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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.
It is an inhibitor of the enzyme janus kinase 1 (JAK1) and janus kinase 3 (JAK 3), which means that it interferes with the JAK-STAT signaling pathway, which transmits extracellular information into the cell nucleus, influencing DNA transcription. [27]
Ruxolitinib is a Janus kinase inhibitor. [6] It was developed and marketed by Incyte Corp in the US under the brand name Jakafi, [6] and by Novartis elsewhere in the world, under the brand name Jakavi. [14] It was approved for medical use in the United States in 2011, [15] and in the European Union in 2012. [8]
Gusacitinib (ASN002) is an investigational drug which acts as a pan-Janus kinase inhibitor, binding with similar affinity at JAK1, JAK2, JAK3 and TYK2, and also inhibiting spleen tyrosine kinase (SYK). [1] It is taken orally and was developed for the treatment of eczema and dermatitis. [2] [3] [4]
It is a selective inhibitor of the enzyme janus kinase 1 (JAK1). [15] It inhibits JAK1 by 28 fold of selectivity over JAK2 and more than 340 fold of selectivity over JAK3. Two mechanisms are involved in atopic dermatitis, one involves epidermal barrier disruptions, and the other one is cutaneous inflammation due to the immune system over response.
JAK inhibitors act by inhibiting Janus Kinases which consequently affect a cascade of enzymes responsible for signaling a variety of cytokine and haematopoietic growth factor receptors. [24] As a consequence, inhibiting these enzymes leads to the control and suppression of immune pathways.
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.
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).