DDInter448 DDInter1628
Crizotinib is a tyrosine kinase receptor inhibitor used for the treatment of anaplastic lymphoma kinase (ALK) or ROS1-positive non-small cell lung cancer (NSCLC) tumors, as well as ALK-positive anaplastic large cell lymphoma (ALCL) and inflammatory myofibroblastic tumor (IMT). By targeting the echinoderm microtubule-associated protein-like 4 (EML4)-ALK fusion protein, crizotinib offers robust effectiveness in treating NSCLC in patients with this type of rearrangement. Crizotinib was the first-in-class drug used to treat ALK-positive tumors. Second- and third-generation ALK-tyrosine kinase-inhibitors have overcome many of the pharmacodynamic and genetic resistance mechanisms crizotinib is prone to. Crizotinib was approved by the FDA in 2011, and its use is accompanied by FDA-approved tests used
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.
Crizotinib {u} (Compound) binds {v} (Gene) BMP2K
BMP2K {u} (Gene) is bound by {v} (Compound) Ruxolitinib
Crizotinib {u} (Compound) downregulates {v} (Gene) PLK1
PLK1 {u} (Gene) is bound by {v} (Compound) Ruxolitinib
Crizotinib {u} (Compound) upregulates {v} (Gene) DUSP4
DUSP4 {u} (Gene) is upregulated by {v} (Compound) Ruxolitinib
Crizotinib {u} (Compound) downregulates {v} (Gene) AKT1
AKT1 {u} (Gene) is downregulated by {v} (Compound) Ruxolitinib
Crizotinib {u} (Compound) upregulates {v} (Gene) NUPR1
NUPR1 {u} (Gene) is downregulated by {v} (Compound) Ruxolitinib
Crizotinib {u} (Compound) causes {v} (Side Effect) Anaemia
Anaemia {u} (Side Effect) is caused by {v} (Compound) Ruxolitinib
Crizotinib {u} (Compound) binds {v} (Gene) IRAK1
IRAK1 {u} (Gene) interacts with {v} (Gene) MAP3K7
MAP3K7 {u} (Gene) is bound by {v} (Compound) Ruxolitinib
Crizotinib {u} (Compound) binds {v} (Gene) LTK
LTK {u} (Gene) regulates {v} (Gene) KIAA0753
KIAA0753 {u} (Gene) is upregulated by {v} (Compound) Ruxolitinib
Crizotinib {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
Crizotinib {u} (Compound) binds {v} (Gene) MAP3K2
MAP3K2 {u} (Gene) interacts with {v} (Gene) MAP3K3
MAP3K3 {u} (Gene) is bound by {v} (Compound) Ruxolitinib
Crizotinib (Compound) binds BMP2K (Gene) and BMP2K (Gene) is bound by Ruxolitinib (Compound)
Crizotinib (Compound) downregulates PLK1 (Gene) and PLK1 (Gene) is bound by Ruxolitinib (Compound)
Crizotinib (Compound) upregulates DUSP4 (Gene) and DUSP4 (Gene) is upregulated by Ruxolitinib (Compound)
Crizotinib (Compound) downregulates AKT1 (Gene) and AKT1 (Gene) is downregulated by Ruxolitinib (Compound)
Crizotinib (Compound) upregulates NUPR1 (Gene) and NUPR1 (Gene) is downregulated by Ruxolitinib (Compound)
Crizotinib (Compound) causes Anaemia (Side Effect) and Anaemia (Side Effect) is caused by Ruxolitinib (Compound)
Crizotinib (Compound) binds IRAK1 (Gene) and IRAK1 (Gene) interacts with MAP3K7 (Gene) and MAP3K7 (Gene) is bound by Ruxolitinib (Compound)
Crizotinib (Compound) binds LTK (Gene) and LTK (Gene) regulates KIAA0753 (Gene) and KIAA0753 (Gene) is upregulated by Ruxolitinib (Compound)
Crizotinib (Compound) binds JAK2 (Gene) and JAK2 (Gene) is associated with hematologic cancer (Disease) and hematologic cancer (Disease) is treated by Ruxolitinib (Compound)
Crizotinib (Compound) binds MAP3K2 (Gene) and MAP3K2 (Gene) interacts with MAP3K3 (Gene) and MAP3K3 (Gene) is bound by Ruxolitinib (Compound)