AEG35156

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

Identification

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Name
AEG35156
Accession Number
DB06184
Type
Small Molecule
Groups
Investigational
Description

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.

Synonyms
Not Available
External IDs
GEM 640 / GEM-640 / GEM640
Categories
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 cancer/tumors (unspecified) and leukemia (myeloid).

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
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. 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. [PubMed:18027851]
  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. [PubMed:16951243]
External Links
Not Available

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentUnspecified Adult Solid Tumor, Protocol Specific2
1TerminatedTreatmentCancer, Advanced1
1, 2TerminatedTreatmentCarcinoma NOS / Pancreas1
1, 2TerminatedTreatmentHuman Mammary Carcinoma1
1, 2TerminatedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
2TerminatedTreatmentLeukemias1

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
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. [PubMed:16394139]
  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. [PubMed:18027851]

Drug created on March 19, 2008 10:16 / Updated on June 04, 2019 06:21