Custirsen

Identification

Name
Custirsen
Accession Number
DB05487
Type
Small Molecule
Groups
Investigational
Description

Custirsen is a benzopyran with potential antineoplastic activity. Custirsen acts as a selective estrogen receptor modulator (SERM), inhibiting the proliferation of estrogen-sensitive breast cancer cells. This agent also inhibits growth and induces apoptosis of glioblastoma cells via a mechanism independent of estrogen receptor-related mechanisms. Custirsen is also being investigated in the treatment of primary brain tumors.

Synonyms
Not Available
External IDs
CC-8490 / OGX-011
Categories
UNII
L26E95NLRK
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 brain cancer and breast cancer.

Structured Indications
Not Available
Pharmacodynamics

CC-8490, a new anti-cancer compound from Celgene's proprietary class of benzopyrans, being evaluated as a potential therapy for brain cancer. The National Cancer Institute also reports applications in breast cancer related to potential antineoplastic activity. CC-8490 acts as a selective estrogen receptor modulator (SERM), inhibiting the proliferation of estrogen-sensitive breast cancer cells. This agent also inhibits growth and induces apoptosis of glioblastoma cells via a mechanism independent of estrogen receptor-related mechanisms.

Mechanism of action

CC-8490 acts as a selective estrogen receptor modulator (SERM), inhibiting the proliferation of estrogen-sensitive breast cancer cells. This agent also inhibits growth and induces apoptosis of glioblastoma cells via a mechanism independent of estrogen receptor-related mechanisms.

Preliminary results in studies regarding the mechanism of action in brain cancer suggest that C-8490 surpresses nuclear factor (NF)-KB with its target genes IEX-3, SOD2, IL6, and IL8.

TargetActionsOrganism
UEstrogen receptor alphaNot AvailableHuman
UNuclear factor NF-kappa-B p100 subunitNot AvailableHuman
UNuclear factor NF-kappa-B p105 subunitNot 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

safe and well tolerated in a Phase I trial in healthy human volunteers.

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. Hui AM, Zhang W, Chen W, Xi D, Purow B, Friedman GC, Fine HA: Agents with selective estrogen receptor (ER) modulator activity induce apoptosis in vitro and in vivo in ER-negative glioma cells. Cancer Res. 2004 Dec 15;64(24):9115-23. [PubMed:15604281]
External Links
PubChem Substance
347910168

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableCancers1
1CompletedTreatmentBrain and Central Nervous System Tumors1
1CompletedTreatmentCardiac Conduction and Repolarization1
1CompletedTreatmentGlioblastomas / Malignant Gliomas1
1, 2CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
2CompletedTreatmentProstate Cancer2
3CompletedTreatmentProstate Cancer2
3RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
3TerminatedTreatmentCastrate-resistant Prostate Cancer (CRPC) / Hormone Refractory Prostate Cancer1

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
Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissu...
Gene Name
ESR1
Uniprot ID
P03372
Uniprot Name
Estrogen receptor
Molecular Weight
66215.45 Da
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Transcriptional activator activity, rna polymerase ii core promoter proximal region sequence-specific binding
Specific Function
NF-kappa-B is a pleiotropic transcription factor present in almost all cell types and is the endpoint of a series of signal transduction events that are initiated by a vast array of stimuli related...
Gene Name
NFKB2
Uniprot ID
Q00653
Uniprot Name
Nuclear factor NF-kappa-B p100 subunit
Molecular Weight
96748.355 Da
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Transcriptional repressor activity, rna polymerase ii transcription regulatory region sequence-specific binding
Specific Function
NF-kappa-B is a pleiotropic transcription factor present in almost all cell types and is the endpoint of a series of signal transduction events that are initiated by a vast array of stimuli related...
Gene Name
NFKB1
Uniprot ID
P19838
Uniprot Name
Nuclear factor NF-kappa-B p105 subunit
Molecular Weight
105355.175 Da

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