Fluoromethylcholine [18F] Injection
Fluoromethylcholine [18F] injection, a positron-emitting radiopharmaceutical containing no carrier added (NCA) radioactive fluoride [18F], is used for diagnostic purposes in conjunction with positron emission tomography (PET) imaging. Choline is an important component in the buildup of phospholipid cell membranes; hence, fast proliferating cells may express high choline uptake. This property has been utilized in several PET studies with [18F]fluoromethylcholine for the detection and differential diagnosis of prostate cancer, breast carcinoma and brain tumors.
- Packaging: 15 mL multi-dose colorless glass vial, type I
- Calibration: 12:00 p.m. CET, same day
- Availability: Wednesday and Thursday. Only available for clinical trials or on patient name basis.
Fluoromethylcholine [18F] InjectionDownload
|Name||Fluoromethylcholine [18F] injection|
|Pharmaceutical form||solution for injection, multi-dose|
|Activity concentration||225 MBq/mL at time and date of calibration|
|Radiochemical purity||≥ 95%|
|pH and composition||4.5-7.5 / Fluoromethylcholine [18F], sodium chloride and water for injections|
|Storage||Storage in the original packaging at controlled room temperature (< 25 °C)|
|Expiry||9 hours after ART|
|Maximum volume||10 mL|
While phosphorylcholine is present at low levels in normal tissues, this enzyme reaches a high content in most cancers. Phosphorylcholine is the first intermediate in the stepwise incorporation of choline into phospholipids . Choline is a body-own substance and is necessary for the normal function of the mammalian organism. In the human body, choline is needed for the synthesis of phospholipids in cell membranes, methyl metabolism, transmembrane signaling, and lipid-cholesterol transport and metabolism. Intracellular choline is rapidly metabolized to phosphorylcholine (PC); the phosphorylation is catalyzed by the enzyme choline kinase. Once phosphorylated, the polar PC molecule is trapped within the cell .
The biological basis for radiolabeled choline uptake in tumors is the malignancy-induced upregulation of choline kinase, which leads to the incorporation and trapping of choline in the form of phosphatidylcholine (lecithin) in the tumor cell membrane . Various published studies have revealed an increased choline uptake as well as an upregulated activity of choline kinase and elevated levels of PC in cancer cells .
Based on the increased choline uptake in tumor cells, [11C]choline was developed. [18F]-labeled choline analog has also been synthesized and investigated, the superior [18F]-labeling being justified on grounds of longer half-life (109 minutes versus 20 minutes in the case of [11C]) and shorter positron range .
The biodistribution of [18F]-labeled choline is very similar to that of choline, except for the very rapid urinary excretion. For this reason, [18F]-radiolabeled choline is extremely feasible to reflect pharmacological behavior of choline itself. The efficacy of radiolabeled choline for localizing primary or metastatic prostate cancer has now been studied extensively .
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(Click on the PMID to see abstracts from PubMed/NCBI)
 Hara T, Koasaka N. Development of 18F-Fluoroethylcholine for Cancer Imaging with PET: Synthesis, Biochemistry, and Prostate Cancer Imaging. J Nucl Med; 43:187–199, 2002. PMID: 11850483.
 Schoeder H, Larson S. Positron Emission Tomography for Prostate, Bladder and Renal Cancer. Sem Nucl Med 34:274-292, 2004. PMID: 15493005.
 Jadvar H. Prostate Cancer: PET with 18F-FDG, 18F- or 11C-Acetate, and 18F- or 11C-Choline. J Nucl Med; 52:81–89, 2011. PMID: 21149473.
 Ratnam S, Kent C. Early increase in choline kinase activity upon induction of the H-ras oncogene in mouse fibroblast cell lines. Arch Biochem Biophys 323:313-322, 1995. PMID: 7487093.
 Ackerstaff E, Pflug BR, Nelson JB, et al. Detection of increased choline compounds with proton nuclear magnetic resonance spectroscopy subsequent to malignant transformation of human prostatic epithelial cells. Cancer Res 61:3599-3603, 2001. PMID: 11325827.
 Katz-Brull R, Degani H. Kinetics of choline transport and phosphorylation in human breast cancer cells; NMR application of the zero trans method. Anticancer Res 16:1375-1380, 1996. PMID: 8694504.
 DeGrado T, Baldwin S. Synthesis and evaluation of (18)F-labeled choline analogs as oncologic PET tracers. J Nucl Med 42:1805-1814, 2001.PMID: 11752077.
 Price D, Coleman R. Comparison of [18 F]fluorocholine and [18 F]fluorodeoxyglucose for positron emission tomography of androgen dependent and androgen independent prostate cancer. J Urol 168:273-280, 2002. PMID: 12050555.
 Picchio M, Messa C. Value of [11C]choline-positron emission tomography for re-staging prostate cancer: a comparison with [18F]fluorodeoxyglucose-positron emission tomography. J Urol 169:1337-1340, 2003. PMID: 12629355.
 Kotzerke J, Prang J. Experience with carbon-11choline positron emission tomography in prostate carcinoma. Eur J Nucl Med 27:1415-1419, 2000. PMID: 11007527.
 de Jong IJ, Pruim J, Elsinga PH, et al. Visualization of prostate cancer with 11C-choline positron emission tomography. Eur Urol 42:18-23, 2002. PMID: 12121724.
 de Jong IJ, Pruim J, Elsinga PH, et al. Preoperative staging of pelvic lymph nodes in prostate cancer by (11C)-choline PET. J Nucl Med 44:331-335, 2003. PMID: 12620996.
 de Jong IJ, Pruim J, Elsinga PH, et al. 11C-choline positron emission tomography for the evaluation after treatment of localized prostate cancer. Eur Urol 44:32-38, 2003; discussion 38-39. PMID: 12814672.
BV Cyclotron VU is a global health science company that produces radiopharmaceuticals and radiochemicals for medical diagnostics and research. Located at the campus of VU University Medical Center in Amsterdam, BV Cyclotron VU produces GMP-compliant medical isotopes in state-of-the-art manufacturing facilities. They are used daily by pharmaceutical and biotechnological companies, medical device manufacturers, hospitals, clinics, and research laboratories.
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