Choline C-11

FDA approved drugs -> Active ingredient

FDA approved drugs -> Active ingredient

Drug Induced Liver Injury Rank (DILIrank 2.0)

Choline c-11

vNo-DILI-concern

0

No match

DOI:10.1016/j.drudis.2016.02.015

Choline is phosphorylated by choline kinase into phosphorylcholine. This phosphorylated form gets trapped inside the cell. Cancer cells exhibit an increased cell wall membrane synthesis as well as an increased activity of choline kinase. Choline C11 presents a small tracer activity in the urinary collecting system and this property makes it a very noble compound in the evaluation of ureters and bladder.

In a study of men with prostatic hyperplasia or primary prostate cancer, PET imaging showed 11C-choline radioactivity accumulated rapidly within the prostate; uptake appeared to peak by five minutes following injection of the drug and activity was retained over the subsequent 30 minute scanning period. Little uptake was observed in the bladder and rectum.

Choline is incorporated into phosphatidylcholine which is a major membrane phospholipid in mammalian cells. The use of choline C11 is based on the knowledge that malignant tumors with increased cellular proliferation take up more choline when compared with normal cells for the formation of cellular membranes. The increased uptake of choline is explained by its use as a substrate in phospholipid synthesis in cell membranes, transmembrane signaling, and lipid and cholesterol transport and metabolism.

Choline C 11 Injection is a radiolabeled analog of choline, a precursor molecule essential for the biosynthesis of cell membrane phospholipids. Choline is involved in synthesis of the structural components of cell membranes, as well as modulation of trans-membrane signaling. Increased phospholipid synthesis (i.e., increased uptake of choline) has been associated with cell proliferation and the transformation process that occurs in tumor cells.

Choline C11 is phosphorylated by choline kinase and incorporated into phospholipids in the body. In some of the tissues, choline oxidation is prominent. The oxidative metabolite of choline is betaine which is the major metabolite of choline C11. A small portion of the administered dose remains unchanged 40 minutes after administration.

Following intravenous administration, 11C-choline undergoes metabolism resulting in the detection of 11C- betaine as the major metabolite in blood. In a study of patients with prostate cancer or brain disorders, the fractional activities of 11C-choline and 11C- betaine in human arterial plasma appeared to reach a plateau within 25 minutes, with 11C- betaine representing 82% ± 9% of the total 11C detected at that time point. A small amount of unmetabolized 11C-choline was detected within the blood at the final sampling time point (40 minutes).