Chemistry:Resiquimod
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| Routes of administration | Topical |
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| Formula | C17H22N4O2 |
| Molar mass | 314.389 g·mol−1 |
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Resiquimod (R-848) is a drug that acts as an immune response modifier, and has antiviral and antitumour activity. It is used as a topical gel[1] in the treatment of skin lesions[2] such as those caused by the herpes simplex virus[3][4] and cutaneous T cell lymphoma,[5] and as an adjuvant to increase the effectiveness of vaccines.[6] In an animal disease model, systemic administration of resiquimod-loaded nanoparticles has been shown to improve response rates to cancer immunotherapy with a checkpoint inhibitor through stimulation of tumor-associated macrophages.[7] It has several mechanisms of action, being both an agonist for toll-like receptor 7 and 8,[8] and an upregulator of the opioid growth factor receptor.[9] On 28 April 2016, orphan designation (EU/3/16/1653) was granted by the European Commission to Galderma R&D, France for resiquimod to be used in the treatment of cutaneous T-cell lymphoma.[10]
See also
References
- ↑ Patents #5, 939, 090 and 6, 365, 166
- ↑ "A phase II dose-ranging study of topical resiquimod to treat actinic keratosis". The British Journal of Dermatology 159 (1): 205–210. July 2008. doi:10.1111/j.1365-2133.2008.08615.x. PMID 18476957.
- ↑ "Resiquimod: a new immune response modifier with potential as a vaccine adjuvant for Th1 immune responses". Antiviral Research 64 (2): 79–83. November 2004. doi:10.1016/j.antiviral.2004.07.002. PMID 15498602.
- ↑ "Effect of resiquimod 0.01% gel on lesion healing and viral shedding when applied to genital herpes lesions". Antimicrobial Agents and Chemotherapy 52 (2): 477–482. February 2008. doi:10.1128/AAC.01173-07. PMID 18039918.
- ↑ "Topical resiquimod can induce disease regression and enhance T-cell effector functions in cutaneous T-cell lymphoma". Blood 126 (12): 1452–1461. September 2015. doi:10.1182/blood-2015-02-630335. PMID 26228486.
- ↑ "Resiquimod and other immune response modifiers as vaccine adjuvants". Expert Review of Vaccines 6 (5): 835–847. October 2007. doi:10.1586/14760584.6.5.835. PMID 17931162.
- ↑ "TLR7/8-agonist-loaded nanoparticles promote the polarization of tumour-associated macrophages to enhance cancer immunotherapy" (in En). Nature Biomedical Engineering 2 (8): 578–588. August 2018. doi:10.1038/s41551-018-0236-8. PMID 31015631.
- ↑ "TLR7 and TLR8 ligands and antiphospholipid antibodies show synergistic effects on the induction of IL-1beta and caspase-1 in monocytes and dendritic cells". Immunobiology 214 (8): 683–691. February 2009. doi:10.1016/j.imbio.2008.12.003. PMID 19249118.
- ↑ "Imiquimod upregulates the opioid growth factor receptor to inhibit cell proliferation independent of immune function". Experimental Biology and Medicine 233 (8): 968–979. August 2008. doi:10.3181/0802-RM-58. PMID 18480416.
- ↑ Committee for Orphan Medicinal Products (27 May 2016). "Resiquimod for the treatment of cutaneous T-cell lymphoma". Public summary of opinion on orphan designation. European Medicines Agency. http://www.ema.europa.eu/docs/en_GB/document_library/Orphan_designation/2016/05/WC500207498.pdf.
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