NAV

AEG35156

This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.

Identification

Generic Name
AEG35156
DrugBank Accession Number
DB06184
Background

A second-generation synthetic antisense oligonucleotide with potential antineoplastic activity. AEG35156 selectively blocks the cellular expression of X-linked inhibitor of apoptosis protein (XIAP), a pivotal inhibitor of apoptosis that is overexpressed in many tumors. This agent reduces total levels of XIAP in tumor cells, working synergistically with cytotoxic drugs to overcome tumor cell resistance to apoptosis. XIAP interferes with both the intrinsic and extrinsic program-death signaling pathways, which may render tumor cells resistant to apoptosis.

Type
Small Molecule
Groups
Investigational
Synonyms
Not Available
External IDs
  • GEM 640
  • GEM-640
  • GEM640
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Pharmacology

Indication

Investigated for use/treatment in cancer/tumors (unspecified) and leukemia (myeloid).

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Contraindications & Blackbox Warnings
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Pharmacodynamics

Not Available

Mechanism of action
TargetActionsOrganism
UE3 ubiquitin-protein ligase XIAPNot 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

Categories

Drug Categories
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. Shaw TJ, Lacasse EC, Durkin JP, Vanderhyden BC: Downregulation of XIAP expression in ovarian cancer cells induces cell death in vitro and in vivo. Int J Cancer. 2008 Mar 15;122(6):1430-4. [Article]
  2. LaCasse EC, Cherton-Horvat GG, Hewitt KE, Jerome LJ, Morris SJ, Kandimalla ER, Yu D, Wang H, Wang W, Zhang R, Agrawal S, Gillard JW, Durkin JP: Preclinical characterization of AEG35156/GEM 640, a second-generation antisense oligonucleotide targeting X-linked inhibitor of apoptosis. Clin Cancer Res. 2006 Sep 1;12(17):5231-41. [Article]
Not Available

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2TerminatedTreatmentLeukemias1
1CompletedTreatmentUnspecified Adult Solid Tumor, Protocol Specific2
1TerminatedTreatmentAdvanced Malignant Neoplasm1
1, 2CompletedTreatmentAdvanced Hepatocellular Carcinoma (HCC)1
1, 2TerminatedTreatmentB-Cell Chronic Lymphocytic Leukemia / B-Cell Lymphoma1

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
Chromatographic Properties
Collision Cross Sections (CCS)
Not Available

Targets

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Details1. E3 ubiquitin-protein ligase XIAP
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
Multi-functional protein which regulates not only caspases and apoptosis, but also modulates inflammatory signaling and immunity, copper homeostasis, mitogenic kinase signaling, cell proliferation,...
Gene Name
XIAP
Uniprot ID
P98170
Uniprot Name
E3 ubiquitin-protein ligase XIAP
Molecular Weight
56684.41 Da
References
  1. Lacasse EC, Kandimalla ER, Winocour P, Sullivan T, Agrawal S, Gillard JW, Durkin J: Application of XIAP antisense to cancer and other proliferative disorders: development of AEG35156/ GEM640. Ann N Y Acad Sci. 2005 Nov;1058:215-34. [Article]
  2. Shaw TJ, Lacasse EC, Durkin JP, Vanderhyden BC: Downregulation of XIAP expression in ovarian cancer cells induces cell death in vitro and in vivo. Int J Cancer. 2008 Mar 15;122(6):1430-4. [Article]

Drug created at March 19, 2008 16:16 / Updated at June 12, 2020 16:52