HSP90-TARGETING CONJUGATES AND FORMULATIONS THEREOF

Conjugates of an active agent attached to a targeting moiety, such as an HSP90 binding moiety, via a linker, and particles comprising such conjugates have been designed. Such conjugates and particlescan provide improved temporospatial delivery of the active agent, improved biodistribution and penetr...

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Hauptverfasser: BILODEAU MARK T, KADIYALA SUDHAKAR, CIRELLO AMANDA L, MOREAU B, PERINO SAMANTHA, WOOSTER RICHARD, WHITE BRIAN H, CIPRIANI TYLER, QUINN JAMES M, WHALEN KERRY
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:Conjugates of an active agent attached to a targeting moiety, such as an HSP90 binding moiety, via a linker, and particles comprising such conjugates have been designed. Such conjugates and particlescan 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 theformulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer. 已设计了经由连接体连接至靶向部分(如HSP90结合部分)的活性物质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。提供了制备缀合物、颗粒及其制剂的方法。提供了向有需要的受试者施用该制剂例如治疗或预防癌症的方法。