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Table 1 PK and PD parameters in healthy subjects and HAE subjects after single oral single doses of BCX7353

From: Abstracts of 11th C1-inhibitor Deficiency & Angioedema Workshop

Population N Dose of BCX7353 mg C max a ng/mL AUC 0-24 a ng h/mL [7353] > 8×EC50 at 0.5,1,8,24 h n KKI at 30 minb % KKI at 24 hb %
Healthy subjects 6 250 104 (24) 995 (25) 0,3,1,0 12 (44) 24 (18)
Healthy subjects 6 500 245 (59) 2700 (43) 0,4,6,0 50 (26) 72 (10)
HAE subjectsc 6 750 584 (26) 5670 (17) 6,6,6,6 80 (7) 81 (11)
  1. aPK parameters are geometric mean (% coefficient of variation)
  2. bPD parameters are mean (standard deviation) in an in ex vivo assay (note that n = 5 in HAE subjects), and results reported are percent reduction in specific amidolytic activity from pre-dose sample. As the reagent volume dilutes the plasma sample 4-fold, BCX7353 concentration ex vivo is 25% of that present in vivo postdosing. The reported ex vivo % inhibition therefore underestimates the in vivo inhibitory activity achieved. For example, a value of 80% inhibition ex vivo corresponds to approximately > 94% inhibition in vivo
  3. cPK study in subjects with HAE was conducted at an HAE reference center at University Hospital, Frankfurt, Germany