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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.
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]
The drug was coded as CP-690,550 [29] during development. Its original recommended International nonproprietary name (rINN) was tasocitinib, [ 30 ] but that was overruled during the INN approval process as being not optimally differentiable from other existing INNs, so the name "tofacitinib" was proposed and became the INN.
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.
When the word "biotechnology" gets thrown around in the pharmaceutical industry, it often implies the biomanufacturing of biologic drugs, such as therapeutic proteins. It makes sense to use these ...
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".
Inhibitors of this enzyme family have shown efficacy in treating certain inflammatory and autoimmune diseases such as rheumatoid arthritis and Crohn's disease. However, the first generation of these drugs, tofacitinib and ruxolitinib , lacked subtype selectivity, affecting JAK1/JAK3 and JAK1/JAK2 respectively.
Tyrosine kinase inhibitor (TKI) with selective activity against RET, VEGFR-2 and EGFR: Medullary thyroid cancer. Diarrhoea, hypertension, QT interval prolongation, depression, electrolyte anomalies, hypothyroidism and GI perforation (uncommon). 2.3 mTOR inhibitors: Everolimus: PO: mTOR inhibitor.