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Radiolabeled and fluorescent PARP inhibitors for imaging and radiotherapy

Patent ·
OSTI ID:1860020
; ; ; ; ;
The present disclosure relates to compounds of Formula I and II, wherein R1-R20 and FL are defined herein. Also provided are methods of targeting alpha-radiation to poly(ADP-ribose)polymerase 1 (PARP-1) enzyme expression, reducing proliferation of cancer cells, reducing proliferation of cancer cells, detecting intact and enzymatically active poly(ADP-ribose)polymerase 1 (PARP-1) enzyme expression, detecting PARP-1 enzyme expression in a subjects tissue sample, monitoring cancer treatment in a subject, or detecting a PARP-1 receptive cancer in a subject.
Research Organization:
Univ. of Pennsylvania, Philadelphia, PA (United States)
Sponsoring Organization:
USDOE; National Institutes of Health (NIH)
DOE Contract Number:
SC0012476;
Other Award/Contract Number:
CA138835
CA17494
Assignee:
The Trustees of the University of Pennsylvania (Philadelphia, PA)
Patent Number(s):
11,161,865
Application Number:
16/616,049
OSTI ID:
1860020
Country of Publication:
United States
Language:
English

References (6)

The pre-clinical characterization of an alpha-emitting sigma-2 receptor targeted radiotherapeutic journal January 2016
Rapid Cu-Catalyzed [ 211 At]Astatination and [ 125 I]Iodination of Boronic Esters at Room Temperature journal March 2018
PARP-1 Expression Quantified by [18F]FluorThanatrace: A Biomarker of Response to PARP Inhibition Adjuvant to Radiation Therapy journal February 2017
A Radiotracer Strategy to Quantify PARP-1 Expression In Vivo Provides a Biomarker That Can Enable Patient Selection for PARP Inhibitor Therapy journal June 2016
Abstract C15: Predicting response to PARP inhibitors through quantitative measurements of PARP activity in live BRCA1 mutated cells with a radio-iodinated PARP inhibitor journal December 2015
Abstract B31: Poly(ADP-ribose) Polymerase 1 as a novel target for alpha-particle therapy in high-risk neuroblastoma journal April 2017

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