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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.
Pacritinib, sold under the brand name Vonjo, is an anti-cancer medication used to treat myelofibrosis. [1] [2] It is a macrocyclic protein kinase inhibitor. It mainly inhibits Janus kinase 2 (JAK2) and Fms-like tyrosine kinase 3\CD135 (FLT3). Common side effects include diarrhea, low platelet counts, nausea, anemia, and swelling in legs. [2]
Since the JAK-STAT pathway plays a major role in many fundamental processes, such as apoptosis and inflammation, dysfunctional proteins in the pathway may lead to a number of diseases. For example, alterations in JAK-STAT signalling can result in cancer and diseases affecting the immune system, such as severe combined immunodeficiency disorder ...
Janus kinase 3 inhibitors work by inhibiting the action of the enzyme Janus kinase 3, thereby interfering with the JAK-STAT signaling pathway.JAK3 is required for signaling by cytokines through the common γ chain of the interleukin receptors for IL-2, IL-4, IL-7, IL-9, IL-15, and IL-21. [4]
Janus kinase (JAK) is a family of intracellular, non-receptor tyrosine kinases that transduce cytokine-mediated signals via the JAK-STAT pathway. They were initially named " just another kinase " 1 and 2 (since they were just two of many discoveries in a PCR -based screen of kinases), [ 1 ] but were ultimately published as "Janus kinase".
[8] [9] [10] It is a janus kinase (JAK) inhibitor, [8] [9] discovered and developed by the National Institutes of Health and Pfizer. Common side effects include diarrhea, headache, and high blood pressure. [10] Serious side effects may include infections, cancer, and pulmonary embolism.
It is a Janus kinase inhibitor and it is taken by mouth. [4] The most common adverse reactions include dizziness, fatigue, bacterial infection, hemorrhage, thrombocytopenia, diarrhea, and nausea. [7] Momelotinib was approved for medical use in the United States in September 2023, [4] [7] [8] and in the European Union in January 2024. [5] [9]
Fedratinib, sold under the brand name Inrebic, is an anti-cancer medication used to treat myeloproliferative diseases including myelofibrosis. [5] It is used in the form of fedratinib hydrochloride capsules that are taken by mouth. It is a semi-selective inhibitor of Janus kinase 2 (JAK-2). [5] [6] It was approved by the FDA on 16 August 2019. [5]