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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.
[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.
Oclacitinib lacks the side effects that most JAK inhibitors have in humans; instead, side effects are infrequent, mild, and mostly self-limiting. [13] [14] [16] The most common side effects are gastrointestinal problems (vomiting, diarrhea, and appetite loss) and lethargy. The GI problems can sometimes be alleviated by giving oclacitinib with food.
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]
This has led to dose-limiting side effects in this otherwise promising class of drugs. [29] [30] Upadacitinib is a second generation Janus kinase inhibitor that is selective for the JAK1 subtype of this enzyme over the JAK2 (74-fold), JAK3 (58-fold) and tyrosine kinase 2 subtypes. [31]
Baricitinib is a Janus kinase (JAK) inhibitor that reversibly inhibits Janus kinase 1 with a half maximal inhibitory concentration (IC 50) of 5.9 nM and Janus kinase 2 with an IC 50 of 5.7 nM. Tyrosine kinase 2 , which belongs to the same enzyme family, is affected less (IC 50 = 53 nM), and Janus kinase 3 far less (IC 50 > 400 nM).
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