stepronin (Tiase / Tioten)

Anti-human immunodeficiency virus activity of a new immunosuppressant drug called stepronin.

de Giorgi L L, Habeshaw J A JA, Broadhurst K K, Carminati P P et al.

Accelerated cell-mediated broncho-obstructive reaction to inhaled stepronin: a case report.

Romano A A, Di Fonso M M, Mormile F F, Quaratino D D et al.

We describe the case of a 20-year-old man who developed an obstructive bronchial reaction accompanied by a maculopapular facial rash 8 h after an aerosol treatment with the mucolytic drug stepronin. The results of intradermal and patch testing with stepronin, together with those of bronchial challenge and histologic findings in patch-tested skin, indicate that the patient's reaction involved an accelerated cell-mediated mechanism of hypersensitivity. Bronchial challenges with methacholine demonstrated a transient increase in nonspecific bronchial hyperreactivity.

Immunosuppressive effect of stepronin (TS-5010680) in mice.

de Giorgi L L, Arrigoni-Martelli E E, Matossian-Rogers A A

An expectorant, stepronin, reduces airway secretion in vitro.

Yamada K K, Satoh M M, Shimura S S, Sasaki T T et al.

Stepronin (SPN) is clinically used as an expectorant, and thenoic acid (TA) is its metabolite. We examined the effects of these drugs on the bioelectric parameters [potential difference (PD), short circuit current (SCC), conductance (G)] of the posterior epithelial membrane of canine trachea and on those of the mucus glycoprotein secretion from feline tracheal isolated glands. PD and SCC were obtained using an Ussing chamber and G was calculated as the ratio SCC/PD. Neither SPN nor TA significantly altered the baseline values of PD and SCC. However, in the mucosal solution, both SPN and TA significantly inhibited PD and SCC evoked by isoproterenol (ISOP), whereas G remained unchanged. Amirolide did not alter the inhibitory action of SPN and TA. Mucus glycoprotein secretion from isolated glands was estimated by measuring trichloride acetic acid-precipitable [3H]-glycoconjugates. SPN and TA significantly reduced mucus glycoprotein secretion. Further, when stimulated by methacholine, these agents significantly inhibited mucus glycoprotein secretion from isolated glands. These findings suggest that SPN inhibits airway secretion in vitro by both decreasing Cl- secretion from epithelial cells and mucus glycoprotein secretion from submucosal glands.