Agents ranging from simple analgesics to antiinflammatory drugs to pow
erful immunomodulators have been used for the treatment of rheumatoid
arthritis with varying success. Despite the availability of agents tha
t are believed to be ''second line'' or ''disease modifying,'' many pa
tients either do not respond adequately to available agents or must di
scontinue their use because of intolerable or dangerous adverse reacti
ons. For this reason, researchers continue to search for more efficaci
ous and less toxic agents for patients with rheumatoid arthritis. This
article describes pharmaceutical agents currently under investigation
for use in rheumatoid arthritis, including the antiinflammatory agent
s, zileuton and tenidap, and the immunosuppressive agents, leflunomide
, mycophenolic acid (RS-61443), tacrolimus (FK-506), sirolimus (rapamy
cin), amiprilose (therafectin), cladribine (2- chlorodeoxyadenosine),
and azaribine.