DDInter1628 DDInter1435
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
Pexidartinib is a selective tyrosine kinase inhibitor that works by inhibiting the colony-stimulating factor (CSF1)/CSF1 receptor pathway. Pexidartinib was originally developed by Daiichi Sankyo, Inc. and it was approved by the FDA in August 2019 as the first systemic therapy for adult patients with symptomatic tenosynovial giant cell tumor. Tenosynovial giant cell tumor is a rare form of non-malignant tumor that causes the synovium and tendon sheaths to thicken and overgrow, leading to damage in surrounding joint tissue.[A182240,L7901] Debilitating symptoms often follow with tenosynovial giant cell tumors, along with a risk of significant functional limitations and a reduced quality of life in patients. While surgical resection is a current standard of care for tenosynovial giant cell tumor, there are tumor types where surgeries are deemed clinically ineffective with a high risk of lifetime recurrence. Pexidartinib works by blocking the immune responses that are activated in tenosynovial giant cell tumors. In clinical trials, pexidartinib was shown to promote improvements in patient symptoms and functional outcomes in TGCT. Pexidartinib is available in oral formulations and it is commonly marketed as Turalio.
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)