Choline C-11

Brand Names: Choline C 11

Drug Class: Radioactive Diagnostic Agent

Overview

11 DESCRIPTION 11.1 Chemical Characteristics Choline C 11 Injection is a positron emitting radiopharmaceutical that is used for diagnostic purposes in conjunction with PET imaging. The active ingredient, 11 C-choline, has the molecular formula of C 4 11 CH 14 NOCl with a molecular weight of 138.

Mechanism of Action

12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action 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. 12.2 Pharmacodynamics In a study of men with prostatic hyperplasia or primary prostate cancer, PET imaging showed 11 C-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...

Indications

  • 1 INDICATIONS AND USAGE Choline C 11 Injection is indicated for positron emission tomography (PET) imaging of patients with suspected prostate cancer recurrence and non-informative bone scintigraphy, computerized tomography (CT) or magnetic resonance imaging (MRI). In these patients, 11 C-choline PET imaging may help identify potential sites of prostate cancer recurrence for subsequent histologic confirmation. Suspected prostate recurrence is based upon elevated blood prostate specific antigen (PSA) levels following initial therapy.

Common Doses

  • Refer to label

Dosage

2 DOSAGE AND ADMINISTRATION Aseptically withdraw Choline C 11 Injection from its container and administer 370 – 740 MBq (10 – 20 mCi) as a bolus intravenous injection. The radioactivity dose (370 – 740 MBq, 10 – 20 mCi) is chosen based on patient body dimensions and the characteristics of the image acquisition system ( 2.1 ). Initiate imaging immediately after administration of Choline C 11 Injection and acquire static emission images 0 – 15 minutes from the time of injection ( 2.5 ). The effective radiation absorbed dose from 740 MBq (20 mCi) dose of Choline C 11 Injection is approximately 3.

Contraindications

  • 4 CONTRAINDICATIONS None. None ( 4 ).

Side Effects

  • 6 ADVERSE REACTIONS Exclusive of an uncommon, mild injection site reaction, no adverse reactions to 11 C-choline have been reported. Exclusive of an uncommon, mild injection site reaction, no other adverse reactions have been reported ( 6 ). To report SUSPECTED ADVERSE REACTIONS, contact Division of Nuclear Medicine, Department of Radiology, Mayo Clinic at 507-284-2511 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch

Interactions

  • 7 DRUG INTERACTIONS Colchicine and androgen-deprivation therapeutic drugs have been reported to interfere with choline-based PET imaging [ see Warnings and Precautions (5.1) ]. The impact of androgen-deprivation therapeutic drugs upon 11 C-choline PET imaging may depend upon the hormonal responsiveness of a patient’s recurrent prostate cancer. Clinical studies have not established this relationship but published reports suggest 11 C-choline PET imaging may be productive in patients with “hormone resistant” recurrent prostate cancer even if the patients are receiving anti-androgen therapy.