatment of adult patients with myelofibrosis by the FDA in 2011, followed by EMA's approval in 2012. In 2014, it was approved for the treatment of polycythemia vera in adults who have an inadequate response to or are intolerant of [hydroxyurea] and in 2019, ruxolitinib was approved for use in steroid-refractory acute graft-versus-host disease in adults and children. The topical formulation of ruxolitinib is used to treat atopic dermatitis and vitiligo. It is being investigated for other inflammatory skin conditions. Ruxolitinib has been investigated to treat patients with coronavirus disease 2019 (COVID-19) accompanied by severe systemic hyperinflammation. In phase II clinical trials, ruxolitinib improved chest computed tomography and improved recovery in patients with lymphopenia.[A229713, A229718] However, phase III clinical trials later determined that ruxolitinib was inadequate in meeting its primary endpoint of reducing the number of hospitalized COVID-19 patients who experienced severe complications thus the drug was not approved as a treatment for COVID-19.
Dasatinib {u} (Compound) treats {v} (Disease) hematologic cancer
hematologic cancer {u} (Disease) is treated by {v} (Compound) Ruxolitinib
Dasatinib {u} (Compound) binds {v} (Gene) MAP3K19
MAP3K19 {u} (Gene) is bound by {v} (Compound) Ruxolitinib
Dasatinib {u} (Compound) downregulates {v} (Gene) PLK1
PLK1 {u} (Gene) is bound by {v} (Compound) Ruxolitinib
Dasatinib {u} (Compound) downregulates {v} (Gene) URB2
URB2 {u} (Gene) is upregulated by {v} (Compound) Ruxolitinib
Dasatinib {u} (Compound) upregulates {v} (Gene) UBQLN2
UBQLN2 {u} (Gene) is upregulated by {v} (Compound) Ruxolitinib
Dasatinib {u} (Compound) upregulates {v} (Gene) NPEPL1
NPEPL1 {u} (Gene) is downregulated by {v} (Compound) Ruxolitinib
Dasatinib {u} (Compound) downregulates {v} (Gene) CDC45
CDC45 {u} (Gene) is downregulated by {v} (Compound) Ruxolitinib
Dasatinib {u} (Compound) causes {v} (Side Effect) Anaemia
Anaemia {u} (Side Effect) is caused by {v} (Compound) Ruxolitinib
Dasatinib {u} (Compound) treats {v} (Disease) hematologic cancer
hematologic cancer {u} (Disease) is associated with {v} (Gene) JAK1
JAK1 {u} (Gene) is bound by {v} (Compound) Ruxolitinib
Dasatinib {u} (Compound) binds {v} (Gene) JAK2
JAK2 {u} (Gene) is associated with {v} (Disease) hematologic cancer
hematologic cancer {u} (Disease) is treated by {v} (Compound) Ruxolitinib
Dasatinib (Compound) treats hematologic cancer (Disease) and hematologic cancer (Disease) is treated by Ruxolitinib (Compound)
Dasatinib (Compound) binds MAP3K19 (Gene) and MAP3K19 (Gene) is bound by Ruxolitinib (Compound)
Dasatinib (Compound) downregulates PLK1 (Gene) and PLK1 (Gene) is bound by Ruxolitinib (Compound)
Dasatinib (Compound) downregulates URB2 (Gene) and URB2 (Gene) is upregulated by Ruxolitinib (Compound)
Dasatinib (Compound) upregulates UBQLN2 (Gene) and UBQLN2 (Gene) is upregulated by Ruxolitinib (Compound)
Dasatinib (Compound) upregulates NPEPL1 (Gene) and NPEPL1 (Gene) is downregulated by Ruxolitinib (Compound)
Dasatinib (Compound) downregulates CDC45 (Gene) and CDC45 (Gene) is downregulated by Ruxolitinib (Compound)
Dasatinib (Compound) causes Anaemia (Side Effect) and Anaemia (Side Effect) is caused by Ruxolitinib (Compound)
Dasatinib (Compound) treats hematologic cancer (Disease) and hematologic cancer (Disease) is associated with JAK1 (Gene) and JAK1 (Gene) is bound by Ruxolitinib (Compound)
Dasatinib (Compound) binds JAK2 (Gene) and JAK2 (Gene) is associated with hematologic cancer (Disease) and hematologic cancer (Disease) is treated by Ruxolitinib (Compound)