AVI-4557

Identification

Name
AVI-4557
Accession Number
DB05447
Type
Small Molecule
Groups
Investigational
Description

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.

Synonyms
Not Available
International/Other Brands
Neugene
Categories
Not Available
UNII
Not Available
CAS number
Not Available
Weight
Not Available
Chemical Formula
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

Pharmacology

Indication

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

Structured Indications
Not Available
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 AvailableHuman
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
Toxicity
Not Available
Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
Not Available
Food Interactions
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. [PubMed:12065433]
External Links
PubChem Substance
347910144

Clinical Trials

Clinical Trials
Not Available

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

Taxonomy

Classification
Not classified

Targets

Kind
Protein
Organism
Human
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. [PubMed:10592235]

Drug created on November 18, 2007 11:25 / Updated on November 06, 2017 06:45