Drug intelligence / Profile preview

fluorine-18 fluorocholine

Development stage
Phase 3
Lead developer
Curium
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

Fluorine-18 fluorocholine is a radiopharmaceutical agent used primarily in positron emission tomography (PET) imaging. It functions as a radiotracer consisting of methylcholine labeled with the positron-emitting radioisotope fluorine-18. Upon administration, it incorporates into tumor cells through an active, carrier-mediated transport mechanism for choline and is then phosphorylated intracellularly by choline kinase, an enzyme frequently upregulated in human tumors. This phosphorylated form is integrated into phospholipids in the cell membrane as part of phosphatidylcholine. Since cancer cells typically have higher proliferation rates than normal cells, they exhibit increased uptake and incorporation of the tracer, enabling tumor visualization with PET imaging. It is primarily indicated for PET scans of prostate cancer, but has also shown utility in imaging breast carcinoma, brain tumors, hepatocellular carcinoma, and parathyroid adenomas.

Brand names
Fluorocholine F-18
Other names
(18F)Fluorocholine(18F)-CholineFluorocholine(18F)Fluourine-18 FluoromethylcholineFluourine18 FluoromethylcholineFluourine 18 FluoromethylcholineFluoromethylcholine (18F)Iasocholine
02

Targets

CHKA (Choline kinase)CHT1 (High-affinity choline transporter 1)

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