Insulin analogs and methods of use thereof

• Main Authors: VERDINO PAOLO, LEE, STEPHEN, L, BERNARD, MICHAEL, J., SR
• Format: Patent
• Language: Chinese; English
• Published: 11.03.2022
• Subjects: CHEMISTRY; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PEPTIDES; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

Insulin (INS) analogs are disclosed that include modifications compared to native human INS that increase half-life, maintain selectivity for insulin receptor (IR), and provide in vitro and in vivo stability to improve druggability and reduce immunogenicity. Also disclosed are pharmaceutical compositions comprising one or more INS analogs described herein in a pharmaceutically acceptable carrier. Also disclosed are methods of making and using the INS analogs, particularly for the treatment of metabolic conditions, diseases, or disorders, particularly for the treatment of diseases such as diabetes and obesity. 公开了胰岛素(INS)类似物，其包括与天然人INS相比的修饰，所述修饰增加半衰期、维持对胰岛素受体(IR)的选择性和提供体外和体内稳定性以改善成药性和降低免疫原性。还公开了药物组合物，其包括在药学上可接受的载体中的一种或多种本文所述的INS类似物。还公开了制备和使用INS类似物的方法，特别是用于治疗代谢病症、疾病或障碍，尤其是治疗疾病诸如糖尿病和肥胖。