The invention describes a vitamin receptor binding drug delivery conjugate, and preparations therefor. The drug delivery conjugate consists of a vitamin receptor binding moiety, a bivalent linker (L), and a drug. The vitamin receptor binding moiety is a vitamin, or a vitamin receptor binding analog or a derivative thereof, and the drug includes analogs or derivatives thereof. The vitamin receptor binding moiety is covalently linked to the bivalent linker, and the drug, or the analog or the derivative thereof, is covalently linked to the bivalent linker, wherein the bivalent linker, where the bivalent linker (L) comprises one or more spacer linkers, releasable linkers, and heteroatom linkers. Methods and pharmaceutical compositions for eliminating pathogenic cell populations using the drug delivery conjugate are also described.
本发明描述了一种与
维生素受体结合的给药共轭物及其制剂。该给药共轭物由
维生素受体结合分子、二价连接体(L)和药物组成。
维生素受体结合分子是
维生素或
维生素受体结合类似物或其衍
生物,药物包括其类似物或衍
生物。
维生素受体结合分子与二价连接体共价连接,药物或其类似物或衍
生物与二价连接体共价连接,其中二价连接体(L)包括一个或多个间隔连接体、可释放连接体和杂原子连接体。此外,还描述了使用该给药共轭物消除致病细胞群的方法和药物组合物。