Identification
- Summary
Choline C-11 is an imaging agent used in positron emission tomography imaging for suspected recurrent prostate cancer and non-informative bone scintigraphy, computerized tomography, or magnetic resonance imaging.
- Generic Name
- Choline C-11
- DrugBank Accession Number
- DB09563
- Background
Choline C 11 Injection is a radioactive diagnostic agent for positron emission tomography (PET) imaging of pat ients with suspected prostate cancer recurrence and non-informative bone scintigraphy, computerized tomography (CT) or magnetic resonance imaging.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Choline C-11 (DB09563)
- Weight
- Average: 103.173
Monoisotopic: 103.118424313 - Chemical Formula
- C5H14NO
- Synonyms
- (11)C-choline
- Choline C11
Pharmacology
- Indication
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. In clinical studies, imag es w ere produced with PET/CT coregistration.
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Diagnostic agent Prostate cancer •••••••••••• - Contraindications & Blackbox Warnings
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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.
- 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.
- Absorption
Not Available
- Volume of distribution
11C-choline distributes mainly to the pancreas, kidneys, liver, spleen and colon
- Protein binding
Not Available
- Metabolism
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).
- Route of elimination
Urinary excretion of 11C-choline was < 2% of the injected radioactivity at 1.5 hours after injection of the drug.
- Half-life
Not Available
- Clearance
The rate of 11C- choline excretion in urine was 0.014 mL/min.
- Adverse Effects
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Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.Not Available
- Food Interactions
- Drink plenty of fluids. Consuming lots of fluid before the PET/CT will reduce excess exposure to radiation by increasing urinary voiding.
- Take on an empty stomach. Avoid eating for at leats 6 hours before the administration of Choline C-11.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Choline C 11 Injection 33.1 mCi/1mL Intravenous Precision Nuclear Llc 2013-06-07 2014-06-07 US 
Choline C 11 Injection 33.1 mCi/1mL Intravenous Mayo Clinic 2012-09-12 2014-11-13 US Choline C 11 Injection 33.1 mCi/1mL Intravenous Mayo Clinic 2012-09-12 Not applicable US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Choline C 11 Injection 33.1 mCi/1mL Intravenous The University of Texas MD Anderson Cancer Center 2015-10-29 2017-07-18 US Choline C 11 Injection 33.1 mCi/1mL Intravenous Washington University School Of Medicine 2017-01-10 Not applicable US Choline C 11 Injection 4 mCi/1mL Intravenous Decatur Memorial Hospital 2019-11-06 Not applicable US Choline C 11 Injection 100 mCi/1mL Intravenous University Of Texas Md Anderson Cancer Center 2015-10-29 Not applicable US Choline C 11 Injection 4 mCi/1mL Intravenous Global Isotopes, Llc D/B/A Zevacor Molecular 2015-12-31 2019-05-17 US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Choline C 11 Choline C-11 (33.1 mCi/1mL) Injection Intravenous Precision Nuclear Llc 2013-06-07 2014-06-07 US Mic B12 Choline C-11 (1 mg/1mL) + Inositol (1 mg/1mL) + Mecobalamin (1 mg/1mL) + Methionine sulfoximine (1 mg/1mL) Injection Intramuscular Perdido Key Health And Wellness Inc 2015-11-23 Not applicable US
Categories
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as cholines. These are organic compounds containing a N,N,N-trimethylethanolammonium cation.
- Kingdom
- Organic compounds
- Super Class
- Organic nitrogen compounds
- Class
- Organonitrogen compounds
- Sub Class
- Quaternary ammonium salts
- Direct Parent
- Cholines
- Alternative Parents
- Tetraalkylammonium salts / 1,2-aminoalcohols / Primary alcohols / Organopnictogen compounds / Organic salts / Hydrocarbon derivatives / Organic cations
- Substituents
- 1,2-aminoalcohol / Alcohol / Aliphatic acyclic compound / Alkanolamine / Amine / Choline / Hydrocarbon derivative / Organic cation / Organic oxygen compound / Organic salt
- Molecular Framework
- Aliphatic acyclic compounds
- External Descriptors
- cholines (CHEBI:72322)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- M4AS4XGD4Q
- CAS number
- 94793-58-5
- InChI Key
- OEYIOHPDSNJKLS-BJUDXGSMSA-N
- InChI
- InChI=1S/C5H14NO/c1-6(2,3)4-5-7/h7H,4-5H2,1-3H3/q+1/i1-1
- IUPAC Name
- (2-hydroxyethyl)((11C)methyl)dimethylazanium
- SMILES
- C[N+](C)([11CH3])CCO
References
- General References
- FDA Approved Drug Products: Choline C 11 Injection, for intravenous use [Link]
- External Links
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 3 Completed Diagnostic Adenocarcinoma of Prostate 1 2 Recruiting Diagnostic Adenocarcinoma of Prostate / Biochemically Recurrent Prostate Carcinoma / PSA Failure / PSA Progression 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection Intravenous 100 mCi/1mL Injection Intravenous 33.1 mCi/1mL Injection Intravenous 4 mCi/1mL Injection Intramuscular - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Not Available
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 3.61 mg/mL ALOGPS logP -3.6 ALOGPS logP -4.7 Chemaxon logS -1.6 ALOGPS pKa (Strongest Acidic) 13.97 Chemaxon pKa (Strongest Basic) -3.2 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 1 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 20.23 Å2 Chemaxon Rotatable Bond Count 2 Chemaxon Refractivity 42.19 m3·mol-1 Chemaxon Polarizability 12.57 Å3 Chemaxon Number of Rings 0 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS splash10-05fr-9100000000-69389426dd865af031f9 Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 114.95599 predictedDeepCCS 1.0 (2019) [M+H]+ 117.50346 predictedDeepCCS 1.0 (2019) [M+Na]+ 125.969315 predictedDeepCCS 1.0 (2019)
Drug created at November 30, 2015 19:10 / Updated at June 12, 2020 16:52