ISS-1018
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Identification
- Generic Name
- ISS-1018
- DrugBank Accession Number
- DB05463
- Background
ISS 1018 is a short, synthetic, unmethylated CpG oligodeoxynucleotide (CpG ODN) with immunostimulatory activity. ISS 1018 signals through Toll-like receptor 9 (TLR9) to induce the production of immunoglobulin by B cells and interferon (IFN) -alpha, IFN-beta, interleukin-12 (IL-12), and tumor necrosis factor - alpha (TNF-alpha) by plasmacytoid dendritic cells (pDC). ISS 1018 CpG ODN promotes antigen presentation and co-stimulatory molecule expression. ISS 1018 is currently being investigated in combination with HBsAg vaccine as a prophylactic treatment for to prevent Hepatitis B in adults. It is also being investigated in combination with rituximab for treatment of b-cell or non-hodgkin's lymphoma.
- Type
- Small Molecule
- Groups
- Investigational
- Synonyms
- Not Available
- External IDs
- 1018 ISS
- CPG 1018
- CPG-1018
- ISS 1018
- ISS 1018 CpG ODN
- ISS-1018
Pharmacology
- Indication
Investigated for use/treatment in colorectal cancer, hepatitis (viral, B), and lymphoma (non-hodgkin's). ISS 1018 is currently being investigated in combination with HBsAg vaccine as a prophylactic treatment for to prevent Hepatitis B in adults. It has also been investigated in combination with rituximab for treatment of b-cell or non-hodgkin's lymphoma.
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- Pharmacodynamics
ISS 1018 is a short, synthetic CpG oligodeoxynucleotide (CpG ODN) with immunostimulatory activity. ISS 1018 is an unmethylated CpG motifs in which regions of genomic DNA containing the cytosine-guanine dinucleotide does not show methylation of cytosine. ISS 1018 signals through Toll-like receptor 9 (TLR9) to induce the production of immunoglobulin by B cells and interferon (IFN) -alpha, IFN-beta, interleukin-12 (IL-12), and tumor necrosis factor - alpha (TNF-alpha) by plasmacytoid dendritic cells (pDC). ISS 1018 CpG ODN also promotes antigen presentation and co-stimulatory molecule expression.
- Mechanism of action
ISS 1018 signals through Toll-like receptor 9 (TLR9) to induce the production of immunoglobulin by B cells and interferon (IFN) -alpha, IFN-beta, interleukin-12 (IL-12), and tumor necrosis factor - alpha (TNF-alpha) by plasmacytoid dendritic cells (pDC). pDC and IFN-alpha and -beta then induce natural killer (NK) cell proliferation, NK cell production of IFN-gamma, and NK cell-mediated cytotoxicity. Secreted IFNs also stimulate bystander T cell activation and differentiation of naive CD4+ T cells into T-helper 1 cells on specific antigen challenge.
Target Actions Organism UToll-like receptor 9 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. View sample adverse effects data in our new Data Library!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
Categories
- Drug Categories
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- 25DT549L0G
- CAS number
- 937402-51-2
References
- General References
- Ponzio NM, Cutro S, Hu J, Marzouk A, Marshall JD: CpG oligodeoxynucleotide-induced immunity prevents growth of germinal center-derived B lymphoma cells. Int Immunopharmacol. 2006 Dec 20;6(13-14):2057-68. Epub 2006 Sep 18. [Article]
- Authors unspecified: Immunostimulatory DNA--Dynavax. AIC, Amb a 1 immunostimulatory conjugate, HBV-ISS, ISS 1018, ISS DNA, ISS DNA--dynavax, ISS1, ISS2. Drugs R D. 2002;3(3):193-6. [Article]
- Halperin SA, Van Nest G, Smith B, Abtahi S, Whiley H, Eiden JJ: A phase I study of the safety and immunogenicity of recombinant hepatitis B surface antigen co-administered with an immunostimulatory phosphorothioate oligonucleotide adjuvant. Vaccine. 2003 Jun 2;21(19-20):2461-7. [Article]
- External Links
- PubChem Substance
- 347910152
Clinical Trials
- Clinical Trials
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Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample data3 Terminated Prevention Coronavirus Disease 2019 (COVID‑19) 1 somestatus stop reason just information to hide 2 Completed Prevention Plague / Pneumonic Plague / Vaccine Preventable Diseases 1 somestatus stop reason just information to hide 2 Completed Treatment Non-Hodgkin's Lymphoma (NHL) 1 somestatus stop reason just information to hide 2 Terminated Prevention Viral Hepatitis B 1 somestatus stop reason just information to hide 2, 3 Completed Prevention Coronavirus Disease 2019 (COVID‑19) 1 somestatus stop reason just information to hide
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
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Key component of innate and adaptive immunity. TLRs (Toll-like receptors) control host immune response against pathogens through recognition of molecular patterns specific to microorganisms. TLR9 is a nucleotide-sensing TLR which is activated by unmethylated cytidine-phosphate-guanosine (CpG) dinucleotides (PubMed:14716310). Acts via MYD88 and TRAF6, leading to NF-kappa-B activation, cytokine secretion and the inflammatory response (PubMed:11564765, PubMed:17932028). Controls lymphocyte response to Helicobacter infection (By similarity). Upon CpG stimulation, induces B-cell proliferation, activation, survival and antibody production (PubMed:23857366)
- Specific Function
- interleukin-1 receptor binding
- Gene Name
- TLR9
- Uniprot ID
- Q9NR96
- Uniprot Name
- Toll-like receptor 9
- Molecular Weight
- 115858.665 Da
Drug created at November 18, 2007 18:25 / Updated at June 12, 2020 16:52