Identification

Summary

Rubidium chloride Rb-82 is a radiopharmaceutical diagnostic agent used for Positron Emission Tomography (PET) imaging of the myocardium to evaluate regional myocardial perfusion in adult patients with suspected or existing coronary artery disease.

Brand Names
Cardiogen-82, Ruby-fill
Generic Name
Rubidium Rb-82
Commonly known or available as Rubidium chloride Rb-82
DrugBank Accession Number
DB09479
Background

Rubidium chloride Rb-82 injection is a sterile nonpyrogenic solutions of rubidium Rb 82 chloride. It is indicated for Positron Emission Tomography (PET) imaging of the myocardium under rest or pharmacologic stress conditions to evaluate regional myocardial perfusion in adult patients with suspected or existing coronary artery disease.

Type
Small Molecule
Groups
Approved, Investigational
Structure
Thumb
Weight
Average: 81.9177
Monoisotopic: 81.917659111
Chemical Formula
Rb
Synonyms
  • Rubidium (82Rb) cation
  • Rubidium cation Rb-82
  • Rubidium Rb-82 cation

Pharmacology

Indication

Rubidium Rb 82 chloride injection is indicated for Positron Emission Tomography (PET) imaging of the myocardium under rest or pharmacologic stress conditions to evaluate regional myocardial perfusion in adult patients with suspected or existing coronary artery disease.

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

In human studies, myocardial activity was noted within the first minute after peripheral intravenous injection of Rb-82. When areas of infarction or ischemia are present in the myocardium, they are visualized within 2-7 minutes after injection as photon-deficient, or “cold”, areas on the myocardial scan. In patients with reduced cardiac function, transit of the injected dose from the peripheral infusion site to the myocardium may be delayed Blood flow brings Rb-82 to all areas of the body during the first pass of circulation. Accordingly, visible uptake is also observed in other highly vascularized organs, such as the kidneys, liver, spleen and lungs.

Mechanism of action

Rb-82 is analogous to potassium ion (K+) in its biochemical behavior and is rapidly extracted by the myocardium proportional to the blood flow. Rb+ participates in the sodium-potassium (Na+/K+) ion exchange pumps that are present in cell membranes. The intracellular uptake of Rb-82 requires maintenance of ionic gradient across cell membranes. Rb-82 radioactivity is increased in viable myocardium reflecting intracellular retention, while the tracer is cleared rapidly from necrotic or infarcted tissue.

Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism

Rubidium is rapidly extracted from the blood and is taken up by the myocardium in relation to myocardial perfusion, which requires energy for myocardial uptake through Na+/K+-ATPase

Route of elimination

It is rapidly extracted by the myocardium proportional to blood flow.

Half-life

1.27 minutes

Clearance

Not Available

Adverse Effects
Adverseeffects
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Toxicity

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.
Not Available
Food Interactions
No interactions found.

Products

Products2
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Product Ingredients
IngredientUNIICASInChI Key
Rubidium chloride Rb-82F0Z746KRKQ132486-03-4FGDZQCVHDSGLHJ-RYDPDVNUSA-M
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
CardioGen-82Injection, solution150 mCi/1IntravenousBracco Diagnostics Inc1989-12-30Not applicableUS flag
Ruby-fillInjection, solution100 mCi/1IntravenousJubilant Draximage Inc.2016-09-30Not applicableUS flag
Ruby-fillInjection, solution100 mCi/1IntravenousJubilant DraxImage Inc., dba Jubilant Radiopharma2016-09-30Not applicableUS flag

Categories

Drug Categories
Classification
Not classified
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
550Z839889
CAS number
Not Available
InChI Key
NCCSSGKUIKYAJD-OIOBTWANSA-N
InChI
InChI=1S/Rb/q+1/i1-3
IUPAC Name
(82Rb)rubidium(1+) ion
SMILES
[82Rb+]

References

General References
  1. Hasbak P, Enevoldsen LH, Fosbol MO, Skovgaard D, Knigge UP, Kjaer A: Rubidium-82 uptake in metastases from neuroendocrine tumors: No flow response to adenosine. J Nucl Cardiol. 2016 Aug;23(4):840-2. doi: 10.1007/s12350-015-0251-z. Epub 2015 Sep 10. [Article]
  2. LOVE WD, BURCH GE: A comparison of potassium 42, rubidium 86, and cesium 134 as tracers of potassium in the study of cation metabolism of human erythrocytes in vitro. J Lab Clin Med. 1953 Mar;41(3):351-62. [Article]
  3. CardioGen-82: Rubidium Rb 82 Generator [Link]
  4. Daily med [Link]
PubChem Compound
71357
PubChem Substance
347827860
ChemSpider
8351588
RxNav
1546434
ChEMBL
CHEMBL1200727

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3CompletedDiagnosticCoronary Artery Disease (CAD)1
Not AvailableCompletedNot AvailableNuclear radiation emergency2

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Injection, solutionIntravenous150 mCi/1
Injection, solutionIntravenous100 mCi/1
Prices
Not Available
Patents
Not Available

Properties

State
Not Available
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
logP0ChemAxon
pKa (Strongest Acidic)3.09ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count0ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area0 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity0 m3·mol-1ChemAxon
Polarizability1.78 Å3ChemAxon
Number of Rings0ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
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
Steroid hormone binding
Specific Function
This is the catalytic component of the active enzyme, which catalyzes the hydrolysis of ATP coupled with the exchange of sodium and potassium ions across the plasma membrane. This action creates th...
Gene Name
ATP1A1
Uniprot ID
P05023
Uniprot Name
Sodium/potassium-transporting ATPase subunit alpha-1
Molecular Weight
112895.01 Da
References
  1. Beck FX, Dorge A, Blumner E, Giebisch G, Thurau K: Cell rubidium uptake: a method for studying functional heterogeneity in the nephron. Kidney Int. 1988 Mar;33(3):642-51. doi: 10.1038/ki.1988.47. [Article]
  2. Jochumsen MR, Sorensen J, Pedersen BG, Nyengaard JR, Krag SRP, Frokiaer J, Borre M, Bouchelouche K, Tolbod LP: Tumour blood flow for prediction of human prostate cancer aggressiveness: a study with Rubidium-82 PET, MRI and Na(+)/K(+)-ATPase-density. Eur J Nucl Med Mol Imaging. 2021 Feb;48(2):532-542. doi: 10.1007/s00259-020-04998-2. Epub 2020 Aug 18. [Article]
  3. CardioGen-82: Rubidium Rb 82 Generator [Link]
  4. Daily med [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Transporter activity
Specific Function
May be involved in forming the receptor site for cardiac glycoside binding or may modulate the transport function of the sodium ATPase.
Gene Name
FXYD2
Uniprot ID
P54710
Uniprot Name
Sodium/potassium-transporting ATPase subunit gamma
Molecular Weight
7283.265 Da
References
  1. Beck FX, Dorge A, Blumner E, Giebisch G, Thurau K: Cell rubidium uptake: a method for studying functional heterogeneity in the nephron. Kidney Int. 1988 Mar;33(3):642-51. doi: 10.1038/ki.1988.47. [Article]
  2. CardioGen-82: Rubidium Rb 82 Generator [Link]
  3. Daily med [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Sodium:potassium-exchanging atpase activity
Specific Function
This is the non-catalytic component of the active enzyme, which catalyzes the hydrolysis of ATP coupled with the exchange of Na(+) and K(+) ions across the plasma membrane. The beta subunit regulat...
Gene Name
ATP1B1
Uniprot ID
P05026
Uniprot Name
Sodium/potassium-transporting ATPase subunit beta-1
Molecular Weight
35061.07 Da
References
  1. Beck FX, Dorge A, Blumner E, Giebisch G, Thurau K: Cell rubidium uptake: a method for studying functional heterogeneity in the nephron. Kidney Int. 1988 Mar;33(3):642-51. doi: 10.1038/ki.1988.47. [Article]
  2. CardioGen-82: Rubidium Rb 82 Generator [Link]
  3. Daily med [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Sodium:potassium-exchanging atpase activity
Specific Function
This is the non-catalytic component of the active enzyme, which catalyzes the hydrolysis of ATP coupled with the exchange of Na(+) and K(+) ions across the plasma membrane. The exact function of th...
Gene Name
ATP1B2
Uniprot ID
P14415
Uniprot Name
Sodium/potassium-transporting ATPase subunit beta-2
Molecular Weight
33366.925 Da
References
  1. Beck FX, Dorge A, Blumner E, Giebisch G, Thurau K: Cell rubidium uptake: a method for studying functional heterogeneity in the nephron. Kidney Int. 1988 Mar;33(3):642-51. doi: 10.1038/ki.1988.47. [Article]
  2. CardioGen-82: Rubidium Rb 82 Generator [Link]
  3. Daily med [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Sodium:potassium-exchanging atpase activity
Specific Function
This is the non-catalytic component of the active enzyme, which catalyzes the hydrolysis of ATP coupled with the exchange of Na(+) and K(+) ions across the plasma membrane. The exact function of th...
Gene Name
ATP1B3
Uniprot ID
P54709
Uniprot Name
Sodium/potassium-transporting ATPase subunit beta-3
Molecular Weight
31512.34 Da
References
  1. Beck FX, Dorge A, Blumner E, Giebisch G, Thurau K: Cell rubidium uptake: a method for studying functional heterogeneity in the nephron. Kidney Int. 1988 Mar;33(3):642-51. doi: 10.1038/ki.1988.47. [Article]
  2. CardioGen-82: Rubidium Rb 82 Generator [Link]
  3. Daily med [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Sodium:potassium-exchanging atpase activity
Specific Function
This is the catalytic component of the active enzyme, which catalyzes the hydrolysis of ATP coupled with the exchange of sodium and potassium ions across the plasma membrane. This action creates th...
Gene Name
ATP1A4
Uniprot ID
Q13733
Uniprot Name
Sodium/potassium-transporting ATPase subunit alpha-4
Molecular Weight
114165.44 Da
References
  1. Beck FX, Dorge A, Blumner E, Giebisch G, Thurau K: Cell rubidium uptake: a method for studying functional heterogeneity in the nephron. Kidney Int. 1988 Mar;33(3):642-51. doi: 10.1038/ki.1988.47. [Article]
  2. CardioGen-82: Rubidium Rb 82 Generator [Link]
  3. Daily med [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Steroid hormone binding
Specific Function
This is the catalytic component of the active enzyme, which catalyzes the hydrolysis of ATP coupled with the exchange of sodium and potassium ions across the plasma membrane. This action creates th...
Gene Name
ATP1A2
Uniprot ID
P50993
Uniprot Name
Sodium/potassium-transporting ATPase subunit alpha-2
Molecular Weight
112264.385 Da
References
  1. Beck FX, Dorge A, Blumner E, Giebisch G, Thurau K: Cell rubidium uptake: a method for studying functional heterogeneity in the nephron. Kidney Int. 1988 Mar;33(3):642-51. doi: 10.1038/ki.1988.47. [Article]
  2. CardioGen-82: Rubidium Rb 82 Generator [Link]
  3. Daily med [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Steroid hormone binding
Specific Function
This is the catalytic component of the active enzyme, which catalyzes the hydrolysis of ATP coupled with the exchange of sodium and potassium ions across the plasma membrane. This action creates th...
Gene Name
ATP1A3
Uniprot ID
P13637
Uniprot Name
Sodium/potassium-transporting ATPase subunit alpha-3
Molecular Weight
111747.51 Da
References
  1. Beck FX, Dorge A, Blumner E, Giebisch G, Thurau K: Cell rubidium uptake: a method for studying functional heterogeneity in the nephron. Kidney Int. 1988 Mar;33(3):642-51. doi: 10.1038/ki.1988.47. [Article]
  2. CardioGen-82: Rubidium Rb 82 Generator [Link]
  3. Daily med [Link]

Drug created at November 30, 2015 19:10 / Updated at October 07, 2021 12:09