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.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- 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.
Target Actions Organism UEstrogen receptor alpha Not Available Humans UNuclear factor NF-kappa-B p100 subunit Not Available Humans UNuclear factor NF-kappa-B p105 subunit Not Available Humans - 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
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.- 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
- 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]
- External Links
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 3 Completed Treatment Prostate Cancer 2 3 Terminated Treatment Castration Resistant Prostate Cancer / Hormone Refractory Prostate Cancer 1 3 Unknown Status Treatment Non-Small Cell Lung Carcinoma (NSCLC) 1 2 Completed Treatment Breast Cancer 1 2 Completed Treatment Prostate Cancer 3 1 Completed Not Available Cancer 1 1 Completed Treatment Bladder Cancer, Cancer / Breast Cancer / Lung Cancers / Ovarian Cancer / Prostate Cancer / Renal Cancers / Unspecified Adult Solid Tumor, Protocol Specific 1 1 Completed Treatment Brain and Central Nervous System Tumors 1 1 Completed Treatment Cardiac Conduction and Repolarization 1 1 Completed Treatment Glioblastoma Multiforme (GBM) / Gliomas, Malignant 1
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
- 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