Manufacture of degarelix

Patent metadata

Field	Value
Publication number	US-2021138024-A1
Application number	US-202117154690-A
Country	US
Kind code	A1
Filing date	Jan 21, 2021
Priority date	Jun 1, 2012
Publication date	May 13, 2021
Grant date	—

Abstract

The present invention provides methods for producing a lyophilized degarelix product which, upon reconstitution with water for injection in an amount of 20 mg/ml, shows a viscosity of up to 15 mPas. The present invention also provides a lyophilized degarelix drug substance which shows, upon dissolution in water in an amount of 20 mg/ml, a viscosity of up to 3.2 mPas, a and processes for providing this lyophilized degarelix drug substance.

First claim

1 - 22 . (canceled)

23 . A lyophilized degarelix drug substance consisting essentially of degarelix, 4.5% to 10.00% (w/w) acetic acid, and up to 10% (w/w) water, wherein the lyophilized degarelix drug substance has a viscosity of up to 3.2 mPas, as determined upon dissolution in an amount of 20 mg degarelix free base in 1 ml of water containing 2.5% (w/V) mannitol.

24 . The lyophilized degarelix drug substance of claim 23 , wherein the lyophilized degarelix drug substance has a viscosity ranging from 1.15 to 2.0 mPas, as determined upon dissolution in an amount of 20 mg degarelix free base in 1 ml of water containing 2.5% (w/V) mannitol.

25 . The lyophilized degarelix drug substance of claim 24 , wherein the viscosity is determined after 240 minutes of producing the degarelix drug substance.

26 . The lyophilized degarelix drug substance of claim 23 , wherein the lyophilized degarelix drug substance shows an optical density of 0.10 AU or less at a concentration of 20 mg degarelix free base/ml in 2.5% aqueous mannitol.

27 . The lyophilized degarelix drug substance of claim 26 , wherein the optical density is determined after 240 minutes of producing the degarelix drug substance.

28 . A stock solution comprising the lyophilized degarelix drug substance of claim 23 , having a concentration of 5, 15, 25, or 35 mg/ml of degarelix.

29 . The lyophilized degarelix drug substance of claim 23 , further containing impurities due to the production process, if any.

Assignees

• Ferring Bv

Inventors

• Schwach Grégoire
• Nilsson Anders
• Gottschalk Bøving Tine Elisabeth
• Rasmussen Jon Holbech
• Mörnstam Birgitta
• Tsirk Anders
• Annby Ulf
• Fomsgaard Jens

Classifications

• A61K38/09

  Luteinising hormone-releasing hormone [LHRH] {, i.e. Gonadotropin-releasing hormone [GnRH]}; Related peptides · CPC title

• C07K7/23

  Luteinising hormone-releasing hormone [LHRH]; Related peptides · CPC title

• A61K9/0024

  Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue (compositions for intravenous administration, normal injectable solutions or dispersions for, e.g. subcutaneous administration A61K9/0019; brain implants A61K9/0085; (coated) prostheses, catheters or stents A61L) · CPC title

• A61K47/26

  Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin · CPC title

• A61K9/1623

  Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules · CPC title