Resiquimod Explained
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
Notes and References
- Patents #5, 939, 090 and 6, 365, 166
- Szeimies RM, Bichel J, Ortonne JP, Stockfleth E, Lee J, Meng TC . A phase II dose-ranging study of topical resiquimod to treat actinic keratosis . The British Journal of Dermatology . 159 . 1 . 205–210 . July 2008 . 18476957 . 10.1111/j.1365-2133.2008.08615.x . 205257237 .
- Wu JJ, Huang DB, Tyring SK . Resiquimod: a new immune response modifier with potential as a vaccine adjuvant for Th1 immune responses . Antiviral Research . 64 . 2 . 79–83 . November 2004 . 15498602 . 10.1016/j.antiviral.2004.07.002 .
- Fife KH, Meng TC, Ferris DG, Liu P . 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 . 18039918 . 2224757 . 10.1128/AAC.01173-07 .
- Rook AH, Gelfand JM, Wysocka M, Troxel AB, Benoit B, Surber C, Elenitsas R, Buchanan MA, Leahy DS, Watanabe R, Kirsch IR, Kim EJ, Clark RA . 6 . Topical resiquimod can induce disease regression and enhance T-cell effector functions in cutaneous T-cell lymphoma . Blood . 126 . 12 . 1452–1461 . September 2015 . 26228486 . 4573868 . 10.1182/blood-2015-02-630335 .
- Tomai MA, Miller RL, Lipson KE, Kieper WC, Zarraga IE, Vasilakos JP . Resiquimod and other immune response modifiers as vaccine adjuvants . Expert Review of Vaccines . 6 . 5 . 835–847 . October 2007 . 17931162 . 10.1586/14760584.6.5.835 . 30401602 .
- Rodell CB, Arlauckas SP, Cuccarese MF, Garris CS, Li R, Ahmed MS, Kohler RH, Pittet MJ, Weissleder R . 6 . TLR7/8-agonist-loaded nanoparticles promote the polarization of tumour-associated macrophages to enhance cancer immunotherapy . En . Nature Biomedical Engineering . 2 . 8 . 578–588 . August 2018 . 31015631 . 6192054 . 10.1038/s41551-018-0236-8 .
- Hurst J, Prinz N, Lorenz M, Bauer S, Chapman J, Lackner KJ, von Landenberg P . 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 . 19249118 . 10.1016/j.imbio.2008.12.003 .
- Zagon IS, Donahue RN, Rogosnitzky M, McLaughlin PJ . 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 . 18480416 . 10.3181/0802-RM-58 . 35164284 .
- Web site: Committee for Orphan Medicinal Products . European Medicines Agency . 27 May 2016 . Resiquimod for the treatment of cutaneous T-cell lymphoma . Public summary of opinion on orphan designation .