Pharmacokinetics and safety of EST, a new thiol protease inhibitor in patients with muscle diseases.

概要

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EST, a newly synthesized inhibitor specific for thiol protease, is developing as a candidate for muscular dystrophy therapy.<BR>A single dose of EST was administered to adult patients with muscle diseases, and a single dose as well as single doses everyday for seven consecutive days was administered to children with Duchenne muscular dystrophy in order to confirm the safety of this drug and also to compare the pharmacokinetics between the patients and healthy adult males.<BR>No side effect attributable to EST was observed in clinical signs or symptoms or in laboratory tests during administration.<BR>EST was detected as E-64-c (effective form of EST) in the serum and urine after oral administration and there was no intrinsic difference between patients and healthy adult males in absorption and excretion of the drug.<BR>Single dose and repeated dose administration did not produce different absorption and excretion patterns, with no accumulation of the drug being observed in either regimen.
一般社団法人日本臨床薬理学会の論文