Myristoylated leptin-related peptides and uses thereof

• Main Authors: NOVAKOVIC ZACHARY, GRASSO PATRICIA
• Format: Patent
• Language: Chinese; English
• Published: 31.05.2017
• Subjects: HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

A pharmaceutical compound for the treatment of obesity related disorder that is a conjugate of myristic acid and a leptin-related peptide. Preferably, the leptin-related peptide is OB3 that has been D-substituted at Leu-4. The resulting conjugate significantly improved the pharmacokinetic profile of the leptin-related peptide by extending its half-life from less than one hour to as long as twenty-eight hours, depending on the route of delivery, increasing uptake, reducing the rate of plasma clearance, and enabling the minimal effective dose to be reduced several fold. 种用于治疗与肥胖相关的疾病的药物化合物，其为肉豆蔻酸和瘦素相关肽的缀合物。优选地，所述瘦素相关肽为在Leu-4处被D-取代的OB3。通过使半衰期从小于1小时延长至长达28小时(这取决于递送途径)、增加吸收、降低血浆清除速率以及使最小有效剂量降低数倍，所得的缀合物显著地改善了瘦素相关肽的药代动力学特征。