Table 1 Spleen tyrosine kinase inhibition therapy in arthritis animal models and patients with rheumatoid arthritis

Braselmann et al. [37]

R406

14 days, twice a day, orally

Collagen-induced arthritis, K/BXN arthritis model

Improved clinical scores, histopathology, and radiography

Pine et al. [38]

R406

18 days, twice a day, orally

Collagen-induced arthritis in rats

Suppressed clinical arthritis, bone erosions, pannus formation, and synovitis

Weinblatt et al. [46]

R406

12 weeks, 100 or 150 mg twice a day, orally

Active RA patients who were incomplete responders to MTX

R788 (100 mg twice a day):

ACR20, 50, and 70 responses (65%, 49%, and 33%)

R788 (150 mg every day):

ACR20, 50, and 70 responses (72%, 57%, and 40%)

Weinblatt et al. [47]

R788

6 months, 100 or 150 mg twice a day, orally

Active RA patients who were incomplete responders to MTX

R788 (100 mg twice a day):

ACR20, 50, and 70 responses (66%, 43%, and 28%)

R788 (150 mg every day):

ACR20, 50, and 70 responses (57%, 32%, and 14%)

Genovese et al. [48]

R788

3 months, 100 mg twice a day, orally

Active RA patients who failed biologic agents

R788 (100 mg twice a day):

ACR20 response (39%).

Response rate was not different from that of placebo.