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
Structure for Technetium Tc-99m succimer (DB09436)
- 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
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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- Contraindications & Blackbox Warnings
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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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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
- Acids, Acyclic
- Compounds used in a research, industrial, or household setting
- Diagnostic Radiopharmaceuticals
- Diagnostic Uses of Chemicals
- Dicarboxylic Acids
- Indicators and Reagents
- Laboratory Chemicals
- Organometallic Compounds
- Organotechnetium Compounds
- Radioactive Diagnostic Agent
- Radiopharmaceutical Activity
- Radiopharmaceuticals
- Renal System
- Succinates
- Sulfhydryl Compounds
- Sulfur Compounds
- Technetium (99Mtc) Compounds
- 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
- 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]
- Muller-Suur R, Gutsche HU: Tubular reabsorption of technetium-99m-DMSA. J Nucl Med. 1995 Sep;36(9):1654-8. [Article]
- 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]
- 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]
- FDA Approved Drug Products: NEPHROSCAN (kit for the preparation of technetium Tc 99m succimer injection), for intravenous use [Link]
- PR Newswire: Theragnostics Announces US FDA Approval for its Radiodiagnostic Imaging Drug NephroScan™ (Kit for the Preparation of Technetium Tc 99m Succimer Injection) [Link]
- External Links
- Not Available
Clinical Trials
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
Property Value Source Water Solubility 2.43 mg/mL ALOGPS logP 0.56 ALOGPS logP 0.26 Chemaxon logS -1.9 ALOGPS pKa (Strongest Acidic) 3.37 Chemaxon Physiological Charge -2 Chemaxon Hydrogen Acceptor Count 4 Chemaxon Hydrogen Donor Count 4 Chemaxon Polar Surface Area 74.6 Å2 Chemaxon Rotatable Bond Count 3 Chemaxon Refractivity 38.47 m3·mol-1 Chemaxon Polarizability 15.61 Å3 Chemaxon Number of Rings 0 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
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Transporters
- 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
- 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]
- 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
- 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