DDInter1642 DDInter1628
Sargramostim is a human recombinant granulocyte macrophage colony-stimulating factor (GM-CSF) expressed in yeast. It is a glycoprotein that is 127 residues. Substitution of Leu23 leads to a difference from native protein.
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.
Ruxolitinib {u} (Compound) treats {v} (Disease) hematologic cancer
Ruxolitinib {u} (Compound) binds {v} (Gene) RPS6KA6
Ruxolitinib {u} (Compound) upregulates {v} (Gene) FOXJ3
Ruxolitinib {u} (Compound) is included by {v} (Pharmacologic Class) Protein Kinase Inhibitors
Ruxolitinib {u} (Compound) downregulates {v} (Gene) AKT1
Ruxolitinib {u} (Compound) causes {v} (Side Effect) Anaemia
Ruxolitinib {u} (Compound) binds {v} (Gene) and {u} (Compound) upregulates {v} (Gene) DYRK1A
Ruxolitinib (Compound) treats hematologic cancer (Disease)
Ruxolitinib (Compound) binds RPS6KA6 (Gene)
Ruxolitinib (Compound) upregulates FOXJ3 (Gene)
Ruxolitinib (Compound) is included by Protein Kinase Inhibitors (Pharmacologic Class)
Ruxolitinib (Compound) downregulates AKT1 (Gene)
Ruxolitinib (Compound) causes Anaemia (Side Effect)
Ruxolitinib (Compound) binds DYRK1A (Gene) and Ruxolitinib (Compound) upregulates DYRK1A (Gene)