"目录号: HY-13740
Immunology/Inflammation-
Resiquimod 是有效的TLR7/TLR8激动剂，可以诱导 TNF-α，IL-6 和 IFN-α 等细胞因子水平变化。
Toll-like Receptor (TLR)
相关产品
TAK-242-Chloroquine diphosphate-GS-9620-Motolimod-Imiquimod-E6446 dihydrochloride-Atractylenolide I-C29-Leonurine-Procyanidin B1-Toll-like receptor modulator-
生物活性
Description
Resiquimod is a Toll-like receptor 7 and 8 (TLR7/TLR8) agonist that induces the levels of cytokines such as TNF-α, IL-6 and IFN-α.
In Vitro
Resiquimod (R-848) induces both hapten- and allergen-specific circulating T cells, including TH2 effectors, to produce IFN-γ and even to lose the ability to produce IL-4[2]. Resiquimod (R848) enhances PBL proliferation in a dose-dependent manner, and increases the number of BrdU-positive cells in BrdU incorporation assay. Cells treated with R848 exhibits significantly increased (3.5-fold) luciferase (a reporter of NF-κB activity) activity[3].
In Vivo
Resiquimod (R-848) (50 μg/bird, i.m. route) significantly up-regulates the expression of IFN-α, IFN-β, IFN-γ, IL-1β, IL-4, iNOS and MHC-II genes in SPF chicken[1].
Clinical Trial
NCT00960752
M.D. Anderson Cancer Center
Melanoma
May 2010
Phase 2
NCT00821652
Nina Bhardwaj-Cancer Research Institute, New York City-Icahn School of Medicine at Mount Sinai
Tumors
February 2009
Phase 1
NCT00470379
Mayo Clinic-National Cancer Institute (NCI)
Melanoma (Skin)
April 2006
Early Phase 1
NCT01676831
Abramson Cancer Center of the University of Pennsylvania
Cutaneous T Cell Lymphoma
February 2012
Phase 1-Phase 2
NCT01583816
Spirig Pharma Ltd.
Actinic Keratosis
May 2012
Phase 2
NCT01748747
Mayo Clinic-National Cancer Institute (NCI)
Recurrent Melanoma-Stage IIA Melanoma-Stage IIB Melanoma-Stage IIC Melanoma-Stage IIIA Melanoma-Stage IIIB Melanoma-Stage IIIC Melanoma-Stage IV Melanoma
October 2012
NCT01808950
Spirig Pharma Ltd.
Nodular Basal Cell Carcinoma
February 2013
Phase 1-Phase 2
NCT00117923
Graceway Pharmaceuticals, LLC
Warts
August 2004
Phase 2
NCT00117871
Graceway Pharmaceuticals, LLC
Warts
October 2004
Phase 2
NCT01737580
University of British Columbia
Influenza Vaccination in Seniors
April 2013
Phase 1
NCT00116675
Graceway Pharmaceuticals, LLC
Warts
March 2005
Phase 2
NCT00116662
Graceway Pharmaceuticals, LLC
Warts
March 2005
Phase 2
NCT00114920
Graceway Pharmaceuticals, LLC
Warts
March 2004
Phase 2
NCT00115141
Graceway Pharmaceuticals, LLC
Warts
April 2004
Phase 2
NCT00948961
Celldex Therapeutics
Advanced Malignancies
September 2009
Phase 1-Phase 2
NCT02126579
Craig L Slingluff, Jr-University of Virginia
Melanoma-Metastatic Melanoma-Mucosal Melanoma
April 2014
Phase 1-Phase 2
NCT00175435
University of British Columbia
Hepatitis B
August 2005
Phase 1-Phase 2
NCT01204684
Jonsson Comprehensive Cancer Center
Glioma-Anaplastic Astrocytoma-Anaplastic Astro-oligodendroglioma-Glioblastoma
September 2010
Phase 2
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References
[1].Sachan S, et al. Adjuvant potential of resiquimod with inactivated Newcastle disease vaccine and its mechanism of action in chicken. Vaccine. 2015 Aug 26;33(36):4526-32.
[2].Brugnolo F, et al. The novel synthetic immune response modifier R-848 (Resiquimod) shifts human allergen-specific CD4+ TH2 lymphocytes into IFN-gamma-producing cells. J Allergy Clin Immunol. 2003 Feb;111(2):380-8.
[3].Zhou ZX, et al. Immune effects of R848: evidences that suggest an essential role of TLR7/8-induced, Myd88- and NF-κB-dependent signaling in the antiviral immunity of Japanese flounder (Paralichthys olivaceus). Dev Comp Immunol. 2015 Mar;49(1):113-20.