OBJECTIVE: To review the pharmacology, pharmacokinetics, efficacy and safety, 
dosage administration, and adverse effects of tofacitinib for rheumatoid 
arthritis (RA) treatment.
DATA SOURCES: 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.
STUDY SELECTION AND DATA EXTRACTION: Data search was limited to include 
publications in English language and from human subjects.
DATA SYNTHESIS: 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.