Drug intelligence / Profile preview

[18F]ENL30

Development stage
Preclinical
Lead developer
The City University of New York
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Positron Emitters → Radiopharmaceuticals, Small Molecules
Administration
Intravenous
01

Overview

`[18F]ENL30` is a fluorine-18 labeled small molecule positron emission tomography (PET) radiotracer designed to target the serotonin 5-HT7 receptor (5-HT7R). Developed as a derivative of the selective 5-HT7R antagonist SB-269970, `[18F]ENL30` is synthesized via a two-step labeling procedure involving the alkylation of SB-269970 with 2-[18F]fluoroethyl tosylate. It has been evaluated preclinically for imaging 5-HT7R expression in the central nervous system and, more recently, as a diagnostic biomarker in prostate cancer models, particularly for imaging androgen receptor (AR)-null tumors. Although `[18F]ENL30` exhibits high affinity and specific binding to 5-HT7R, preclinical studies in rodents have noted some off-target affinity for sigma receptors and susceptibility to P-glycoprotein (P-gp) efflux.

Other names
18F-ENL30[18F]15
02

Targets

HTR7 (5-hydroxytryptamine receptor 7)

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