Technetium Tc-99m sestamibi

Identification

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Name
Technetium Tc-99m sestamibi
Accession Number
DB09161
Type
Small Molecule
Groups
Approved, Investigational
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.

Structure
Thumb
Synonyms
  • 99m Tc-sestamibi
  • 99m-Tc sestamibi
  • 99mTc sestamibi
  • 99mTc-sestamibi
  • Sestamibi
  • Technetium (99m Tc) sestamibi
  • Technetium (99mTc) sestamibi
  • Technetium Tc 99m sestamibi
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Technetium Tc 99m SestamibiInjection1 mg/10mLIntravenousJubilant HollisterStier General Partnership2009-07-012018-01-23Us
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Kit for the Preparation of Technetium Tc99m SestamibiInjection1 mg/10mLIntravenousPharmalucence, Inc.2009-07-10Not applicableUs
Kit for the Preparation of Technetium Tc99m SestamibiInjection, powder, lyophilized, for solution1 mg/5mLParenteralCardinal Health 414, Llc2010-06-01Not applicableUs
Technetium Tc 99m SestamibiInjection, powder, for solution1 mg/1mLIntravenousJubilant Draximage (Usa) Inc.2009-07-01Not applicableUs
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

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Categories
UNII
971Z4W1S09
CAS number
109581-73-9
Weight
Average: 775.96
Monoisotopic: 775.5
Chemical Formula
C36H66N6O6Tc
InChI Key
ZBTQTVSNLRPJHI-UHFFFAOYSA-N
InChI
InChI=1S/6C6H11NO.Tc/c6*1-6(2,8-4)5-7-3;/h6*5H2,1-2,4H3;/q;;;;;;+1
IUPAC Name
technetium(1+) ion hexakis(1-isocyano-2-methoxy-2-methylpropane)
SMILES
[Tc+].COC(C)(C)C[N+]#[C-].COC(C)(C)C[N+]#[C-].COC(C)(C)C[N+]#[C-].COC(C)(C)C[N+]#[C-].COC(C)(C)C[N+]#[C-].COC(C)(C)C[N+]#[C-]

Pharmacology

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.

Associated Conditions
Pharmacodynamics
Not Available
Mechanism of action
Not Available
Additional Data Available
Adverse Effects

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Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available
Blackbox Warnings

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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.

Volume of distribution
Not Available
Protein binding

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

Metabolism

The agent is excreted without any evidence of metabolism.

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.

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.

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.

Toxicity

The following adverse reactions have been reported in > 0.5% of patients: signs and symptoms consistent with seizure occurring shortly after administration of the agent; transient arthritis; angioedema, arrhythmia, dizziness, syncope, abdominal pain, vomiting, and severe hypersensitivity characterized by dyspnea, hypotension, bradycardia, asthenia, and vomiting within two hours after a second injection of Technetium Tc 99m Sestamibi. A few cases of flushing, edema, injection site inflammation, dry mouth, fever, pruritis, rash, urticaria and fatigue have also been attributed to administration of the agent.

Affected organisms
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
AbemaciclibThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Abemaciclib.
AcebutololThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Acebutolol.
AcetaminophenThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Acetaminophen.
Acetylsalicylic acidThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Acetylsalicylic acid.
AfatinibThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Afatinib.
AlbendazoleThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Albendazole.
AldosteroneThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Aldosterone.
AlectinibThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Alectinib.
AlfentanilThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Alfentanil.
AlitretinoinThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Alitretinoin.
Additional Data Available
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  • Severity
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Food Interactions
Not Available

References

General References
  1. Hendrikse NH, Franssen EJ, van der Graaf WT, Meijer C, Piers DA, Vaalburg W, de Vries EG: 99mTc-sestamibi is a substrate for P-glycoprotein and the multidrug resistance-associated protein. Br J Cancer. 1998;77(3):353-8. [PubMed:9472628]
  2. Ma Q, Chen B, Gao S, Ji T, Wen Q, Song Y, Zhu L, Xu Z, Liu L: 99mTc-3P4-RGD2 scintimammography in the assessment of breast lesions: comparative study with 99mTc-MIBI. PLoS One. 2014 Sep 24;9(9):e108349. doi: 10.1371/journal.pone.0108349. eCollection 2014. [PubMed:25250628]
  3. Tiling R, Tatsch K, Sommer H, Meyer G, Pechmann M, Gebauer K, Munzing W, Linke R, Khalkhali I, Hahn K: Technetium-99m-sestamibi scintimammography for the detection of breast carcinoma: comparison between planar and SPECT imaging. J Nucl Med. 1998 May;39(5):849-56. [PubMed:9591588]
External Links
KEGG Drug
D01060
PubChem Compound
22617237
PubChem Substance
310265074
ChemSpider
58829659
ChEBI
9423
ChEMBL
CHEMBL2074398
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Technetium_(99mTc)_sestamibi
ATC Codes
V09GA01 — Technetium (99mtc) sestamibi
FDA label
Download (4.09 MB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0RecruitingDiagnosticBreast Cancer / Estrogen Receptor Negative / HER2/Neu Negative / Malignant Neoplasm of Breast / Progesterone Receptor Negative / Triple-Negative Breast Carcinoma1
1, 2CompletedDiagnosticMucocutaneous Lymph Node Syndrome1
2CompletedDiagnosticMalignancies1
3CompletedDiagnosticCoronary Artery Disease2
3CompletedDiagnosticMucocutaneous Lymph Node Syndrome1
4CompletedDiagnosticCoronary Artery Disease / Type 1 Insulin-Dependent Diabetes Mellitus1
4CompletedDiagnosticCoronary Artery Restenosis / Type 2 Diabetes Mellitus1
4CompletedDiagnosticDiabetes Mellitus (DM)1
4CompletedDiagnosticMyocardial Infarction1
Not AvailableCompletedDiagnosticBreast Cancer2
Not AvailableCompletedDiagnosticMyocardial Perfusion1
Not AvailableRecruitingDiagnosticBreast Cancer1
Not AvailableTerminatedDiagnosticIschaemic Heart Diseases / Myocardial Infarction1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Injection, powder, lyophilized, for solutionParenteral1 mg/5mL
InjectionIntravenous1 mg/10mL
Injection, powder, for solutionIntravenous1 mg/1mL
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00465 mg/mLALOGPS
logP5.44ALOGPS
logP-1.3ChemAxon
logS-5.2ALOGPS
pKa (Strongest Acidic)16.14ChemAxon
pKa (Strongest Basic)-4.2ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area13.59 Å2ChemAxon
Rotatable Bond Count12ChemAxon
Refractivity41.61 m3·mol-1ChemAxon
Polarizability12.7 Å3ChemAxon
Number of Rings0ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Classification
Not classified

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Hendrikse NH, Franssen EJ, van der Graaf WT, Meijer C, Piers DA, Vaalburg W, de Vries EG: 99mTc-sestamibi is a substrate for P-glycoprotein and the multidrug resistance-associated protein. Br J Cancer. 1998;77(3):353-8. [PubMed:9472628]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Transporter activity
Specific Function
Mediates export of organic anions and drugs from the cytoplasm. Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotre...
Gene Name
ABCC1
Uniprot ID
P33527
Uniprot Name
Multidrug resistance-associated protein 1
Molecular Weight
171589.5 Da
References
  1. Hendrikse NH, Franssen EJ, van der Graaf WT, Meijer C, Piers DA, Vaalburg W, de Vries EG: 99mTc-sestamibi is a substrate for P-glycoprotein and the multidrug resistance-associated protein. Br J Cancer. 1998;77(3):353-8. [PubMed:9472628]

Drug created on October 02, 2015 14:20 / Updated on November 02, 2019 02:34