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Cytokines such as Interleukin-1 (IL-1) are important modulators of the cell-mediated immune response and play a paramount role in inflammatory autoimmune disease. We report on preliminary clinical experiences with a new, tricyclic substance [( 10-Methoxy-4H-benzo[4,5]cyclo-hepta-[1,2-b]thiophene-4- ylidene]acetic acid, MW 284), which inhibits the release of interleukin-1 alpha and -beta from cultured murine macrophages or human mononuclear cells. The study included 12 patients (rheumatoid arthritis, n = 9; hemochromatotic arthropathy, n = 1; psoriatic arthropathy, n = 1; seronegative spondylarthropathy, n = 1). Eight patients were treated for a total of 8 weeks, receiving a median dose of 800 mg/d of the substance. Due to significant clinical benefits, two patients continued for a total of six months. Administration of the drug was discontinued in two patients because of severe urticaria and lack of compliance, respectively. Four out of 10 patients showed clinical improvement according to Ritchie-Index, pain score, ESR and CRP. Side effects were diffuse gastrointestinal symptoms (4/12), temporary impairment of liver function (4/12) and allergic skin reactions (3/12).