Small molecular compounds in development for rheumatoid arthritis

Curr Opin Rheumatol. 2013 May;25(3):391-7. doi: 10.1097/BOR.0b013e32835fd828.


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.

Publication types

  • Review

MeSH terms

  • Antirheumatic Agents / therapeutic use*
  • Arthritis, Rheumatoid / drug therapy*
  • Humans
  • Janus Kinases / antagonists & inhibitors
  • Protein Kinase Inhibitors / therapeutic use
  • Protein-Tyrosine Kinases / antagonists & inhibitors


  • Antirheumatic Agents
  • Protein Kinase Inhibitors
  • Protein-Tyrosine Kinases
  • Janus Kinases