Identification
- Summary
Technetium Tc-99m sestamibi is a radiopharmaceutical diagnostic agent used in nuclear medicine imaging tests to detect coronary artery disease and evaluate myocardial function.
- Brand Names
- Cardiolite
- Generic Name
- Technetium Tc-99m sestamibi
- DrugBank Accession Number
- DB09161
- Background
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.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Technetium Tc-99m sestamibi (DB09161)
- Weight
- Average: 775.96
Monoisotopic: 775.5 - Chemical Formula
- C36H66N6O6Tc
- Synonyms
- 99m Tc-sestamibi
- 99m-Tc sestamibi
- 99mTc sestamibi
- 99mTc-sestamibi
- Sestamibi
- Technetium (99m Tc) sestamibi
- Technetium (99mTc) sestamibi
- Technetium Tc 99m sestamibi
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.
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- Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- Pharmacodynamics
Not Available
- Mechanism of action
- Not Available
- 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.
- Adverse Effects
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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.
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbemaciclib The serum concentration of Abemaciclib can be increased when it is combined with Technetium Tc-99m sestamibi. Abrocitinib The serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Abrocitinib. Adagrasib The serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Adagrasib. Afatinib The serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Afatinib. Ambrisentan The serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Ambrisentan. Amiodarone The serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Amiodarone. Apalutamide The serum concentration of Technetium Tc-99m sestamibi can be decreased when it is combined with Apalutamide. Apixaban The serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Apixaban. Arsenic trioxide The serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Arsenic trioxide. Asciminib The serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Asciminib. 
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- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Technetium Tc 99m Sestamibi Injection 1 mg/10mL Intravenous Jubilant HollisterStier General Partnership 2009-07-01 2018-01-23 US 
- Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Kit for the Preparation of Technetium Tc99m Sestamibi Injection, powder, lyophilized, for solution 1 mg/5mL Parenteral Cardinal Health 414, Llc 2010-06-01 Not applicable US Kit for the Preparation of Technetium Tc99m Sestamibi Injection 1 mg/10mL Intravenous Sun Pharmaceutical Industries, Inc. 2009-07-10 Not applicable US Technetium Tc 99m Sestamibi Injection 1 mg/1mL Intravenous Mallinckrodt Inc. 2011-10-31 2017-07-01 US Technetium Tc 99m Sestamibi Injection, powder, for solution 1 mg/1mL Intravenous Jubilant Draximage (Usa) Inc. 2009-07-01 Not applicable US
Categories
- ATC Codes
- V09GA01 — Technetium (99mtc) sestamibi
- Drug Categories
- Compounds used in a research, industrial, or household setting
- Diagnostic Radiopharmaceuticals
- Diagnostic Uses of Chemicals
- Indicators and Reagents
- Laboratory Chemicals
- Nitriles
- Organometallic Compounds
- Organotechnetium Compounds
- P-glycoprotein substrates
- Radioactive Diagnostic Agent
- Radiopharmaceutical Activity
- Radiopharmaceuticals
- Technetium (99Mtc) Compounds
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- 971Z4W1S09
- CAS number
- 109581-73-9
- 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-]
References
- General References
- 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. [Article]
- 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. [Article]
- 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. [Article]
- External Links
- KEGG Drug
- D01060
- PubChem Compound
- 22617237
- PubChem Substance
- 310265074
- ChemSpider
- 58829659
- 1482913
- ChEBI
- 9423
- ChEMBL
- CHEMBL2074398
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Technetium_(99mTc)_sestamibi
- FDA label
- Download (4.09 MB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Diagnostic Coronary Artery Disease (CAD) / Type 1 Diabetes Mellitus 1 4 Completed Diagnostic Coronary Artery Restenosis / Type 2 Diabetes Mellitus 1 4 Completed Diagnostic Diabetes 1 4 Completed Diagnostic Myocardial Infarction 1 4 Terminated Diagnostic Thyroid Cancer 1 3 Completed Diagnostic Coronary Artery Disease (CAD) 2 3 Completed Diagnostic Mucocutaneous Lymph Node Syndrome 1 2 Completed Diagnostic Cancer 1 1, 2 Completed Diagnostic Mucocutaneous Lymph Node Syndrome 1 0 Active Not Recruiting Diagnostic Estrogen Receptor Negative / HER2/Neu Negative / Progesterone Receptor Negative / Triple Negative Breast Carcinoma 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, powder, lyophilized, for solution Intravenous 0.12 mg Injection, powder, lyophilized, for solution Parenteral 1 mg/5mL Kit 500 mcg Kit Kit 1 mg Injection Intravenous 1 mg/10mL Injection Intravenous 1 mg/1mL Injection, powder, for solution Intravenous 1 mg/1mL - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.00465 mg/mL ALOGPS logP 5.44 ALOGPS logP -1.3 Chemaxon logS -5.2 ALOGPS pKa (Strongest Acidic) 16.14 Chemaxon pKa (Strongest Basic) -4.2 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 1 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 13.59 Å2 Chemaxon Rotatable Bond Count 12 Chemaxon Refractivity 41.61 m3·mol-1 Chemaxon Polarizability 12.7 Å3 Chemaxon Number of Rings 0 Chemaxon Bioavailability 0 Chemaxon Rule of Five No 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
- Not Available
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
- 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. [Article]
- 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
- 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. [Article]
Drug created at October 02, 2015 20:20 / Updated at December 04, 2021 06:47