title: Tofacitinib: The First Janus Kinase (JAK) inhibitor for the treatment of rheumatoid arthritis.
abstract: OBJECTIVE
  To review the pharmacology, pharmacokinetics, efficacy and safety, dosage administration, and adverse effects of tofacitinib for rheumatoid arthritis (RA) treatment.
  
  
  METHODS
  Primary sources of information were obtained from clinical studies, which were identified through PubMed (1966 to June 2013) and International Pharmaceutical Abstracts (1970 to March 2013) using terms: tofacitinib, tasocitinib, CP-690550, and CP-690,550. Information was used from tofacitinib package insert, guidelines, and published abstracts from the American College of Rheumatology (ACR) and the European League Against Rheumatism.
  
  
  METHODS
  Data search was limited to include publications in English language and from human subjects.
  
  
  RESULTS
  Tofacitinib is the first oral Janus kinase inhibitor indicated for treatment of moderate to severe RA. Tofacitinib demonstrated efficacy and safety comparable to other disease-modifying antirheumatic drugs (DMARDs). Tofacitinib was efficacious in RA patients, indicated by achievements of ACR20, ACR50, and ACR70 criteria. Similar improvements were observed in patients who met remission criteria based on the Disease Activity Scores 28 criteria and quality of life as measured by the Health Assessment Questionnaire-Disability Index (HAQ-DI). Tofacitinib was associated with infections and malignancies; and elevations in serum creatinine and lipids were observed. Drug interactions with inducers and inhibitors of the cytochrome P-450 3A4 and 2C9 isoenzymes were reported.
  
  
  CONCLUSIONS
  Tofacitinib is an oral treatment option for RA patients who have inadequate response or intolerance to methotrexate. Postmarket surveillance will provide further insight to tofacitinib's role in RA therapy, especially in patients who may require different types of combination therapy with DMARDS.
authors.affiliation: University of the Pacific, Stockton, CA, USA.
authors.forename: Deepti
authors.initials: D
authors.lastname: Vyas
authors.forename: Kate M
authors.initials: KM
authors.lastname: O'Dell
authors.forename: Jason L
authors.initials: JL
authors.lastname: Bandy
authors.forename: Eric G
authors.initials: EG
authors.lastname: Boyce
mesh_terms: D001172:Arthritis, Rheumatoid / Q000188:drug therapy* / Q000201:enzymology; D001189:Aryl Hydrocarbon Hydroxylases / Q000378:metabolism; D017322:Clinical Trials, Phase II as Topic; D017326:Clinical Trials, Phase III as Topic; D065729:Cytochrome P-450 CYP2C9; D051544:Cytochrome P-450 CYP3A / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D004347:Drug Interactions; D006801:Humans; D053612:Janus Kinases / Q000037:antagonists & inhibitors*; D010880:Piperidines / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D047428:Protein Kinase Inhibitors / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D011743:Pyrimidines / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D011758:Pyrroles / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D016896:Treatment Outcome
chemical_list: D010880:Piperidines; D047428:Protein Kinase Inhibitors; D011743:Pyrimidines; D011758:Pyrroles; C479163:tofacitinib; C450260:CYP2C9 protein, human; D065729:Cytochrome P-450 CYP2C9; D001189:Aryl Hydrocarbon Hydroxylases; D051544:Cytochrome P-450 CYP3A; C510163:CYP3A4 protein, human; D053612:Janus Kinases
keywords: CP-690550; Janus kinase (JAK) inhibitor; rheumatoid arthritis; tofacitinib