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BioCryst Selects Two Plasma Kallikrein Inhibitors for Hereditary Angioedema into Preclinical Development

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BioCryst
Pharmaceuticals (NASDAQ: BCRX) today announced that it has
selected two optimized plasma kallikrein inhibitors to advance into
preclinical development as potential once-daily, oral treatments for the
prevention of hereditary angioedema (HAE) attacks.

The second generation discovery program's goals of improving selectivity
and bioavailability compared to BCX4161
were both met, with no effect on prothrombin time at high concentrations
(>50 micromolar), and oral fraction absorbed exceeding 25%. Similar to
BCX4161, these BioCryst discovered compounds demonstrate sub-nanomolar
potency on the isolated enzyme and single digit nanomolar potency in
suppressing kallikrein activity in an ex vivo activated human plasma
kallikrein inhibition (aPKI) assay. Plasma concentrations of each of

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