发明名称 CONJUGATION OF PHARMACEUTICALLY ACTIVE AGENTS WITH TRANSTHYRETIN LIGANDS THROUGH ADJUSTABLE LINKERS TO INCREASE SERUM HALF-LIFE
摘要 A delivery system for active agents, and methods of making and using the systems, are provided. The delivery systems have (i) a ligand that is selective for an endogeneous plasma protein in the serum of a subject; and, (ii) a linker configured for operatively attaching the ligand covalently to an active agent to increase the half-life of the active agent in the serum.
申请公布号 US2016045609(A1) 申请公布日期 2016.02.18
申请号 US201514804024 申请日期 2015.07.20
申请人 ALHAMADSHEH MAMOUN M. 发明人 ALHAMADSHEH MAMOUN M.;PARK MIKI S.;CHAN WILLIAM K.;LI XIAOLING;PENCHALA SRAVAN C.;MILLER MARK R.
分类号 A61K47/48;A61K49/00;A61K38/24;A61K31/4745;A61K38/06;A61K38/22 主分类号 A61K47/48
代理机构 代理人
主权项 1. A delivery system for an active agent, comprising: a ligand with (i) a high selectivity for a plasma protein endogeneous to the subject, the molecular weight of the plasma protein ranging from about 30 kDa to about 80 kDa; (ii) a high binding affinity, Kd, of at least 10−6 M for the plasma protein; and, (iii) a molecular weight ranging from about 200 Da to about 2000 Da; and, a linker that ranges in length from about 10 angstroms to about 50 angstroms, or from 8 atoms to 50 atoms; wherein, the active agent has a structure selected from the group consisting of a peptide, an oligopeptide, a polypeptide, a protein, an antibody, an oligonucleotide, a polynucleotide, a virus-like particle, a small molecule, an imaging agent, and combinations thereof.
地址 STOCKTON CA US