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1. (WO2017035263) COMPOSITIONS COMPRISING A PLASMA KALLIKREIN INHIBITOR

Pub. No.:    WO/2017/035263    International Application No.:    PCT/US2016/048456
Publication Date: Fri Mar 03 00:59:59 CET 2017 International Filing Date: Thu Aug 25 01:59:59 CEST 2016
IPC: A61K 9/08
A61K 31/44
C07D 213/81
Applicants: BIOCRYST PHARMACEUTICALS, INC.
Inventors: BABU, Yarlagadda S.
BLOOM, Corey J.
BONE, Scott Joseph
KAUSHAL, Aditya Mohan
Title: COMPOSITIONS COMPRISING A PLASMA KALLIKREIN INHIBITOR
Abstract:
The present disclosure provides for compositions comprising 3-[2-(4-carbamimidoyl- phenylcarbamoyl)-5-methoxy-4-vinyl-phenyl]-6-(cyclopropylmethyl-carbamoyl)-pyridine-2- carboxylic acid, or a pharmaceutically acceptable form thereof, and a matrix, particularly compositions comprising a solid dispersion or combination of 3-[2-(4-carbamimidoyl- phenylcarbamoyl)-5-methoxy-4-vinyl-phenyl]-6-(cyclopropylmethyl-carbamoyl)-pyridine-2- carboxylic acid, or a pharmaceutically acceptable form thereof, and a concentration enhancing polymer. The compositions provide for higher exposure of 3-[2-(4-carbamimidoyl- phenylcarbamoyl)-5-methoxy-4-vinyl-phenyl]-6-(cyclopropylmethyl-carbamoyl)-pyridine-2- carboxylic acid in the blood for a given dose while at the same time provide for a higher concentration of 3-[2-(4-carbamimidoyl-phenylcarbamoyl)-5-methoxy-4-vinyl-phenyl]-6- (cyclopropylmethyl-carbamoyl)-pyridine-2-carboxylic acid in the blood over time. Dosage forms, dosing protocols and methods of treatment are also provided.