Masahiro Ohzeki

Phase I study of EST, a new thiol protease inhibitor. The 2nd report: Safety and pharmacokinetics in continuous administration.

EST is a specific thiol protease inhibitor newly synthesized as a drug for muscular dystrophy.Following the first Phase I study of EST single dose (First report), the second Phase I study on EST continuous administration was performed in healthy adult male volunteers to investigate its safety and pharmacokinetics.In the first stage, 100mg was administered 3 times a day after meals for 1 day, and in the next stage, 100 mg was administered 3 times a day after meals for 7 consecutive days.No change due to EST was found from the observation of the subjective and objective symptoms and clinical tests.EST was detected as E-64-c (effective form of EST) in serum and urine after oral administration. No accumulation of EST was observed after continuous administration, and approximately 30% of total EST was collected in urine.