PURPOSE OF REVIEW: To provide an update on the development of small molecular 
compounds as novel therapeutics for the treatment of rheumatoid arthritis. The 
development of such orally available agents has long been hoped for in 
rheumatology; in the past year, it has become clear that the expectations are 
becoming fulfilled.
RECENT FINDINGS: Over the past year, a large number of clinical trials have been 
published or presented reporting positive therapeutic results with tyrosine 
kinase inhibitors, a large class of orally available drugs that are also being 
developed in other medical fields. This class of drugs includes the Janus kinase 
(JAK) inhibitors, and data on tofacitinib published during the past year have 
attested to the biologic-like efficacy of this drug and supported its subsequent 
U.S. Food and Drugs Administration (FDA) approval. Positive clinical trial 
results have also been reported for several other JAK inhibitors including 
baricitinib. Several other JAK inhibitors and other small molecular entities are 
also being developed in studies ranging from preclinical models to large 
clinical trials.
SUMMARY: Tyrosine kinase inhibition has emerged as a major new direction in 
rheumatoid arthritis therapy.