Identification

Generic Name
Custirsen
DrugBank Accession Number
DB05487
Background

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.

Type
Biotech
Groups
Investigational
Biologic Classification
Gene Therapies
Antisense oligonucleotides
Synonyms
  • Custirsen
External IDs
  • CC-8490
  • OGX-011

Pharmacology

Indication

Investigated for use/treatment in brain cancer and breast cancer.

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Contraindications & Blackbox Warnings
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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 AvailableHumans
UNuclear factor NF-kappa-B p100 subunitNot AvailableHumans
UNuclear factor NF-kappa-B p105 subunitNot 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

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

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
L26E95NLRK
CAS number
890056-27-6

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. [Article]
PubChem Substance
347910168
ChemSpider
34983386
Wikipedia
Custirsen

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3CompletedTreatmentProstate Cancer2
3TerminatedTreatmentCastration Resistant Prostate Cancer / Hormone Refractory Prostate Cancer1
3Unknown StatusTreatmentNon-Small Cell Lung Carcinoma (NSCLC)1
2CompletedTreatmentBreast Cancer1
2CompletedTreatmentProstate Cancer3
1CompletedNot AvailableCancer1
1CompletedTreatmentBladder Cancer, Cancer / Breast Cancer / Lung Cancers / Ovarian Cancer / Prostate Cancer / Renal Cancers / Unspecified Adult Solid Tumor, Protocol Specific1
1CompletedTreatmentBrain and Central Nervous System Tumors1
1CompletedTreatmentCardiac Conduction and Repolarization1
1CompletedTreatmentGlioblastoma Multiforme (GBM) / Gliomas, Malignant1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available

Targets

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Kind
Protein
Organism
Humans
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
Humans
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
Humans
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 at November 18, 2007 18:25 / Updated at September 05, 2022 12:50