SSTR-TARGETED CONJUGATES AND PARTICLES AND FORMULATIONS THEREOF

Conjugates of an active agent such as DM1 attached to a targeting moiety, such as a somatostatin receptor binding moiety, via a linker, and particles comprising such conjugates have been designed. Such conjugates and particles can provide improved temporospatial delivery of the active agent, improve...

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Bibliographische Detailangaben
Hauptverfasser: LIM SOO PATRICK, SWERYDA-KRAWIEC BEATA, ALARGOVA ROSSITZA G, ALLAND LEILA, SHINDE RAJESH R, SEARS CHRIS
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:Conjugates of an active agent such as DM1 attached to a targeting moiety, such as a somatostatin receptor binding moiety, via a linker, and particles comprising such conjugates have been designed. Such conjugates and particles can provide improved temporospatial delivery of the active agent, improved biodistribution and penetration in tumor, and/or decreased toxicity. Methods of making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer. 已设计经由连接体连接至靶向部分(诸如生长激素抑制素受体结合部分)的活性物质(诸如DM1)的缀合物和包含此类缀合物的颗粒。此类缀合物和颗粒可提供改善的活性物质时空递送;改善的生物分布和在肿瘤中的渗透;和/或降低的毒性。提供制备缀合物、颗粒及其制剂的方法。提供向有需要的受试者施用制剂以例如治疗或预防癌症的方法。