Function of Tofacitinib Citrate 1. Rheumatoid arthritis (RA) Tofacitinib citrate is a new class of anti-rheumatic drugs approved by the US FDA for the first time in ten years. Compared with other traditional anti-rheumatic drugs, it can not only relieve symptoms, but also slow or stop disease damage. Its clinical therapeutic effect is also comparable to biological drugs such as adalimumab. So far, monoclonal antibodies or fusion proteins are the main clinical treatments for RA, which require injections, and tofacitinib has greater advantages as an oral drug. The results of clinical studies show that tofacitinib still has satisfactory clinical effects for RA patients whose treatment with biological agents is ineffective. Therefore, these studies have further established its therapeutic status in patients with moderate to severe RA. 2. Treatment of active psoriatic arthritis (PsA) In May 2017, the US FDA accepted the supplementary new drug application of Xeljanz and Xeljanz XR for the treatment of adult patients with active psoriatic arthritis (PsA). The new drug supplement application is based on data from the Phase III clinical development project OPAL. The project includes two pivotal Phase III clinical studies (OPAL Broaden, OPAL Beyond) and a long-term extension study (OPAL Balance), which evaluated the use of tofacitinib in adult patients with active PsA who have previously failed PsA drug therapy. Efficacy and safety. 3. Treat ulcerative colitis (UC) In May 2017, in the New England Journal of Medicine, the small molecule JAK inhibitor tofacitinib developed by Pfizer in the treatment of ulcerative colitis (UC) in three phase III clinical trials proved that it is in moderate to severe In UC patients, the treatment of tofacitinib is effective, and the efficacy of many patients can last for more than a year. 4. Treatment of ankylosing spondylitis (AS) Ankylosing spondylitis (AS) is an immune-mediated chronic systemic inflammatory disease that affects the spine. Phase II clinical studies have confirmed the efficacy and safety of tofacitinib in the treatment of active AS. Clinical trial showed that nearly 30% of patients with AS who received tofacitinib can achieve a clinically significant reduction in MRI inflammation of the spine; compared with patients in the placebo group, the sacroiliac of the tofacitinib group The joint scores and spine scores both improved and were dose-related; the proportion of patients in the tofacitinib group that achieved MCID of the sacroiliac joint or spine was 4 times that of the placebo group; the clinical response rate of patients in the tofacitinib group who achieved MCID higher.

CAS NO:540737-29-9

EC NO:

Molecular Formula:C₁₆H₂₀N₆O·C₆H₈O₇

Molecular Weight:504.497

Synonyms:;Tofacitinib citrate;1-Piperidinepropanenitrile, 4-Methyl-3-(Methyl-7H-Pyrrolo[2,3-D]Pyrimidin-4-Ylamino)-Beta-Oxo-, (3R,4R)-, 2-Hydroxy-1,2,3-Propanetricarboxylate (1:1);1-PIPERIDINEPROPANENITRILE,4-METHYL-3-(METHYL-7H-PYRROLO[2,3-D]PYRIMIDIN-4-YLAMINO)-BETA-OXO-,(3R,4R)-,2-HYDROXY-1,2,3-PROPANETRICARBOXYLATE(1:1);Tasocitinib citrate;(3R,4R)-1-(Cyanoacetyl)-4-methyl-N-methyl-N-1H-pyrrolo[2,3-d]pyrimidin-4-yl-3-piperidinamine 2-hydroxy-1,2,3-propanetricarboxylate;CP 690500-10;CP 690550-10;(3R,4R)-4-Methyl-3-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-beta-oxo-1-piperidinepropanenitrile 2-Hydroxy-1,2,3-propanetricarboxylate;Tofacitnib Citrate;

Molecular Structure: