DDInter909 DDInter1628
Imatinib is a small molecule kinase inhibitor that revolutionized the treatment of cancer, particularly chronic myeloid leukemia, in 2001. It was deemed a "miracle drug" due to its clinical success, as oncologist Dr. Brian noted that "complete hematologic responses were observed in 53 of 54 patients with CML treated with a daily dosage of 300 mg or more and typically occurred in the first four weeks of therapy".. The discovery of imatinib also established a new group of therapy called "targeted therapy", since treatment can be tailored specifically to the unique cancer genetics of each patient. Imatinib was approved on February 1st,2001 by the FDA and November 7th, 2001 by the EMA; however, its European approval has been withdrawn in October 2023.[A263036,L49746,L49751]
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.
Imatinib {u} (Compound) treats {v} (Disease) hematologic cancer
hematologic cancer {u} (Disease) is treated by {v} (Compound) Ruxolitinib
Imatinib {u} (Compound) binds {v} (Gene) CYP3A4
CYP3A4 {u} (Gene) is bound by {v} (Compound) Ruxolitinib
Imatinib {u} (Compound) downregulates {v} (Gene) NPDC1
NPDC1 {u} (Gene) is downregulated by {v} (Compound) Ruxolitinib
Imatinib {u} (Compound) causes {v} (Side Effect) Anaemia
Anaemia {u} (Side Effect) is caused by {v} (Compound) Ruxolitinib
Imatinib {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
Imatinib {u} (Compound) downregulates {v} (Gene) NPDC1
NPDC1 {u} (Gene) covaries with {v} (Gene) MKNK2
MKNK2 {u} (Gene) is bound by {v} (Compound) Ruxolitinib
Imatinib {u} (Compound) resembles {v} (Compound) and {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Nilotinib
Nilotinib {u} (Compound) treats {v} (Disease) hematologic cancer
hematologic cancer {u} (Disease) is treated by {v} (Compound) Ruxolitinib
Imatinib {u} (Compound) downregulates {v} (Gene) NPDC1
NPDC1 {u} (Gene) is regulated by {v} (Gene) LRRK2
LRRK2 {u} (Gene) is bound by {v} (Compound) Ruxolitinib
Imatinib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Epirubicin
Epirubicin {u} (Compound) treats {v} (Disease) hematologic cancer
hematologic cancer {u} (Disease) is treated by {v} (Compound) Ruxolitinib
Imatinib {u} (Compound) resembles {v} (Compound) and {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Nilotinib
Nilotinib {u} (Compound) binds {v} (Gene) CYP3A4
CYP3A4 {u} (Gene) is bound by {v} (Compound) Ruxolitinib
Imatinib (Compound) treats hematologic cancer (Disease) and hematologic cancer (Disease) is treated by Ruxolitinib (Compound)
Imatinib (Compound) binds CYP3A4 (Gene) and CYP3A4 (Gene) is bound by Ruxolitinib (Compound)
Imatinib (Compound) downregulates NPDC1 (Gene) and NPDC1 (Gene) is downregulated by Ruxolitinib (Compound)
Imatinib (Compound) causes Anaemia (Side Effect) and Anaemia (Side Effect) is caused by Ruxolitinib (Compound)
Imatinib (Compound) treats hematologic cancer (Disease) and hematologic cancer (Disease) is associated with JAK1 (Gene) and JAK1 (Gene) is bound by Ruxolitinib (Compound)
Imatinib (Compound) downregulates NPDC1 (Gene) and NPDC1 (Gene) covaries with MKNK2 (Gene) and MKNK2 (Gene) is bound by Ruxolitinib (Compound)
Imatinib (Compound) resembles Nilotinib (Compound) and Imatinib may cause a moderate interaction that could exacerbate diseases when taken with Nilotinib and Nilotinib (Compound) treats hematologic cancer (Disease) and hematologic cancer (Disease) is treated by Ruxolitinib (Compound)
Imatinib (Compound) downregulates NPDC1 (Gene) and NPDC1 (Gene) is regulated by LRRK2 (Gene) and LRRK2 (Gene) is bound by Ruxolitinib (Compound)
Imatinib may cause a moderate interaction that could exacerbate diseases when taken with Epirubicin and Epirubicin (Compound) treats hematologic cancer (Disease) and hematologic cancer (Disease) is treated by Ruxolitinib (Compound)
Imatinib (Compound) resembles Nilotinib (Compound) and Imatinib may cause a moderate interaction that could exacerbate diseases when taken with Nilotinib and Nilotinib (Compound) binds CYP3A4 (Gene) and CYP3A4 (Gene) is bound by Ruxolitinib (Compound)