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Technetium Tc-99m sestamibi

PubChem Reference Collection SID
PubChem CID
Not available and might not be a discrete structure.
Synonyms
  • Technetium Tc-99m sestamibi
  • Technetium Tc 99m Sestamibi
  • 109581-73-9
  • 971Z4W1S09
  • 99mTc-sestamibi
Description
Technetium Tc-99m sestamibi (commonly sestamibi) is a pharmaceutical agent used in nuclear medicine imaging. The drug is a coordination complex consisting of the radioisotope technetium-99m bound to six methoxyisobutylisonitrile (MIBI) ligands, hence the name sesta (6) MIBI.. Following intravenous injection of the drug, Technetium Tc-99m sestamibi is taken up by the myocardium, parathyroid, and/or breast tissue. The mechanism by which sestamibi localizes to these tissues has not been established. Single photon emission computed tomography (SPECT) is then performed to detect the gamma ray emmitted by the decay of Technetium-99m to Technetium-99. Currently available within a preparation kit for injection, Technetium Tc 99m Sestamibi is indicated for: 1) detecting coronary artery disease by localizing myocardial ischemia (reversible defects) and infarction (non-reversible defects); and 2) evaluating myocardial function and developing information for use in patient management decisions.
Technetium tc-99m sestamibi is a Radioactive Diagnostic Agent. The mechanism of action of technetium tc-99m sestamibi is as a Radiopharmaceutical Activity.
Technetium Tc-99m Sestamibi is sestamibi is a large synthetic molecule of the isonitrile family, which can be labeled with Tc99m. It passes through cells membranes passively, collecting in cells with large numbers of mitochondria. It is often used for imaging of the thyroid and parathyroid.

1 Preferred InChI Key

ZBTQTVSNLRPJHI-UHFFFAOYSA-N

2 Synonyms

  • Technetium Tc-99m sestamibi
  • Technetium Tc 99m Sestamibi
  • 109581-73-9
  • 971Z4W1S09
  • 99mTc-sestamibi
  • Sestamibi
  • Technetium (99m Tc) sestamibi
  • 99mTc sestamibi
  • 99m Tc-sestamibi
  • 99m-Tc sestamibi
  • 99mTc Hexamibi
  • DTXCID501475550
  • DTXSID00911248
  • TC99M RP-30A
  • TC99M-RP-30A
  • Tc 99m Methoxy 2 isobutylisonitrile
  • Tc 99m Sestamibi
  • Tc-99m MIBI
  • Tc99m Sestamibi
  • Technetium Tc 99m 2 Methoxy 2 methylpropylisonitrile
  • Technetium Tc 99m 2-Methoxy-2-methylpropylisonitrile
  • Technetium-99m-Hexamibi
  • Technetium-99m-Sestamibi

3 Names and Identifiers

3.1 Other Identifiers

3.1.1 CAS

109581-73-9

3.1.2 Deprecated CAS

113720-90-4

3.1.3 UNII

3.1.4 DSSTox Substance ID

3.1.5 NCI Thesaurus Code

5 Drug and Medication Information

5.1 Drug Indication

Technetium Tc 99m Sestamibi is indicated for: 1) detecting coronary artery disease by localizing myocardial ischemia (reversible defects) and infarction (non-reversible defects); and 2) evaluating myocardial function and developing information for use in patient management decisions.

5.2 Drug Classes

Breast Feeding; Lactation; Milk, Human; Radiopharmaceuticals; Technetium Compounds; Diagnostic Agents

5.3 FDA National Drug Code Directory

5.4 Drug Labels

Drug and label
Active ingredient and drug

6 Pharmacology and Biochemistry

6.1 FDA Pharmacological Classification

1 of 3
FDA UNII
971Z4W1S09
Active Moiety
Pharmacological Classes
Established Pharmacologic Class [EPC] - Radioactive Diagnostic Agent
Pharmacological Classes
Mechanisms of Action [MoA] - Radiopharmaceutical Activity
FDA Pharmacology Summary
Technetium tc-99m sestamibi is a Radioactive Diagnostic Agent. The mechanism of action of technetium tc-99m sestamibi is as a Radiopharmaceutical Activity.
2 of 3
Non-Proprietary Name
Pharmacological Classes
Radiopharmaceutical Activity [MoA]; Radioactive Diagnostic Agent [EPC]
3 of 3
Non-Proprietary Name
TECHNETIUM TC-99M SESTAMIBI
Pharmacological Classes
Radioactive Diagnostic Agent [EPC]; Radiopharmaceutical Activity [MoA]

6.2 Absorption, Distribution and Excretion

Absorption
At five minutes post injection about 8% of the injected dose remains in circulation. Myocardial uptake which is coronary flow dependent is 1.2% of the injected dose at rest and 1.5% of the injected dose at exercise.
Route of Elimination
The major pathway for clearance of Tc 99m Sestamibi is the hepatobiliary system. Activity from the gall bladder appears in the intestines within one hour of injection. Twenty-seven percent of the injected dose is excreted in the urine, and approximately thirty-three percent of the injected dose is cleared through the feces in 48 hours.
Clearance
The effective half-life of clearance (which includes both the biological half-life and radionuclide decay) for the heart is approximately 3 hours, and for the liver is approximately 30 minutes, after a rest or exercise injection.

6.3 Metabolism / Metabolites

The agent is excreted without any evidence of metabolism.

6.4 Biological Half-Life

Technetium Tc 99m decays by isomeric transition with a physical half-life of 6.02 hours. Blood clearance studies indicate that the fast clearing component clears with a t½ of 4.3 minutes at rest, and clears with a t½ of 1.6 minutes under exercise conditions. The myocardial biological half-life is approximately six hours after a rest or exercise injection. The biological half-life for the liver is approximately 30 minutes after a rest or exercise injection.

7 Toxicity

7.1 Toxicological Information

7.1.1 Effects During Pregnancy and Lactation

◉ Summary of Use during Lactation

Information in this record refers to the use of technetium Tc 99m sestamibi (Tc 99m-methoxyisobutylisonitrile; Tc 99m MIBI) as a diagnostic agent. A US Nuclear Regulatory Commission subcommittee has recommended that nursing be discontinued for 24 hours after administration of all technetium Tc 99m diagnostic products to simplify guidance recommendations, although this time interval may be longer than necessary. Other experts state that breastfeeding need not be interrupted after administration of technetium Tc 99m sestamibi in doses up to 1000 MBq (27 mCi) to a nursing mother. However, to follow the principle of keeping exposure "as low as reasonably achievable", some experts recommend nursing the infant just before administration of the radiopharmaceutical and interrupting breastfeeding for 3 to 4 hours after the dose, then expressing the milk completely once and discarding it. If the mother has expressed and saved milk prior to the examination, she can feed it to the infant during the period of nursing interruption. Mothers need not refrain from close contact with their infants after usual clinical doses.

Mothers concerned about the level of radioactivity in their milk could ask to have it tested at a nuclear medicine facility at their hospital. When the radioactivity is at a safe level, she may resume breastfeeding. A method for measuring milk radioactivity and determining the time when a mother can safely resume breastfeeding has been published.

For nursing mothers who work with Tc 99m substances in their workplace, there is no need to take any precautions other than those appropriate for general radiation protection.

◉ Effects in Breastfed Infants

Relevant published information was not found as of the revision date.

◉ Effects on Lactation and Breastmilk

Relevant published information was not found as of the revision date.

7.1.2 Protein Binding

There is less than 1% protein binding of Technetium Tc 99m Sestamibi in plasma.

8 Interactions and Pathways

8.1 Chemical-Target Interactions

8.2 Drug-Drug Interactions

9 Information Sources

  1. PubChem
  2. ChemIDplus
  3. DrugBank
    LICENSE
    Creative Common's Attribution-NonCommercial 4.0 International License (http://creativecommons.org/licenses/by-nc/4.0/legalcode)
    https://www.drugbank.ca/legal/terms_of_use
    Technetium Tc-99m sestamibi
    https://www.drugbank.ca/drugs/DB09161
  4. EPA DSSTox
  5. FDA Global Substance Registration System (GSRS)
    LICENSE
    Unless otherwise noted, the contents of the FDA website (www.fda.gov), both text and graphics, are not copyrighted. They are in the public domain and may be republished, reprinted and otherwise used freely by anyone without the need to obtain permission from FDA. Credit to the U.S. Food and Drug Administration as the source is appreciated but not required.
    https://www.fda.gov/about-fda/about-website/website-policies#linking
  6. DailyMed
  7. FDA Pharm Classes
    LICENSE
    Unless otherwise noted, the contents of the FDA website (www.fda.gov), both text and graphics, are not copyrighted. They are in the public domain and may be republished, reprinted and otherwise used freely by anyone without the need to obtain permission from FDA. Credit to the U.S. Food and Drug Administration as the source is appreciated but not required.
    https://www.fda.gov/about-fda/about-website/website-policies#linking
  8. NCI Thesaurus (NCIt)
    LICENSE
    Unless otherwise indicated, all text within NCI products is free of copyright and may be reused without our permission. Credit the National Cancer Institute as the source.
    https://www.cancer.gov/policies/copyright-reuse
  9. Drugs and Lactation Database (LactMed)
  10. National Drug Code (NDC) Directory
    LICENSE
    Unless otherwise noted, the contents of the FDA website (www.fda.gov), both text and graphics, are not copyrighted. They are in the public domain and may be republished, reprinted and otherwise used freely by anyone without the need to obtain permission from FDA. Credit to the U.S. Food and Drug Administration as the source is appreciated but not required.
    https://www.fda.gov/about-fda/about-website/website-policies#linking
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