发明名称 Tissue targeting
摘要 Methods and compositions related to targeting agents to tumor tissue are described.
申请公布号 US9387256(B2) 申请公布日期 2016.07.12
申请号 US201113641278 申请日期 2011.04.15
申请人 MOMENTA PHARMACEUTICALS, INC. 发明人 Zhou He;Cochran Edward;Kishimoto Takashi Kei
分类号 A61K9/00;A61K47/48;A61K31/00;A61K31/727;A61K49/00;A61K51/06 主分类号 A61K9/00
代理机构 Lando & Anastasi, LLP 代理人 Lando & Anastasi, LLP
主权项 1. A method of targeting a therapeutic or imaging agent to a tumor tissue of a patient, the method comprising (a) identifying a patient with a tumor tissue, wherein the patient is in need of administration of a therapeutic or imaging agent to treat or image the tumor; (b) providing a conjugate of the therapeutic or imaging agent and a polysaccharide preparation; and (c) administering the conjugate to the patient, wherein the polysaccharide preparation targets the conjugate to the tumor tissue, and wherein the polysaccharide preparation has the following characteristics: a weight average chain molecular weight between 3,500 and 8,000 Da; anti-Xa activity and anti-IIa activity each less than 50 IU/mg; and greater than 5% and less than 50% glycol split uronic acid residues; and wherein the polysaccharide preparation comprises polysaccharides of the Formula I: [Uw—Hx,y,z]m˜[UG—Hx,y,z]n  (I) wherein each occurrence of U indicates a uronic acid residue and each occurrence of H indicates a hexosamine residue; wherein m and n are integers such that m=4-16, and n=1-4; each of w, x, y and z can independently be the same or different for each occurrence of [Uw—Hx,y,z] and each of x, y and z can independently be the same or different for each occurrence of [UG—Hx,y,z], wherein w=-2OS or -2OH; x=-NS or -NAc; y=-3OS or -3OH; z=-6OS or -6OH; andwherein the symbol ˜ indicates that the units marked m and n are distributed along the polysaccharide chain and are not necessarily in sequence to thereby target the agent to the tumor tissue.
地址 Cambridge MA US