IndraLab
Statements
2-[1-ethylsulfonyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1-pyrazolyl]-3-azetidinyl]acetonitrile inhibits JAK1. 64 / 64
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"Early clinical trial results of baricitinib, by itself or in combination with remdesivir, on hospitalized COVID‐19 patients, showed reduced inflammation and favorable clinical outcomes [156, 157], supporting the efficacy of JAK1/JAK2 inhibitors in resolving SARS‐CoV‐2 infection‐induced inflammation."
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"In this regard, in vitro assays using human peripheral blood mononuclear cells showed that baricitinib inhibited the signalling of several JAK1 and JAK2 dependent cytokines, including IL-6 signalling [XREF_BIBR, XREF_BIBR] and also reduced the mean change from baseline of plasma IL-6 in adult patients with active RA [XREF_BIBR]."
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"38 Notably, in spite of the (partially) distinct pharmacodynamic effects of the two compounds (ie, tofacitinib predominantly inhibiting JAK1 and JAK3, baricitinib predominantly inhibiting JAK1 and JAK2), their safety profile is very similar, suggesting that the actual in vivo effects might not be predicted entirely by in vitro " selectivity " assays."
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"Therefore, it is likely that JAK inhibitors such as tofacitinib (a selective inhibitor of JAK1 and 3) and baricitinib (a selective inhibitor of JAK1 and 2) interupt the intracellular signaling of IL-20R ligands as well as the signaling of other members of the type I/II cytokine family (Table 1) (76)."
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"Current Food and Drug Administration (FDA) and European Medical Agency (EMA) licensed JAK inhibitors include two first-generation agents [11]; i) tofacitinib which inhibits JAK3 and JAK1 with some affinity for JAK2 and limited affinity for TYK2 and was licensed in 2012, and ii) baricitinib which inhibits JAK1 and JAK2 (and to a much lesser extent TYK2) and was licensed in 2017."
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"From the studies conducted, various strategies that block ACE2 receptor; TMPRSS2 inhibitors like Camostat mesylate; anti-IFN-gamma drugs like Emapalumab that target STAT1; JAK1 and JAK2 inhibitors like Baricitinib, Ruxolinib that inhibit ACE2 mediated endocytosis; monoclonal antibody targeting S protein; PARPs intervening antiviral ADP ribosylation can aid in the treatment of this disease [XREF_BIBR, XREF_BIBR, XREF_BIBR]."
reach
"From the studies conducted, various strategies that block ACE2 receptor; TMPRSS2 inhibitors like Camostat mesylate; anti-IFN-gamma drugs like Emapalumab that target STAT1; JAK1 and JAK2 inhibitors like Baricitinib, Ruxolinib that inhibit ACE2 mediated endocytosis; monoclonal antibody targeting S protein; PARPs intervening antiviral ADP ribosylation can aid in the treatment of this disease [47,60,78]."
reach
"The use of JAK1 and JAK2 inhibitors such as ruxolitinib and baricitinib for GvHD prophylaxis may limit the need for expensive and labor-intensive ex vivo cellular manipulations 38 and may also reduce the use of broadly immunosuppressive agents that may themselves contribute to disease relapse, morbidity, and mortality after allo-HSCT."