Identification

Generic Name
AVI-4557
DrugBank Accession Number
DB05447
Background

AVI-4557 is an oral antisense compound that selectively inhibits the metabolic enzyme cytochrome P450 3A4 (CYP), a liver enzyme responsible for the metabolism or breakdown of approximately half of currently marketed drugs. Studies indicate that AVI-4557 can successfully reduce the rate of metabolism for certain drugs, therefore allowing greater and longer availability of the drug in the patient's system through a decrease in clearance and an increase in maximal blood concentration (Cmax). AVI-4557 is therefore indicated to limit toxicity for patients receiving highly-toxic therapeutic drugs for treatment of anxiety, cancer, and a number of other serious conditions.

Type
Small Molecule
Groups
Investigational
Synonyms
Not Available

Pharmacology

Indication

Investigated for use/treatment in adverse effects (chemotherapy) and adverse effects (drug).

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Contraindications & Blackbox Warnings
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Pharmacodynamics

selectively inhibits the metabolic enzyme cytochrome P450 3A4 (CYP), a liver enzyme responsible for the metabolism or breakdown of approximately half of currently marketed drugs. Studies indicate that AVI-4557 can successfully reduce the rate of metabolism when co-administered with certain therapeutic drugs, allowing greater and longer availability of the drug in the patient's system without an increase in toxicity.

Mechanism of action

selectively inhibits the metabolic enzyme cytochrome P450 3A4 (CYP), a liver enzyme responsible for the metabolism or breakdown of approximately half of currently marketed drugs. S

TargetActionsOrganism
UHepatocyte nuclear factor 4-alphaNot 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
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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

Products

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International/Other Brands
Neugene

Categories

Drug Categories
Not Available
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
Not Available
CAS number
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

References

General References
  1. Arora V, Cate ML, Ghosh C, Iversen PL: Phosphorodiamidate morpholino antisense oligomers inhibit expression of human cytochrome P450 3A4 and alter selected drug metabolism. Drug Metab Dispos. 2002 Jul;30(7):757-62. [Article]
PubChem Substance
347910144

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

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Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
Transcriptionally controlled transcription factor. Binds to DNA sites required for the transcription of alpha 1-antitrypsin, apolipoprotein CIII, transthyretin genes and HNF1-alpha. May be essentia...
Gene Name
HNF4A
Uniprot ID
P41235
Uniprot Name
Hepatocyte nuclear factor 4-alpha
Molecular Weight
52784.205 Da
References
  1. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [Article]

Drug created at November 18, 2007 18:25 / Updated at June 12, 2020 16:52