Recently, in Japan, auranofin (6 mg/day) has been demonstrated to be a useful treatment for patients with moderate to severe asthma in a double-blind clinical trial. Therefore, to investigate the mechanism of auranofin on bronchial asthma, we examined pulmonary functions and bronchial responsiveness to inhaled methacholine in well-controlled asthmatics after 12 wks of treatment with auranofin, in a double-blind, placebo-controlled fashion. Twenty-five adult patients with asthma received orally 3 mg of auranofin or inactive placebo twice daily for 12 weeks. Bronchial responsiveness, pulmonary function tests and concentrations of gold in the blood were measured before and 6 and 12 wks after the therapy. Bronchial responsiveness (PD35-Grs) was significantly decreased after 12 wks of treatment with auranofin, compared with that 12 wks after treatment with inactive placebo. We suggest that inhibition of bronchial hyperresponsiveness by auranofin is one of the mechanisms by which auranofin is effective against bronchial asthma.