Conjugate based systems for controlled insulin delivery

US11820805B2 · kind B2 · utility

Assignee

• Merck Sharp & Dohme LLC · US

Inventors

• Lin Yan · East Brunswick Township, US
• Pei Huo · Millburn, US
• Ahmet Kekec · Jersey City, US
• Danqing Feng · Green Brook, US
• Yuping Zhu · Edison, US
• Dmitri Pissarnitski · Scotch Plains, US
• Chris R. Moyes · Westfield, US
• Songnian Lin · Sparta, US

Key dates

• Filing date: Dec 13, 2018
• Grant date: Nov 21, 2023
• Expiry date: Nov 22, 2039

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K38/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present disclosure provides conjugates that comprise an insulin molecule conjugated via a conjugate framework to two or more separate ligands that each include a saccharide, wherein the framework, ligand, saccharide and insulin molecule optionally comprise a fatty chain (e.g., a C8-30 fatty chain), wherein when said insulin molecule is conjugated both to a C8-30 fatty chain and one or more separate ligands that each include a saccharide, said C8-30 fatty chain is linked to insulin molecule only, and wherein when the framework or ligand comprises a fatty chain the insulin molecule is conjugated to two or more separate ligands. In certain embodiments, a conjugate is characterized in that, when the conjugate is administered to a mammal, at least one pharmacokinetic (PK) and/or pharmacodynamic (PD) property of the conjugate is sensitive to serum concentration of a second saccharide. In certain embodiments, a conjugate is also characterized by having a protracted PK profile. Exemplary conjugates and sustained release formulations are provided in addition to methods of use and preparation.