公开(公告)号：US20210190788A1

公开(公告)日：2021-06-24

申请号：US17129352

申请日：2020-12-21

Applicant: THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM

Inventor： James BRUGAROLAS ,  Xiankai SUN ,  Sashi DEBNATH

IPC: G01N33/574 ,  C07K14/47 ,  G01N33/534 ,  A61B6/03

Abstract: Provided herein are hypoxia inducible factor 2-alpha (HIF-2α)-specific radioactive tracers, methods of use thereof, and methods of synthesis thereof. Specifically, provided herein are HIF-2α-specific radioactive tracers comprising an HIF-2α-specific agent developed as a therapeutic inhibitor and a positron emitting radioactive label. Embodiments provide methods of detecting an HIF-2α-expressing tumor, detecting an HIF-2α inhibitor resistant tumor, evaluating a change in HIF-2α expression in response to an anti-cancer treatment, detecting acquisition of HIF-2α inhibitor resistance, evaluating efficacy of an HIF-2α depletion therapy, or detecting or monitoring an ischemic area in a subject. Also provided are methods of synthesizing an HIF-2α-specific radioactive tracer.

公开(公告)号：US20210187130A1

公开(公告)日：2021-06-24

申请号：US17153128

申请日：2021-01-20

Applicant: THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM

Inventor： James BRUGAROLAS ,  Xiankai SUN ,  Sashi DEBNATH

IPC: A61K51/04 ,  A61K49/00 ,  A61B6/03 ,  A61B6/00

Abstract: Provided herein are hypoxia inducible factor 2-alpha (HIF-2α)-specific radioactive tracers, methods of use thereof, and methods of synthesis thereof. Specifically, provided herein are HIF-2α-specific radioactive tracers comprising an HIF-2α-specific agent developed as a therapeutic inhibitor and a positron emitting radioactive label. Embodiments provide methods of detecting an HIF-2α-expressing tumor, detecting an HIF-2α inhibitor resistant tumor, evaluating a change in HIF-2α expression in response to an anti-cancer treatment, detecting acquisition of HIF-2α inhibitor resistance, evaluating efficacy of an HIF-2α depletion therapy, detecting or monitoring an ischemic area in a subject, or detecting and monitoring pulmonary hypertension in a subject. Also provided are methods of synthesizing an HIF-2α-specific radioactive tracer.