NAV

Xenon Xe-129

Identification

Summary

Xenon Xe-129 is as a hyperpolarized contrast agent, it is indicated for use with magnetic resonance imaging (MRI) for evaluation of lung ventilation.

Generic Name
Xenon Xe-129
DrugBank Accession Number
DB17386
Background

Hyperpolarized Xenon-129 (Xe-129) is a contrast agent used in the lung's clinical magnetic resonance imaging (MRI). Lung MRIs are challenging due to the low proton density of this tissue, as well as the presence of artifacts due to respiration and cardiovascular pulsation movement and air–tissue interfaces.1,2 The use of hyperpolarized noble gases makes lung MRIs feasible. They undergo a process that increases nuclear polarization up to five orders of magnitude, leading to a higher MRI signal. Helium-3 (He-3) is the one most commonly used due to its strong signal and favorable safety profile, but its use in other applications has affected its availability.1 Xe-129 has a lower cost, and adverse effects are normally resolved shortly after administration.2 In December 2022, the FDA approved the use of hyperpolarized Xe-129 for use with MRI for the evaluation of lung ventilation.7 Hyperpolarized Xe-129 is chemically identical to non-polarized Xe-129, and xenon is a clear, colorless, monoatomic, inert, stable, noble gas.6

Type
Small Molecule
Groups
Approved
Structure
Similar Structures
Weight
Average: 128.9048
Monoisotopic: 128.90478086
Chemical Formula
Xe
Synonyms
  • Xenon xe-129m
  • Xenon-129m
  • Xenon, isotope of mass 129
  • Xenon, isotope of mass 129m(8.88 d)
  • Xenon, xe-129m
External IDs
  • XE-129M
  • XENON XE-129
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Pharmacology

Indication

Hyperpolarized Xenon-129 is a contrast agent indicated for use with magnetic resonance imaging (MRI) for the evaluation of lung ventilation in adults and pediatric patients aged 12 years and older.6

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Diagnostic agentVentilation of the lung••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

The volume of gas inhaled, the degree of xenon-129 isotopic enrichment, and the degree of hyperpolarization affect the MRI signal obtained with hyperpolarized xenon-129.6 When inhaled for long periods of time, xenon acts as an anesthetic at concentrations higher than 50%. Xenon has also been used in computerized tomography (CT) scans to measure cerebral blood flow.2

Mechanism of action

The nuclear polarisation of xenon-129 (Xe-129) is increased up to five orders of magnitude in a process called hyperpolarization. This process compensates for the low density of gas compared to that of solid tissue.5

After being inhaled, hyperpolarized xenon-129 (Xe-129) is distributed throughout the ventilated lung. Lung ventilation can be visualized using a multi-nuclear capable magnetic resonance imaging (MRI) scanner with a Xe-129 MRI coil.6

Absorption

The pharmacokinetic parameters of hyperpolarized xenon-129 are similar to those of non-polarized xenon. Xenon has low solubility; however, it is higher in fatty tissues compared to aqueous tissues and body compartments such as plasma.4,6 A study that modelled the pharmacokinetics of hyperpolarized xenon-129 suggests that 80% is the maximum concentration that can be inhaled. Hyperpolarized xenon-129 delivered through inhalation can be detected in both pulmonary and cerebral tissues.3

Volume of distribution

Xenon is readily diffusible and able to disperse in the ventilated areas of the lung. There is a small amount of xenon uptake into the pulmonary vessels, followed by distribution to more distal organs.6

Protein binding

Not available.

Metabolism

As an inert gas, xenon is not metabolized under normal conditions. It does not have an effect on renal or hepatic function.4

Route of elimination

Xenon-129 administered through inhalation is eliminated through exhalation.6

Half-life

Xenon-129 in a 75% Xe/25% N2 gas mixture has an elimination half-life of 14.5 seconds. In a 25% Xe/75% N2 gas mixture, xenon-129 has an elimination half-life of 14.3 seconds.6

Clearance

Not available.

Adverse Effects
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Toxicity

Toxicity information regarding hyperpolarized Xenon-129 is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as transient hypoxia.6 Symptomatic and supportive measures are recommended. The mutagenic and carcinogenic potential of hyperpolarized Xenon-129 has not been evaluated.6

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
Not Available

Products

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dosage, form, labeller, route of administration, and marketing period.
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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
XenoviewGas75 mL/1LRespiratory (inhalation)Polarean, Inc.2022-12-23Not applicableUS flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
XenoviewXenon Xe-129 (63.5 L/1) + Helium (5651.5 L/1) + Nitrogen (635 L/1)GasRespiratory (inhalation)Polarean, Inc.2022-12-23Not applicableUS flag

Categories

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

Chemical Identifiers

UNII
9C7571UDT5
CAS number
13965-99-6
InChI Key
FHNFHKCVQCLJFQ-YPZZEJLDSA-N
InChI
InChI=1S/Xe/i1-2
IUPAC Name
(129Xe)xenon
SMILES
[129Xe]

References

Synthesis Reference

Honig, A. (2000). Bulk production and usage of hyperpolarized 129 Xenon. (U.S. Patent No. 6,125,654 A). U.S. Patent and Trademark Office. https://patentimages.storage.googleapis.com/07/b2/0d/d93e5d29439e56/US6125654.pdf

General References
  1. Mugler JP 3rd, Altes TA: Hyperpolarized 129Xe MRI of the human lung. J Magn Reson Imaging. 2013 Feb;37(2):313-31. doi: 10.1002/jmri.23844. [Article]
  2. Liu Z, Araki T, Okajima Y, Albert M, Hatabu H: Pulmonary hyperpolarized noble gas MRI: recent advances and perspectives in clinical application. Eur J Radiol. 2014 Jul;83(7):1282-1291. doi: 10.1016/j.ejrad.2014.04.014. Epub 2014 Apr 30. [Article]
  3. Wang Y, Dmochowski IJ: An Expanded Palette of Xenon-129 NMR Biosensors. Acc Chem Res. 2016 Oct 18;49(10):2179-2187. doi: 10.1021/acs.accounts.6b00309. Epub 2016 Sep 19. [Article]
  4. Bajaj T, Cascella M, Borger J: Xenon. . [Article]
  5. Eddy RL, Parraga G: Pulmonary xenon-129 MRI: new opportunities to unravel enigmas in respiratory medicine. Eur Respir J. 2020 Feb 6;55(2):1901987. doi: 10.1183/13993003.01987-2019. Print 2020 Feb. [Article]
  6. FDA Approved Drug Products: XENOVIEW (xenon Xe 129 hyperpolarized) for oral inhalation [Link]
  7. Globe News Wire: FDA Approves Polarean’s XENOVIEW (xenon Xe 129 hyperpolarized) for use with MRI for the Evaluation of Lung Ventilation [Link]
ChemSpider
8466280
RxNav
2626219
ChEBI
52453
ChEMBL
CHEMBL4594411

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
GasRespiratory (inhalation)
GasRespiratory (inhalation)75 mL/1L
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US10583205No2020-03-102035-02-20US flag
US11052161No2021-07-062035-12-29US flag

Properties

State
Gas
Experimental Properties
PropertyValueSource
melting point (°C)161.7 KBajaj et al. (2022). Xenon, StatPearls Publishing.
boiling point (°C)166.6 KBajaj et al. (2022). Xenon, StatPearls Publishing.
Predicted Properties
PropertyValueSource
logP0Chemaxon
Physiological Charge0Chemaxon
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
Chromatographic Properties
Collision Cross Sections (CCS)
Not Available

Drug created at January 03, 2023 20:01 / Updated at January 11, 2023 00:13