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1. WO2008017603 - G-CSF SITE-SPECIFIC MONO-CONJUGATES

Publication Number WO/2008/017603
Publication Date 14.02.2008
International Application No. PCT/EP2007/057824
International Filing Date 30.07.2007
IPC
C07K 14/535 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
14Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435from animals; from humans
52Cytokines; Lymphokines; Interferons
53Colony-stimulating factor (CSF)
535Granulocyte CSF; Granulocyte-macrophage CSF
A61K 47/48 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
48the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
CPC
A61K 47/60
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
56the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
59obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
60the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A61P 31/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
04Antibacterial agents
A61P 43/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
A61P 7/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7Drugs for disorders of the blood or the extracellular fluid
C07K 14/535
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
14Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435from animals; from humans
52Cytokines; Lymphokines; Interferons
53Colony-stimulating factor [CSF]
535Granulocyte CSF; Granulocyte-macrophage CSF
Applicants
  • BIO-KER SRL [IT]/[IT] (AllExceptUS)
  • TONON, Giancarlo [IT]/[IT] (UsOnly)
  • ORSINI, Gaetano [IT]/[IT] (UsOnly)
  • SCHREPFER, Rodolfo [IT]/[IT] (UsOnly)
  • TAYLOR, Geoffrey [GB]/[IT] (UsOnly)
  • SERGI, Mauro [IT]/[IT] (UsOnly)
Inventors
  • TONON, Giancarlo
  • ORSINI, Gaetano
  • SCHREPFER, Rodolfo
  • TAYLOR, Geoffrey
  • SERGI, Mauro
Agents
  • PISTOLESI, Roberto
Priority Data
MI2006A00162411.08.2006IT
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) G-CSF SITE-SPECIFIC MONO-CONJUGATES
(FR) MONO-CONJUGUÉS DE G-CSF SITE SPÉCIFIQUES
Abstract
(EN)
Novel site-specific mono-conjugates of Granulocyte Colony Stimulating Factor (G-CSF) are hereby described, with analogues and derivatives thereof, which stimulate proliferation and differentiation of progenitor cells to mature neutrophiles. These conjugates have been obtained using transglutaminase to covalently and site-specifically bind a hydrophilic, non-immunogenic polymer to a single glutamine residue of the human G-CSF native sequence and analogues thereof. These novel site-specific mono-conjugated derivatives are recommended for therapeutic use since they are stable in solution and exhibit significant biological activity in vitro and a longer bloodstream half-life, as compared to the non-conjugated protein, with a consequent prolonged pharmacological activit y.
(FR)
La présente invention concerne de nouveaux mono-conjugués de Facteur de Stimulation des Colonies de Granulocytes (G-CSF) site spécifiques, ainsi que des analogues et des dérivés de ceux-ci, qui stimulent la prolifération et la différenciation de cellules progénitrices en neutrophiles matures. Ces conjugués ont été obtenus à l'aide de la transglutaminase pour lier de façon covalente et site spécifique un polymère hydrophile non-immunogène à un résidu glutamine unique de la séquence native du G-CSF humain et d'analogues de celle-ci. Ces nouveaux dérivés de mono-conjugués site spécifiques sont recommandés pour une utilisation thérapeutique dans la mesure où ils sont stables en solution et où ils présentent une activité biologique importante in vitro et une demi-vie prolongée dans le sang, par rapport à la protéine non conjuguée, avec en conséquence une activité pharmacologique prolongée.
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