Drug intelligence / Profile preview

[18F]FCFN

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

Overview

[18F]FCFN (fluorine-18 labeled fluorocarfentanil) is a positron emission tomography (PET) radiotracer developed as a safer, more widely accessible alternative to carbon-11 labeled carfentanil ([11C]CFN) for neuroimaging of the mu-opioid receptor (MOR) system. Carfentanil is an extremely potent synthetic opioid, which poses safety risks and has limited clinical research utility due to the short 20.4-minute half-life of carbon-11. In contrast, [18F]FCFN can be manufactured at higher molar activity, administered at lower, safer doses, and benefits from the longer half-life of fluorine-18 (109.8 minutes). Preclinical evaluations in rodents and non-human primates demonstrate that [18F]FCFN exhibits rapid brain uptake, favorable pharmacokinetics, and high specific binding in MOR-rich brain regions (such as the thalamus) with low non-specific binding, making it a promising tool for studying opioid addiction neurobiology and receptor availability.

Other names
[18F]fluorocarfentanilfluorocarfentanil
02

Targets

MOR (Mu opioid receptor)

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