Phase I Study of the Modified Tissue Plasminogen Activator E6010.

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E6010 is a novel modified human tissue plasminogen activator, in which cysteine 84 inthe epidermal growth factor domain of human tissue-type plasminogen activator (t-PA) isreplaced by serine. The safety, pharmacological activity and pharmacokinetics of E6010 were studied in 6healthy volunteers following a rapid infusion (3-min intravenous infusion) of a dose of 0. 25to 6. 0 mg. No drug related subjective symptoms or objective findings were observed . Noclinically significant change was found in clinical laboratory findings. There was a dosedependent decrease of plasminogen and α2-PI. In the 6. 0 mg dose study, plasminogen andα2-PI decreased maximally by 19% and 40% of the preinfusion value at 2 hours after thestart of infusion, respectively. The half-lives for α-and β-phases of plasma E6010 concentration measured by enzyme-linked immunosorbent assay (ELISA) were 22. 85-47. 06 min and7. 39-10. 29 hr, respectively. A one-compartment model was used for the analysis of the plasma E6010 concentration measured by the fibrin plate method since a β-phase for fibrin plate activity could not be defined due to insufficient analytical sensitivity of this assay . The half-lifeof plasma E6010 concentration measured by the fibrin plate method was 25 . 75-33. 12 min. These results suggest that a rapid infusion of E6010 could be effective for clot lysis as E6010 has a long duration of fibrinolytic activity due to its longer half-life than other fibrinolytic agents.
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Phase I Study of the Modified Tissue Plasminogen Activator E6010.

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