NAV

Technetium Tc-99m succimer

Identification

Summary

Technetium Tc-99m succimer is a radioactive diagnostic agent used as an aid in the scintigraphic evaluation of renal parenchymal disorders.

Generic Name
Technetium Tc-99m succimer
DrugBank Accession Number
DB09436
Background

Technetium Tc-99m (99mTc) succimer, also known as technetium Tc-99m dimercaptosuccinic acid (DMSA),1 is a radioactive diagnostic agent used to evaluate functional renal tissue and tubular function in patients with renal parenchymal disorders. It works by binding to the cortical region of the kidneys. Technetium Tc-99m succimer is used with gamma scintigraphy or single-photon emission computed tomography (SPECT).5 The use of technetium Tc-99m succimer for the detection of kidney cortical defects was first approved by the FDA on February 23, 2022, under the market name NephroScan.6

Type
Small Molecule
Groups
Approved
Structure
Similar Structures
Weight
Average: 281.11
Monoisotopic: 280.877005575
Chemical Formula
C4H6O4S2Tc
Synonyms
  • (99m)Tc-DMSA
  • Technetium (99mTc) succimer
  • Technetium Tc 99m dimercaptosuccinic acid
  • Technetium tc 99m succimer
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Pharmacology

Indication

Technetium Tc-99m succimer is a radioactive diagnostic agent indicated for use as an aid in the scintigraphic evaluation of renal parenchymal disorders in adults and pediatric patients including term neonates.5

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Diagnostic agentRenal parenchymal disorders••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Technetium Tc-99m succimer stays bound to viable cortical tissue for more than 24 hours following administration. The relationship between technetium Tc-99m succimer plasma concentrations and successful imaging is unknown.5 In one study consisting of children with acute pyelonephritis, the sensitivity of technetium Tc-99m succimer in predicting vesicoureteral reflux, a manifestation that is often seen in urinary tract infections, was 84.1%.3

About six hours after administration, approximately 20% of the dose of technetium Tc-99m succimer accumulates in each kidney.5 Early physiological studies suggest that more than 50% of the drug is retained in the kidneys for up to 24 hours.4

Mechanism of action

Evaluating the quantity of functional renal tissue is essential in renal parenchymal disorders, as it assesses the patient's ability to maintain renal function.4 Technetium Tc-99m succimer is used to image the renal cortices in conjunction with gamma scintigraphy or single-photon emission computed tomography (SPECT).5 Technetium Tc-99m succimer is taken up by tubular cells within the renal cortex regardless of renal flow.4 Technetium Tc-99m succimer binds to normal renal cortical tissue, distinguishing it from nonfunctioning dysplastic tissue, even in the presence of renal insufficiency.5

Absorption

Upon intravenous administration, technetium Tc-99m succimer penetrates the glomerular filter at very low rates.2

Volume of distribution

There is no information available.

Protein binding

Technetium Tc-99m succimer is distributed in the plasma, bound to plasma proteins following intravenous administration. In humans, 53% to 70% of the intravenously administered technetium Tc-99m is protein bound. There is a negligible activity in the red blood cells.5

Metabolism

Technetium Tc-99m decays via isomeric transition.5

Route of elimination

Approximately 16% of the technetium Tc-99m succimer activity is excreted in the urine within two hours.5 Technetium Tc-99m succimer in the tubular system is completely excreted and not reabsorbed from the tubular fluid.2

Half-life

Technetium Tc-99m decays by isomeric transition with a physical half-life of 6.02 hours.5

Clearance

There is no information available.

Adverse Effects
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Toxicity

There is no information on the LD50 of technetium Tc-99m succimer.

In the event of an overdose of technetium Tc-99m succimer, reduce the radiation absorbed dose to the patient where possible by increasing the elimination of the drug from the body using hydration and frequent bladder voiding. A diuretic might also be considered. If possible, an estimate of the radiation-effective dose given to the patient should be made.5

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
No interactions found.

Categories

ATC Codes
V09CA02 — Technetium (99mtc) succimer
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as thia fatty acids. These are fatty acid derivatives obtained by insertion of a sulfur atom at specific positions in the chain.
Kingdom
Organic compounds
Super Class
Lipids and lipid-like molecules
Class
Fatty Acyls
Sub Class
Fatty acids and conjugates
Direct Parent
Thia fatty acids
Alternative Parents
Dicarboxylic acids and derivatives / alpha-Mercaptocarboxylic acids / Alkylthiols / Organic oxides / Hydrocarbon derivatives / Carbonyl compounds
Substituents
2-mercaptocarboxylic acid / Aliphatic acyclic compound / Alkylthiol / Carbonyl group / Carboxylic acid / Carboxylic acid derivative / Dicarboxylic acid or derivatives / Hydrocarbon derivative / Organic oxide / Organic oxygen compound
Molecular Framework
Not Available
External Descriptors
Not Available
Affected organisms
Not Available

Chemical Identifiers

UNII
494JNQ8L28
CAS number
65438-08-6
InChI Key
UEGHKGHBANZTIM-SFJYCVELSA-N
InChI
InChI=1S/C4H6O4S2.Tc/c5-3(6)1(9)2(10)4(7)8;/h1-2,9-10H,(H,5,6)(H,7,8);/t1-,2+;/i;1+2
IUPAC Name
(2R,3S)-2,3-disulfanylbutanedioic acid (99Tc)technetium
SMILES
[99Tc].OC(=O)[C@@H](S)[C@@H](S)C(O)=O

References

General References
  1. Galbraith W, Nguyen A, Harrison DL, Chen X, Talley K: Evaluation of 99mTc-succimer dosing in pediatric patients. J Nucl Med Technol. 2013 Jun;41(2):81-4. doi: 10.2967/jnmt.112.118836. Epub 2013 Apr 22. [Article]
  2. Muller-Suur R, Gutsche HU: Tubular reabsorption of technetium-99m-DMSA. J Nucl Med. 1995 Sep;36(9):1654-8. [Article]
  3. Mohkam M, Maham S, Rahmani A, Naghi I, Otokesh B, Raiiati H, Mohseni N, Shamshiri AR, Sharifian M, Dalirani R, Ghazi R, Ahoopai M: Technetium Tc 99m dimercaptosuccinic acid renal scintigraphy in children with acute pyelonephritis: correlation with other imaging tests. Iran J Kidney Dis. 2010 Oct;4(4):297-301. [Article]
  4. Copely DJ, Smith R, Murakami ME: Renal scintigraphy with technetium Tc 99m succimer: clinical utility in newborns with cystic renal dysplasia. South Med J. 1988 Jan;81(1):99-100. doi: 10.1097/00007611-198801000-00025. [Article]
  5. FDA Approved Drug Products: NEPHROSCAN (kit for the preparation of technetium Tc 99m succimer injection), for intravenous use [Link]
  6. PR Newswire: Theragnostics Announces US FDA Approval for its Radiodiagnostic Imaging Drug NephroScan™ (Kit for the Preparation of Technetium Tc 99m Succimer Injection) [Link]
Not Available

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Not Available
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility2.43 mg/mLALOGPS
logP0.56ALOGPS
logP0.26Chemaxon
logS-1.9ALOGPS
pKa (Strongest Acidic)3.37Chemaxon
Physiological Charge-2Chemaxon
Hydrogen Acceptor Count4Chemaxon
Hydrogen Donor Count4Chemaxon
Polar Surface Area74.6 Å2Chemaxon
Rotatable Bond Count3Chemaxon
Refractivity38.47 m3·mol-1Chemaxon
Polarizability15.61 Å3Chemaxon
Number of Rings0Chemaxon
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
Chromatographic Properties
Collision Cross Sections (CCS)
Not Available

Transporters

Details1. Sodium-dependent phosphate transporter 1
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Not Available
Specific Function
Not Available
Gene Name
SLC20A1
Uniprot ID
Q8WUM9
Uniprot Name
Sodium-dependent phosphate transporter 1
Molecular Weight
73699.01 Da
References
  1. Denoyer D, Perek N, Le Jeune N, Frere D, Dubois F: Evidence that 99mTc-(V)-DMSA uptake is mediated by NaPi cotransporter type III in tumour cell lines. Eur J Nucl Med Mol Imaging. 2004 Jan;31(1):77-84. doi: 10.1007/s00259-003-1334-7. Epub 2003 Oct 14. [Article]
Details2. Sodium-dependent phosphate transporter 2
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Virus receptor activity
Specific Function
Sodium-phosphate symporter which seems to play a fundamental housekeeping role in phosphate transport by absorbing phosphate from interstitial fluid for normal cellular functions such as cellular m...
Gene Name
SLC20A2
Uniprot ID
Q08357
Uniprot Name
Sodium-dependent phosphate transporter 2
Molecular Weight
70391.755 Da
References
  1. Denoyer D, Perek N, Le Jeune N, Frere D, Dubois F: Evidence that 99mTc-(V)-DMSA uptake is mediated by NaPi cotransporter type III in tumour cell lines. Eur J Nucl Med Mol Imaging. 2004 Jan;31(1):77-84. doi: 10.1007/s00259-003-1334-7. Epub 2003 Oct 14. [Article]

Drug created at November 30, 2015 19:10 / Updated at April 01, 2022 19:23