Compositions containing the anti-angiogenic phscn-peptide

Details Compositions containing the anti-angiogenic phscn-peptide Compositions containing the anti-angiogenic phscn-peptide

A - Human Necessities

61

K

A61K 38/04 (2006.01)

Patent

CA 2596255

Described herein are compositions/formulations of the Cys-containing anti- angiogenic peptide Pro-His-Ser-Cys-Asn (preferably in its capped form as Ac- PHSCN-NH2) or acid addition salts thereof or analogue thereof, that comprise at least one additional compound that stabilizes the peptide or analogue against spontaneous tandem dimerization or higher oligomerization. Preferred formulations include an acidic buffer such as citrate, glycine as an excipient and bulking agent. Optional additional components of the formulation are a reducing agent, a non-thiol biocompatible anti-oxidant, a lyoprotectant (typically one or more sugars, one or more amino acids, one or more methylamine, one or more lyotropic salts, and/or one or more polyols. Also provided is an article of manufacture or kit comprising the formulation in solution or in lyophilized form. A method of inhibiting angiogenesis in a subject, comprising administering to the subject the peptide in the above formulation is also disclosed.

L'invention concerne des compositions/préparations du peptide Pro-His-Ser-Cys-Asn anti-angiogénique contenant une cystéine (de préférence sous sa forme coiffée Ac-PHSCN-NH2) ou de sels d'addition d'acide dudit peptide ou d'un analogue dudit peptide, comprenant au moins un composé supplémentaire qui stabilise le peptide ou un analogue contre la dimérisation en tandem spontanée ou l'oligomérisation plus élevée. Les préparations préférées comprennent un tampon acide tel que du citrate, de la glycine en tant qu'excipient et agent gonflant. Les constituants supplémentaires éventuels de la préparation sont un agent réducteur, un anti-oxydant biocompatible non thiol, un lyoprotecteur (généralement un ou plusieurs sucres, un ou plusieurs acides aminés, une ou plusieurs méthylamines, un ou plusieurs sels lyotropiques, et/ou un ou plusieurs polyols. L'invention concerne également un article manufacturé ou un nécessaire comprenant la préparation en solution ou sous forme lyophilisée. L'invention concerne enfin un procédé d'inhibition de l'angiogenèse chez un sujet, consistant à administrer au sujet le peptide contenu dans la préparation susmentionnée.

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