Identification
- Summary
Technetium Tc-99m mebrofenin is a diagnostic radiopharmaceutical agent used during hepatobiliary imaging tests.
- Generic Name
- Technetium Tc-99m mebrofenin
- DrugBank Accession Number
- DB09137
- Background
Technetium Tc 99m Mebrofenin is a diagnostic radiopharmaceutical composed of diisopropyl-iminodiacetic acid (DISIDA) attached to a technetium-99m ion. Following intravenous injection, single photon emission computer tomography (SPECT) imaging of the liver or gallbladder is performed using a gamma camera to detect the gamma rays emitted by the technetium-99m as it decays. This is possible as Technetium-99m decays by isomeric transition to technetium-99 through the release of a gamma ray. Liver and gallbladder imaging is enabled through attachment to mebrofenin as this molecule has high hepatic uptake and fast biliary excretion, resulting in improved hepatic imaging. More specifically, mebrofenin is taken up into hepatocytes through the action of OATP1B1 and OATP1B3 transporters.
Currently available within a sterile kit, Tc-99m Mebrofenin is indicated for imaging of the liver and gallbladder.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Technetium Tc-99m mebrofenin (DB09137)
- Weight
- Average: 484.23
Monoisotopic: 483.05 - Chemical Formula
- C15H19BrN2O5Tc
- Synonyms
- Bis(2-[[2-(3-bromo-2,4,6-trimethylanilino)-2-oxoethyl]-(carboxymethyl)amino]acetate) technetium
- Technetium (99mTc) mebrofenin
- Technetium Tc 99m diisopropyl-iminodiacetic acid
- Technetium Tc 99m DISIDA
- Technetium Tc 99m Mebrofenin
Pharmacology
- Indication
Technetium Tc 99m Mebrofenin is indicated as a hepatobiliary imaging agent.
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Not Available
- Mechanism of action
Technetium Tc 99m Mebrofenin has no known pharmacologic activity at the recommended doses. It is used as a diagnostic agent as Technetium-99m decays by isomeric transition to technetium-99 through the release of a detectable gamma ray.
- Absorption
Visualisation in the liver could be detected by 5 minutes and maximum liver uptake occurred at 11 minutes post-injection. Hepatic duct and gallbladder visualization occurred by 10 to 15 minutes and intestinal activity was visualized by 30 to 60 minutes in subjects with normal hepatobiliary function The mean percent injected dose remaining in the blood at 10 minutes was 17%.
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
The mean percent injected dose excreted in the urine during the first 3 hours was 1%.
- Half-life
Technetium Tc 99m decays by isomeric transition with a physical half-life of 6.02 hours.
- Clearance
Following intravenous administration in normal subjects, Technetium Tc 99m Mebrofenin was rapidly cleared from the circulation.
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbacavir Abacavir may decrease the excretion rate of Technetium Tc-99m mebrofenin which could result in a higher serum level. Aceclofenac Aceclofenac may decrease the excretion rate of Technetium Tc-99m mebrofenin which could result in a higher serum level. Acemetacin Acemetacin may decrease the excretion rate of Technetium Tc-99m mebrofenin which could result in a higher serum level. Acetaminophen Acetaminophen may decrease the excretion rate of Technetium Tc-99m mebrofenin which could result in a higher serum level. Acetazolamide Acetazolamide may increase the excretion rate of Technetium Tc-99m mebrofenin which could result in a lower serum level and potentially a reduction in efficacy. Acetylcysteine The excretion of Technetium Tc-99m mebrofenin can be decreased when combined with Acetylcysteine. Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Technetium Tc-99m mebrofenin which could result in a higher serum level. Aclidinium Aclidinium may decrease the excretion rate of Technetium Tc-99m mebrofenin which could result in a higher serum level. Acrivastine Technetium Tc-99m mebrofenin may decrease the excretion rate of Acrivastine which could result in a higher serum level. Acyclovir Acyclovir may decrease the excretion rate of Technetium Tc-99m mebrofenin which could result in a higher serum level. 
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- Take on an empty stomach. Administer Technetium Tc-99m mebrofenin at least 4 hours after food to avoid false positives caused by food stimulating emptying of the gallbladder.
Products
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Categories
- ATC Codes
- V09DA04 — Technetium (99mtc) mebrofenin
- Drug Categories
- Amines
- Amino Acids
- Amino Acids, Peptides, and Proteins
- Compounds used in a research, industrial, or household setting
- Diagnostic Radiopharmaceuticals
- Diagnostic Uses of Chemicals
- Drugs that are Mainly Renally Excreted
- Hepatic and Reticulo Endothelial System
- Indicators and Reagents
- Laboratory Chemicals
- OATP1B1/SLCO1B1 Substrates
- OATP1B3 substrates
- Organometallic Compounds
- Radioactive Diagnostic Agent
- Radiopharmaceutical Activity
- Radiopharmaceuticals
- Technetium (99Mtc) Compounds
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- F2NQ468L52
- CAS number
- 1415247-71-0
- InChI Key
- JLJSYHOPCNWUNE-UHFFFAOYSA-N
- InChI
- InChI=1S/C15H19BrN2O5.Tc/c1-8-4-9(2)15(10(3)14(8)16)17-11(19)5-18(6-12(20)21)7-13(22)23;/h4H,5-7H2,1-3H3,(H,17,19)(H,20,21)(H,22,23);
- IUPAC Name
- 2-({[(3-bromo-2,4,6-trimethylphenyl)carbamoyl]methyl}(carboxymethyl)amino)acetic acid technetium
- SMILES
- [Tc].CC1=CC(C)=C(Br)C(C)=C1NC(=O)CN(CC(O)=O)CC(O)=O
References
- General References
- Krishnamurthy GT, Turner FE: Pharmacokinetics and clinical application of technetium 99m-labeled hepatobiliary agents. Semin Nucl Med. 1990 Apr;20(2):130-49. [Article]
- de Graaf W, Hausler S, Heger M, van Ginhoven TM, van Cappellen G, Bennink RJ, Kullak-Ublick GA, Hesselmann R, van Gulik TM, Stieger B: Transporters involved in the hepatic uptake of (99m)Tc-mebrofenin and indocyanine green. J Hepatol. 2011 Apr;54(4):738-45. doi: 10.1016/j.jhep.2010.07.047. Epub 2010 Oct 1. [Article]
- External Links
- KEGG Drug
- D06037
- PubChem Compound
- 11431716
- PubChem Substance
- 310265052
- ChemSpider
- 28476619
- ChEMBL
- CHEMBL2110555
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Technetium_(99mTc)_mebrofenin
- FDA label
- Download (2.51 MB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 1 Completed Basic Science Non Alcoholic Steatohepatitis (NASH) 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, powder, for solution Intravenous 45 mg - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.0568 mg/mL ALOGPS logP -0.39 ALOGPS logP -0.42 ChemAxon logS -3.8 ALOGPS pKa (Strongest Acidic) 2.81 ChemAxon pKa (Strongest Basic) 2.14 ChemAxon Physiological Charge -1 ChemAxon Hydrogen Acceptor Count 6 ChemAxon Hydrogen Donor Count 3 ChemAxon Polar Surface Area 106.94 Å2 ChemAxon Rotatable Bond Count 7 ChemAxon Refractivity 89.27 m3·mol-1 ChemAxon Polarizability 35.23 Å3 ChemAxon Number of Rings 1 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter No ChemAxon Veber's Rule No ChemAxon MDDR-like Rule No ChemAxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
- Gene Name
- SLCO1B1
- Uniprot ID
- Q9Y6L6
- Uniprot Name
- Solute carrier organic anion transporter family member 1B1
- Molecular Weight
- 76447.99 Da
References
- de Graaf W, Hausler S, Heger M, van Ginhoven TM, van Cappellen G, Bennink RJ, Kullak-Ublick GA, Hesselmann R, van Gulik TM, Stieger B: Transporters involved in the hepatic uptake of (99m)Tc-mebrofenin and indocyanine green. J Hepatol. 2011 Apr;54(4):738-45. doi: 10.1016/j.jhep.2010.07.047. Epub 2010 Oct 1. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotre...
- Gene Name
- SLCO1B3
- Uniprot ID
- Q9NPD5
- Uniprot Name
- Solute carrier organic anion transporter family member 1B3
- Molecular Weight
- 77402.175 Da
References
- de Graaf W, Hausler S, Heger M, van Ginhoven TM, van Cappellen G, Bennink RJ, Kullak-Ublick GA, Hesselmann R, van Gulik TM, Stieger B: Transporters involved in the hepatic uptake of (99m)Tc-mebrofenin and indocyanine green. J Hepatol. 2011 Apr;54(4):738-45. doi: 10.1016/j.jhep.2010.07.047. Epub 2010 Oct 1. [Article]
Drug created at September 29, 2015 22:59 / Updated at October 07, 2021 12:09