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Janus kinase inhibitor information


A Janus kinase inhibitor, also known as JAK inhibitor or jakinib,[1] is a type of immune modulating medication, which inhibits the activity of one or more of the Janus kinase family of enzymes (JAK1, JAK2, JAK3, TYK2), thereby interfering with the JAK-STAT signaling pathway in lymphocytes.

It is used in the treatment of cancer and inflammatory diseases[1][2] such as rheumatoid arthritis[3] and various skin conditions.[4] A Janus kinase 3 inhibitor is attractive as a possible treatment of various autoimmune diseases since its function is mainly restricted to lymphocytes. As of 2017, development of a selective JAK3 inhibitor was ongoing.[5]

  1. ^ a b Kontzias A, Kotlyar A, Laurence A, Changelian P, O'Shea JJ (August 2012). "Jakinibs: a new class of kinase inhibitors in cancer and autoimmune disease". Current Opinion in Pharmacology. 12 (4): 464–70. doi:10.1016/j.coph.2012.06.008. PMC 3419278. PMID 22819198.
  2. ^ Pesu M, Laurence A, Kishore N, Zwillich SH, Chan G, O'Shea JJ (June 2008). "Therapeutic targeting of Janus kinases". Immunological Reviews. 223: 132–42. doi:10.1111/j.1600-065X.2008.00644.x. PMC 2634846. PMID 18613833.
  3. ^ Norman P (August 2014). "Selective JAK inhibitors in development for rheumatoid arthritis". Expert Opinion on Investigational Drugs. 23 (8): 1067–77. doi:10.1517/13543784.2014.918604. PMID 24818516. S2CID 21143324.
  4. ^ "JAK Inhibitors Showing Promise for Many Skin Problems - Conditions ranging from alopecia to vitiligo". 6 July 2017. Archived from the original on 13 July 2017. Retrieved 9 July 2017.
  5. ^ Forster M, Gehringer M, Laufer SA (September 2017). "Recent advances in JAK3 inhibition: Isoform selectivity by covalent cysteine targeting". Bioorganic & Medicinal Chemistry Letters. 27 (18): 4229–4237. doi:10.1016/j.bmcl.2017.07.079. PMID 28844493.

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Janus kinase inhibitor

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A Janus kinase inhibitor, also known as JAK inhibitor or jakinib, is a type of immune modulating medication, which inhibits the activity of one or more...

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Janus kinase 3 inhibitor

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Janus kinase 3 inhibitors, also called JAK3 inhibitors, are a new class of immunomodulatory agents that inhibit Janus kinase 3. They are used for the treatment...

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Janus kinase 2

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Janus kinase 2 (commonly called JAK2) is a non-receptor tyrosine kinase. It is a member of the Janus kinase family and has been implicated in signaling...

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Janus kinase

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Janus kinase (JAK) is a family of intracellular, non-receptor tyrosine kinases that transduce cytokine-mediated signals via the JAK-STAT pathway. They...

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Ruxolitinib

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levels. Ruxolitinib is a Janus kinase inhibitor (JAK inhibitor) with selectivity for subtypes JAK1 and JAK2. Ruxolitinib inhibits dysregulated JAK signaling...

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Antiarthritics

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unlike biologics. Examples: Tofacitinib Baricitinib JAK inhibitors act by inhibiting Janus Kinases which consequently affect a cascade of enzymes responsible...

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Janus kinase 1

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IRS1, IL10RA, PTPN11, STAM2, STAT3, STAT5A, STAT5B, and TNFRSF1A. Janus kinase inhibitor GRCh38: Ensembl release 89: ENSG00000162434 – Ensembl, May 2017...

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Oclacitinib

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synthetic cyclohexylamino pyrrolopyrimidine janus kinase inhibitor that is relatively selective for JAK1. It inhibits signal transduction when the JAK is activated...

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Momelotinib

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It is an inhibitor of Janus kinases JAK1 and JAK2, acting as an ATP competitor with IC50 values of 11 and 18 nM, respectively. The inhibitor is significantly...

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Janus kinase 3

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Tyrosine-protein kinase JAK3 is a tyrosine kinase enzyme that in humans is encoded by the JAK3 gene. Janus kinase 3 is a tyrosine kinase that belongs to the janus family...

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Deuruxolitinib

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Deuruxolitinib (CTP-543) is a Janus kinase inhibitor selective for JAK1 and JAK2. It is in development to treat alopecia areata. If approved the drug would...

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Abrocitinib

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medication used for the treatment of atopic dermatitis (eczema). It is a Janus kinase inhibitor and it was developed by Pfizer. It is taken by mouth. The most common...

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Vitiligo

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2002.04837.x. PMID 12410698. S2CID 42396825. Qi F, Liu F, Gao L. Janus Kinase Inhibitors in the Treatment of Vitiligo: A Review. Front Immunol. 2021 Nov...

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Atopic dermatitis

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Crisaborole, an inhibitor of PDE-4, is also effective and safe as a topical treatment for mild-to-moderate AD. Ruxolitinib, a Janus kinase inhibitor, has uncertain...

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Peficitinib

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rheumatoid arthritis. It belongs to the class of drugs known as Janus kinase inhibitors (JAK inhibitors). Peficitinib was approved for use in Japan in 2019. Kivitz...

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Tofacitinib

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juvenile idiopathic arthritis, and ulcerative colitis. It is a janus kinase (JAK) inhibitor, discovered and developed by the National Institutes of Health...

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Baricitinib

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rheumatoid arthritis, alopecia areata, and COVID-19. It acts as an inhibitor of janus kinase (JAK), blocking the subtypes JAK1 and JAK2. Baricitinib is approved...

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Jaktinib

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Jaktinib is a janus kinase inhibitor under development for myelofibrosis. It is a deuterated-drug analog of momelotinib. Zhang, Yi; Zhou, Hu; Jiang, Zhongxing;...

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Dermatitis

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treatment of mild to moderate atopic dermatitis. It is a topical Janus kinase inhibitor. Atopic dermatitis (AD) may be treated with narrowband UVB, which...

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Gandotinib

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Eli Lilly for treatment of cancer. It is a small molecule JAK2 (Janus kinase) inhibitor, with additional minor inhibition of STAT3. In phase I trial, 16%...

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Ritlecitinib

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alopecia areata (hair loss). Ritlecitinib is a kinase inhibitor which inhibits Janus kinase 3 and tyrosine kinase. Ritlecitinib was approved for medical use...

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Lestaurtinib

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of cancer. It is an inhibitor of the kinases fms-like tyrosine kinase 3 (FLT3), Janus kinase 2 (JAK2), tropomyosin receptor kinase (trk) A (TrkA), TrkB...

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Alopecia universalis

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of treatment; folliculitis is also an occasional complication. Janus kinase inhibitors, previously used in the treatment of cancer and other diseases...

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Enzyme inhibitor

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may result in cancer. Hence kinase inhibitors such as imatinib are frequently used to treat malignancies. Janus kinases are another notable example of...

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Ivarmacitinib

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Ivarmacitinib (SHR0302) is a small molecule drug and selective janus kinase 1 (JAK1) inhibitor. It is being developed for ulcerative colitis, eczema, alopecia...

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Antipruritic

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and effective in animal models of other prurituses Oclacitinib, a janus kinase inhibitor used to control pruritus in dogs. Burow's solution, an astringent...

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Fedratinib

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who are Janus kinase (JAK) inhibitor naïve or have been treated with ruxolitinib. Fedratinib acts as a competitive inhibitor of protein kinase JAK-2 with...

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