Identification
- Generic Name
- Apatorsen
- DrugBank Accession Number
- DB06094
- Background
Apatorsen is a second generation antisense drug which in preclinical experiments, inhibits production of Heat Shock Protein 27 (Hsp27) a cell survival protein found at elevated levels in many human cancers including prostate, lung, breast, ovarian, bladder, renal, pancreatic, multiple myeloma and liver cancer.
- Type
- Biotech
- Groups
- Investigational
- Biologic Classification
- Gene Therapies
Antisense oligonucleotides - Synonyms
- Apatorsen
Pharmacology
- Indication
Investigated for use/treatment in cancer/tumors (unspecified).
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
OGX-427 significantly decreases levels of Hsp27, induces apoptosis in several human cancer cell lines, has single agent anti-tumor activity, and acts as a chemosensitizer in combination with several cytotoxic drugs including docetaxel.
- Mechanism of action
Target Actions Organism UHeat shock protein beta-1 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
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
Products
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Ingredient UNII CAS InChI Key Apatorsen sodium 3N4G7RE66Y 915443-09-3 Not applicable
Categories
- Drug Categories
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- IFJ6X26JW6
- CAS number
- 1002331-21-6
References
- General References
- Kamada M, So A, Muramaki M, Rocchi P, Beraldi E, Gleave M: Hsp27 knockdown using nucleotide-based therapies inhibit tumor growth and enhance chemotherapy in human bladder cancer cells. Mol Cancer Ther. 2007 Jan;6(1):299-308. Epub 2007 Jan 11. [Article]
- Rocchi P, Jugpal P, So A, Sinneman S, Ettinger S, Fazli L, Nelson C, Gleave M: Small interference RNA targeting heat-shock protein 27 inhibits the growth of prostatic cell lines and induces apoptosis via caspase-3 activation in vitro. BJU Int. 2006 Nov;98(5):1082-9. Epub 2006 Jul 28. [Article]
- Zoubeidi A, Zardan A, Beraldi E, Fazli L, Sowery R, Rennie P, Nelson C, Gleave M: Cooperative interactions between androgen receptor (AR) and heat-shock protein 27 facilitate AR transcriptional activity. Cancer Res. 2007 Nov 1;67(21):10455-65. [Article]
- External Links
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 2 Completed Treatment Bladder Cancer / Urothelial Carcinoma 1 2 Completed Treatment Castration Resistant Prostate Cancer 1 2 Completed Treatment Metastatic Bladder Cancer / Urinary Tract Neoplasms / Urologic Neoplasms 1 2 Completed Treatment Non-squamous Non-small-cell Lung Cancer (NSQ NSCLC) 1 2 Completed Treatment Pancreatic Cancer 1 2 Terminated Treatment Metastatic Castration-Resistant Prostate Cancer (mCRPC) / Prostate Cancer / Prostate Specific Antigen 1 2 Unknown Status Treatment Squamous Cell Lung Cancer 1 1 Completed Treatment Neoplasm 1 1 Unknown Status Treatment Bladder Cancer 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
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Ubiquitin binding
- Specific Function
- Involved in stress resistance and actin organization.
- Gene Name
- HSPB1
- Uniprot ID
- P04792
- Uniprot Name
- Heat shock protein beta-1
- Molecular Weight
- 22782.3 Da
Drug created at November 18, 2007 18:29 / Updated at September 05, 2022 12:50