Technetium Tc-99m mebrofenin

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
Thumb
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.

Pharmacology
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Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

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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Toxicity

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.
DrugInteraction
AbacavirAbacavir may decrease the excretion rate of Technetium Tc-99m mebrofenin which could result in a higher serum level.
AceclofenacAceclofenac may decrease the excretion rate of Technetium Tc-99m mebrofenin which could result in a higher serum level.
AcemetacinAcemetacin may decrease the excretion rate of Technetium Tc-99m mebrofenin which could result in a higher serum level.
AcetaminophenAcetaminophen may decrease the excretion rate of Technetium Tc-99m mebrofenin which could result in a higher serum level.
AcetazolamideAcetazolamide may increase the excretion rate of Technetium Tc-99m mebrofenin which could result in a lower serum level and potentially a reduction in efficacy.
AcetylcysteineThe excretion of Technetium Tc-99m mebrofenin can be decreased when combined with Acetylcysteine.
Acetylsalicylic acidAcetylsalicylic acid may decrease the excretion rate of Technetium Tc-99m mebrofenin which could result in a higher serum level.
AclidiniumAclidinium may decrease the excretion rate of Technetium Tc-99m mebrofenin which could result in a higher serum level.
AcrivastineTechnetium Tc-99m mebrofenin may decrease the excretion rate of Acrivastine which could result in a higher serum level.
AcyclovirAcyclovir may decrease the excretion rate of Technetium Tc-99m mebrofenin which could result in a higher serum level.
Interactions
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Food Interactions
  • 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

Products
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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
MebrofeninInjection, powder, lyophilized, for solution10 mg/1IntravenousAnazao Health Corporation2012-06-19Not applicableUS flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Kit for the Preparation of Technetium Tc 99m MebrofeninInjection, powder, lyophilized, for solution45 mg/10mLIntravenousSun Pharmaceutical Industries, Inc.2008-01-29Not applicableUS flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
MebrofeninTechnetium Tc-99m mebrofenin (10 mg/1)Injection, powder, lyophilized, for solutionIntravenousAnazao Health Corporation2012-06-19Not applicableUS flag

Categories

ATC Codes
V09DA04 — Technetium (99mtc) mebrofenin
Drug Categories
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
  1. Krishnamurthy GT, Turner FE: Pharmacokinetics and clinical application of technetium 99m-labeled hepatobiliary agents. Semin Nucl Med. 1990 Apr;20(2):130-49. [Article]
  2. 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]
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
PhaseStatusPurposeConditionsCount
1CompletedBasic ScienceNon-Alcoholic Steatohepatitis1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Injection, powder, lyophilized, for solutionIntravenous45 mg/10mL
Injection, powder, for solutionIntravenous45 mg
Injection, powder, lyophilized, for solutionIntravenous10 mg/1
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0568 mg/mLALOGPS
logP-0.39ALOGPS
logP-0.42ChemAxon
logS-3.8ALOGPS
pKa (Strongest Acidic)2.81ChemAxon
pKa (Strongest Basic)2.14ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area106.94 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity89.27 m3·mol-1ChemAxon
Polarizability35.23 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Yes
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
  1. 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
Yes
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
  1. 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 on September 29, 2015 22:59 / Updated on August 21, 2020 19:35