Degarelix organic solvent formulations
OwnerJohn Downing, Bennet Harding +4inventors
InventorsJohn Downing, Bennet Harding, Dileep Janagam, Jinqiu Xu, David Loffredo, Natalie Akagi Bath
Life of this patent
Estimating the term…
Abstract
Described herein are long-acting injectable compositions as well as methods of using such long-acting injectable compositions. The long-acting injectable compositions comprise degarelix (a decapeptide gonadotropin-releasing hormone (GnRH) receptor antagonist) or a pharmaceutically acceptable salt thereof. These compositions can also comprise a biocompatible organic solvent, optionally with one or more additives in a single syringe system.
Claims39
A composition, comprising:
- a therapeutically effective amount of degarelix or a pharmaceutically acceptable salt thereof;
- and
- an organic biocompatible solvent selected from dimethyl sulfoxide (DMSO) and N-methyl-2-pyrrolidone (NMP),
- wherein:
- the composition is free of any biodegradable polymer;
- the composition is formulated for subcutaneous injection into a subject;
- a single dose of the composition is provided in a volume of about 2 mL or less;
- and
- upon a single injection into the subject, the composition forms an in situ depot that releases the degarelix or the pharmaceutically acceptable salt thereof over a time period of at least about 2 months.
4-6. (canceled)
8-9. (canceled)
11-12. (canceled)
14-17. (canceled)
19-24. (canceled)
27-30. (canceled)
(canceled)
34-40. (canceled)
42-45. (canceled)
52-59. (canceled)
62-71. (canceled)
A composition comprising:
- (a) degarelix or a pharmaceutically acceptable salt thereof in an amount of from about 31 wt % to about 33 wt % degarelix free base equivalent;
- and
- (b) dimethyl sulfoxide (DMSO);
- wherein the composition is free of any biodegradable polymer.
A composition comprising:
- (a) degarelix of a pharmaceutically acceptable salt thereof in an amount of from about 20 wt % to about 40 wt % degarelix free base equivalent;
- (b) N-methyl-2-pyrrolidone (NMP);
- and
- (c) an acid additive or an alcohol additive;
- wherein the composition is free of any biodegradable polymer.
Dependencies are inferred from the claim text.