Drug intelligence / Profile preview

18F-choline

Development stage
Phase 3
Lead developer
Iason
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

**18F-choline** is a radiolabeled choline analog used as a positron emission tomography (PET) imaging agent. It is primarily utilized for the detection and staging of prostate cancer and for identifying biochemical recurrence after initial treatment. The compound consists of choline labeled with the radioisotope fluorine-18 (half-life ~110 minutes), which allows for centralized production and distribution to imaging centers without on-site cyclotrons[3][5][6]. Mechanistically, 18F-choline is taken up by cells via choline transporters and phosphorylated by choline kinase; its accumulation reflects increased cell membrane synthesis—a hallmark of proliferating tumor cells such as those in prostate cancer[3][9]. This property enables sensitive detection of both primary tumors and metastatic lesions. Beyond prostate cancer, 18F-choline PET/CT has shown utility in preoperative localization of parathyroid adenomas in primary hyperparathyroidism due to its superior sensitivity compared to conventional nuclear medicine techniques[7]. It has also been explored for imaging other cancers like hepatocellular carcinoma[3]. The agent offers advantages over other tracers such as longer half-life than carbon-11-labeled compounds (e.g., 11C-choline), enabling broader clinical use. However, newer agents like PSMA-targeted tracers may offer higher sensitivity/specificity in some settings.

Brand names
Iasocholine
Other names
18F-fluoromethylcholinefluoromethylcholine F-18
02

Targets

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

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