XEN-2174

Identification

Generic Name
XEN-2174
DrugBank Accession Number
DB05012
Background

XEN-2174 is a synthetic drug modeled on a peptide from the venom of a cone shell found on Australia's Great Barrier Reef. XEN-2174 represents a new class of molecules, called the chi conopeptides that selectively inhibit the Norepinephrine Transporter (NET). NET is the primary mechanism regulating the biological effects of norepinephrine (NE) on the body. In episodes of pain, inhibition of NET by XEN-2174 elevates the levels of NE leading to the activation of inhibitory pathways preventing pain signals from reaching the brain.

Type
Small Molecule
Groups
Investigational
Synonyms
Not Available
External IDs
  • XEN-2174
  • XEN2174

Pharmacology

Indication

For the treatment of chronic cancer pain.

Pharmacology
Reduce drug development failure rates
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Contraindications & Blackbox Warnings
Contraindications
Avoid life-threatening adverse drug events
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Pharmacodynamics

Not Available

Mechanism of action

XEN-2174 targets the Norepinephrine Transporter (NET). Inhibition of this transporter elevates the levels of norepinephrine (NE) in the spinal cord preventing pain signals from reaching the brain. XEN-2174 acts to restore the balance by promoting the activation of inhibitory pain pathways to relieve the sensation of pain.

TargetActionsOrganism
USodium-dependent noradrenaline transporterNot AvailableHumans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

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
Not Available

Categories

Drug Categories
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
3MY01D9YW4
CAS number
701909-57-1

References

General References
  1. Obata H, Conklin D, Eisenach JC: Spinal noradrenaline transporter inhibition by reboxetine and Xen2174 reduces tactile hypersensitivity after surgery in rats. Pain. 2005 Feb;113(3):271-6. [Article]
  2. Nielsen CK, Lewis RJ, Alewood D, Drinkwater R, Palant E, Patterson M, Yaksh TL, McCumber D, Smith MT: Anti-allodynic efficacy of the chi-conopeptide, Xen2174, in rats with neuropathic pain. Pain. 2005 Nov;118(1-2):112-24. Epub 2005 Sep 9. [Article]
PubChem Substance
347909891

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
Not Available
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

Drugtargets2
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Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Norepinephrine:sodium symporter activity
Specific Function
Amine transporter. Terminates the action of noradrenaline by its high affinity sodium-dependent reuptake into presynaptic terminals.
Gene Name
SLC6A2
Uniprot ID
P23975
Uniprot Name
Sodium-dependent noradrenaline transporter
Molecular Weight
69331.42 Da

Drug created on October 21, 2007 22:23 / Updated on March 26, 2021 03:54