Small molecular compounds in development for rheumatoid arthritis.

Area of Science:

• Rheumatology
• Pharmacology
• Immunology

Background:

• Rheumatoid arthritis (RA) treatment historically relied on biologics.
• The development of orally available small molecules for RA has been a long-standing goal in rheumatology.
• Recent advancements indicate these goals are being realized.

Purpose of the Study:

• To update on the progress of small molecular compounds as novel therapeutics for rheumatoid arthritis.
• To highlight the emergence of orally available agents in RA treatment.
• To review recent findings in small molecule drug development for RA.

Main Methods:

• Review of recently published clinical trials and presented data.
• Focus on tyrosine kinase inhibitors, specifically Janus kinase (JAK) inhibitors.
• Examination of preclinical and clinical studies of small molecular entities for RA.

Main Results:

• Numerous clinical trials reported positive therapeutic results for tyrosine kinase inhibitors over the past year.
• Tofacitinib, a Janus kinase (JAK) inhibitor, demonstrated biologic-like efficacy and received FDA approval.
• Positive trial results were also reported for other JAK inhibitors, such as baricitinib.
• Multiple other JAK inhibitors and small molecules are in various stages of development.

Conclusions:

• Tyrosine kinase inhibition represents a significant new therapeutic strategy for rheumatoid arthritis.
• Orally available small molecules are becoming a reality in RA management.
• The field of RA therapeutics is expanding with novel small molecule drug candidates.