IUPAC name
2-hydroxypropane-1,2,3-tricarboxylic acid;3-[(3R,4R)-4-methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropanenitrile
2-hydroxypropane-1,2,3-tricarboxylic acid;3-[(3R,4R)-4-methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropanenitrile
540737-29-9
504.5 g·mol−1
C22H28N6O8
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Tofacitinib exerts its mechanism of action by inhibiting intracellular cytoplasmic non-receptor tyrosine kinase JAK enzymes, which are involved in adaptive and innate immune reactions in the process of immune-mediated inflammatory diseases. It is a reversible and competitive JAK inhibitor that binds to the ATP binding site of the kinase domain of JAK. It is similar in structure to ATP and binds to the ATP-binding site of JAK, thus competing with ATP for binding to the active site of the kinase domain. As a result, the drug inhibits the phosphorylation and activation of JAK, thereby preventing the phosphorylation and activation of STATs, and thus the activation of gene transcription; this leads to decreased cytokine production and modulation of the immune response. Tofacitinib is a pan-JAK inhibitor but targets JAK1 and JAK3 with a higher specificity over JAK2 and TYK2.
Tofacitinib is used to treat adults who have tried TNF blockers with:
Tofacitinib Oral Solution is used to treat patients 2 years of age and older with: