DDInter1628 DDInter1658
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. Rux
Selpercatinib is a kinase inhibitor with enhanced specificity for RET tyrosine kinase receptors (RTKs) over other RTK classes.[A202055, A202052, L13604] Enhanced RET (Rearranged during transfection) oncogene expression is a hallmark of many cancers. Although multikinase inhibitors, including [cabozantinib], [ponatinib], [sorafenib], [sunitinib], and [vandetanib], have shown efficacy in RET-driven cancers, their lack of specificity is generally associated with substantial toxicity. Selpercatinib (LOXO-292) and pralsetinib (BLU-667) represent the first generation of specific RET RTK inhibitors for the treatment of RET-driven cancers.[A202049, A202055, A202052, L13604] Although selpercatinib is currently still under investigation in clinical trial NCT04211337, it was granted accelerated FDA approval on May 8, 2020, for specific RET-driven cancer indications. It is currently marketed under the brand name RETEVMO™ by Loxo Oncology Inc. Selpercatinib is also approved by the European Commission.
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)