DDInter150 DDInter1628
Azathioprine is a prodrug of 6-mercaptopurine, first synthesized in 1956 by Gertrude Elion, William Lange, and George Hitchings in an attempt to produce a derivative of 6-mercaptopurine with a better therapeutic index.[A189678,A189687,A189690] Azathioprine is used to treat inflammatory conditions like rheumatoid arthritis and as an immunosuppressant in the prevention of renal transplant rejection. Azathiprine was granted FDA approval on 20 March 1968.
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.
Azathioprine {u} (Compound) downregulates {v} (Gene) PLK1
PLK1 {u} (Gene) is bound by {v} (Compound) Ruxolitinib
Azathioprine {u} (Compound) upregulates {v} (Gene) RRS1
RRS1 {u} (Gene) is upregulated by {v} (Compound) Ruxolitinib
Azathioprine {u} (Compound) causes {v} (Side Effect) Anaemia
Anaemia {u} (Side Effect) is caused by {v} (Compound) Ruxolitinib
Azathioprine {u} (Compound) downregulates {v} (Gene) PLK1
PLK1 {u} (Gene) is regulated by {v} (Gene) LRRK2
LRRK2 {u} (Gene) is bound by {v} (Compound) Ruxolitinib
Azathioprine {u} (Compound) upregulates {v} (Gene) RRS1
RRS1 {u} (Gene) is upregulated by {v} (Disease) hematologic cancer
hematologic cancer {u} (Disease) is treated by {v} (Compound) Ruxolitinib
Azathioprine {u} (Compound) treats {v} (Disease) systemic lupus erythematosus
systemic lupus erythematosus {u} (Disease) is associated with {v} (Gene) POLB
POLB {u} (Gene) is downregulated by {v} (Compound) Ruxolitinib
Azathioprine {u} (Compound) upregulates {v} (Gene) RRS1
RRS1 {u} (Gene) is regulated by {v} (Gene) IRAK1
IRAK1 {u} (Gene) is bound by {v} (Compound) Ruxolitinib
Azathioprine {u} (Compound) treats {v} (Disease) Crohn's disease
Crohn's disease {u} (Disease) downregulates {v} (Gene) KLHDC2
KLHDC2 {u} (Gene) is downregulated by {v} (Compound) Ruxolitinib
Azathioprine {u} (Compound) treats {v} (Disease) systemic lupus erythematosus
systemic lupus erythematosus {u} (Disease) is associated with {v} (Gene) JAK1
JAK1 {u} (Gene) is bound by {v} (Compound) Ruxolitinib
Azathioprine {u} (Compound) treats {v} (Disease) rheumatoid arthritis
rheumatoid arthritis {u} (Disease) downregulates {v} (Gene) AKAP8
AKAP8 {u} (Gene) is upregulated by {v} (Compound) Ruxolitinib
Azathioprine (Compound) downregulates PLK1 (Gene) and PLK1 (Gene) is bound by Ruxolitinib (Compound)
Azathioprine (Compound) upregulates RRS1 (Gene) and RRS1 (Gene) is upregulated by Ruxolitinib (Compound)
Azathioprine (Compound) causes Anaemia (Side Effect) and Anaemia (Side Effect) is caused by Ruxolitinib (Compound)
Azathioprine (Compound) downregulates PLK1 (Gene) and PLK1 (Gene) is regulated by LRRK2 (Gene) and LRRK2 (Gene) is bound by Ruxolitinib (Compound)
Azathioprine (Compound) upregulates RRS1 (Gene) and RRS1 (Gene) is upregulated by hematologic cancer (Disease) and hematologic cancer (Disease) is treated by Ruxolitinib (Compound)
Azathioprine (Compound) treats systemic lupus erythematosus (Disease) and systemic lupus erythematosus (Disease) is associated with POLB (Gene) and POLB (Gene) is downregulated by Ruxolitinib (Compound)
Azathioprine (Compound) upregulates RRS1 (Gene) and RRS1 (Gene) is regulated by IRAK1 (Gene) and IRAK1 (Gene) is bound by Ruxolitinib (Compound)
Azathioprine (Compound) treats Crohn's disease (Disease) and Crohn's disease (Disease) downregulates KLHDC2 (Gene) and KLHDC2 (Gene) is downregulated by Ruxolitinib (Compound)
Azathioprine (Compound) treats systemic lupus erythematosus (Disease) and systemic lupus erythematosus (Disease) is associated with JAK1 (Gene) and JAK1 (Gene) is bound by Ruxolitinib (Compound)
Azathioprine (Compound) treats rheumatoid arthritis (Disease) and rheumatoid arthritis (Disease) downregulates AKAP8 (Gene) and AKAP8 (Gene) is upregulated by Ruxolitinib (Compound)