G-CSF site-specific mono-conjugates

US7893019B2 · kind B2 · utility

Assignee

• Bio-Ker SRL · IT

Inventors

• Giancarlo Tonon · Milano, IT
• Gaetano Orsini · Varese, IT
• Rodolfo Schrepfer · Villa Guardia, IT
• Geoffrey L. Taylor · Winnipeg, CA
• Mauro Sergi · Padova, IT

Key dates

• Filing date: Jul 30, 2007
• Grant date: Feb 22, 2011
• Expiry date: Jul 30, 2027

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P43/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

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 activity.