Auranofin. A preliminary review of its pharmacological properties and therapeutic use in rheumatoid arthritis.
Auranofin is the first orally active gold compound for the treatment of rheumatoid arthritis. Like other chrysotherapeutic agents, its exact mechanism of action is unknown, but it probably acts via immunological mechanisms and alteration of lysosomal enzyme activity. Although long term clinical experience with auranofin is limited, its efficacy appears to approach that of sodium aurothiomalate. Further comparative studies with aurothioglucose, hydroxychloroquine and D-penicillamine are required before definitive statements can be made regarding the relative efficacy of auranofin and these agents. While patients have demonstrated clinical remission of rheumatoid arthritis in response to auranofin therapy, radiological studies have been inconclusive regarding its effect on the occurrence or progression of erosive lesions. Auranofin is relatively well tolerated in most patients, but diarrhoea, skin rash, and pruritus are sometimes troublesome, and thrombocytopenia and proteinuria are potentially serious side effects which may occur during therapy. Whereas mucocutaneous side effects are more frequent with injectable gold compounds, gastrointestinal reactions are the most common adverse effect seen with auranofin. The frequency of side effects has been similar with auranofin and sodium aurothiomalate, but they are generally less severe with auranofin. While some of the side effects are controlled by a reduction in dosage, temporary or permanent withdrawal of auranofin may be necessary. Auranofin is clearly a useful addition to the limited list of agents with disease-modifying potential presently available for the treatment of rheumatoid arthritis. It will doubtless generate much interest as its final place in therapy becomes better defined through additional well-designed studies and wider clinical experience.
D000042:Absorption; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000627:therapeutic use*; D001172:Arthritis, Rheumatoid / Q000188:drug therapy*; D001310:Auranofin; D006051:Aurothioglucose / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000276:immunology / Q000378:metabolism / Q000627:therapeutic use; D002986:Clinical Trials as Topic; D003967:Diarrhea / Q000139:chemically induced; D004305:Dose-Response Relationship, Drug; D005260:Female; D006046:Gold / Q000031:analogs & derivatives*; D006052:Gold Sodium Thiomalate / Q000627:therapeutic use; D006801:Humans; D007111:Immunity, Cellular; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D051379:Mice; D008875:Middle Aged; D011247:Pregnancy; D051381:Rats; D012098:Reproduction / Q000187:drug effects; D014018:Tissue Distribution
D000893:Anti-Inflammatory Agents; D006052:Gold Sodium Thiomalate; D006051:Aurothioglucose; D001310:Auranofin; D006046:Gold