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US 9,872,864 B2Granted
Sustained release composition of prostacyclin
AssigneeAscendis Pharma A/S
InventorsKennett Sprogøe, Harald Rau, Ulrich Hersel, Thomas Wegge, Oliver Keil, Joachim Zettler
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Abstract
The present invention relates to sustained release compositions of prostacyclin, as well as uses thereof, in particular for the prevention and/or treatment of pulmonary arterial hypertension.
Claims13
A pharmaceutical composition comprising:
- a treprostinil carrier-linked prodrug;
- and
- optionally one or more pharmaceutically acceptable excipients;
- wherein the concentration of the treprostinil carrier-linked prodrug is sufficient to maintain a therapeutically effective level of treprostinil in blood plasma for at least 12 hours after a single subcutaneous or intramuscular injection;
- and
- wherein the treprostinil carrier-linked prodrug comprises:
- a treprostinil drug;
- and
- a promoiety, which promoiety comprises:
- a carrier;
- a reversible prodrug linker moiety;
- and
- optionally one or more spacer moieties;
- wherein one end of the reversible prodrug linker moiety is attached to the treprostinil through a reversible linkage;
- wherein another end of the reversible prodrug linker moiety is attached through a permanent bond to either a spacer moiety permanently attached to the carrier moiety, or is directly attached through a permanent bond to the carrier moiety;
- and
- wherein the prodrug linker moiety is non-enzymatically hydrolytically degradable.
14 more elements
Dependencies are inferred from the claim text.