Drug intelligence / Profile preview

[18F]F-ERi

Development stage
Preclinical
Lead developer
Yale University
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Positron Emitters → Radiopharmaceuticals, Small Molecules
Administration
Intravenous
01

Overview

[18F]F-ERi is a non-steroidal, fluorine-18 labeled radiotracer designed for positron emission tomography (PET) imaging of estrogen receptor alpha (ERα). Developed as an alternative to the steroidal tracer [18F]F-FES (fluoroestradiol), [18F]F-ERi is based on a diaryltetrahydronaphthalene scaffold (derived from the selective estrogen receptor modulator lasofoxifene) modified with a piperazine linker. It exhibits high selectivity and nanomolar affinity for ERα, with significantly lower binding to ERβ. Preclinical studies in breast cancer models demonstrate ERα-specific tumor uptake, favorable tumor-to-background contrast, and rapid brain uptake, highlighting its potential for both breast cancer characterization and neuroimaging.

Other names
18F-ERi[18F]F-ERi PET
02

Targets

ESR1 (ERα)

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