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1. (WO2017019520) COMPOSITIONS AND METHODS OF CERENKOV TARGETED AND ACTIVATED IMAGING AND THERAPEUTICS

Pub. No.:    WO/2017/019520    International Application No.:    PCT/US2016/043601
Publication Date: Fri Feb 03 00:59:59 CET 2017 International Filing Date: Sat Jul 23 01:59:59 CEST 2016
IPC: A61K 51/04
A61P 35/00
Applicants: MEMORIAL SLOAN KETTERING CANCER CENTER
Inventors: GRIMM, Jan
DAS, Sudeep
Title: COMPOSITIONS AND METHODS OF CERENKOV TARGETED AND ACTIVATED IMAGING AND THERAPEUTICS
Abstract:
Described herein are compositions and methods that confine Cerenkov light to a localized area for targeted treatment and/or imaging of tumor cells. In certain embodiments, such compositions include a Cerenkov-activated tagging agent comprising a payload and a covalent binding unit such as an azide. The payload can be an imaging agent, a contrast agent, and/or a therapeutic. In certain embodiments, a radiolabelled biomarker (e.g., 18F-FDG (fluorodeoxyglucose), 18F-FLT (fluorothymidine)) or other radiolabelled tumor cell targeting agent that emits Cerenkov luminescence is also administered. Upon local illumination by the Cerenkov luminescence at or near the location of the tumor cells, the payload (the imaging agent, contrast agent, and/or therapeutic) is activated. In this way, activation of the imaging agent, contrast agent, and/or therapeutic agent is limited to the region at or near the location of the tumor cells.