Viral and Nonviral Uses of Imiquimod: A Review

Gupta, Aditya K.; Cherman, Andrea M.; Tyring, Stephen K.

doi:10.1007/s10227-005-0023-5

Cited by 93 publications

(94 citation statements)

References 94 publications

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“…These results are similar to those obtained with 3 applications/week (Edwards et al 1998;Garland et al 2001). Therefore, 3 times per week treatment schedule is recommended because of a relatively lower rate of side effects (Perry and Lamb 1999;Gupta et al 2004;Chang et al 2005;Scheinfeld and Lehman 2006).…”

Section: External Genital and Perianal Wartssupporting

confidence: 83%

Advances in the use of topical imiquimod to treat dermatologic disorders

Micali¹

2008

TCRM

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Imiquimod (IQ) is an immune-response modifying agent, fi rst approved by FDA for the topical treatment of external genital and perianal warts in 1997. It induces, through stimulation of Toll-like receptors (TLRs) localized on the surface of antigen-presenting cells, synthesis and release of several endogenous pro-infl ammatory cytokines such as interferon-α (IFN-α), tumor necrosis factor-α (TNF-α) and interleukins (IL) 6 and 12, which in turn stimulate both the innate and acquired immune pathways, resulting in upregulation of natural antiviral and antitumor activity. IQ 5% cream has been used for the treatment of a wide variety of dermatologic conditions in which the immune system is thought to play a role in regression of the disease. In some disorders, such as genital and perianal warts, actinic keratoses, basal cell carcinomas, Bowen's disease and molluscum contagiosum, relative safety and effi cacy are supported by randomized controlled trials of IQ. However, it is common for patients to experience local skin reactions, which can range from mild to severe in intensity, but usually resolve 1-2 weeks after interrupting treatment. Additional randomized trials are encouraged to assess safety and effi cacy of IQ in the treatment of an even wider range of cutaneous disorders.

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Section: External Genital and Perianal Wartssupporting

confidence: 83%

Advances in the use of topical imiquimod to treat dermatologic disorders

Micali¹

2008

TCRM

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“…Furthermore, Wang et al (43) investigated the action of a dual TLR7/8 agonist in tumor-bearing mice, and demonstrated that subcutaneous administration of the above TLR7/8 agonist effectively prevented lung metastasis by inducing Th1-type immune responses and potent antitumor activity in mice via TLR7 and MyD88-dependent pathways (43). In addition, the TLR7 agonist imiquimod has been successfully applied in the treatment of actinic keratosis, basal cell carcinoma, Bowen's disease and lentigo maligna (44,45).…”

Section: Resultsmentioning

confidence: 99%

TLR7 Gln11Leu single nucleotide polymorphism and susceptibility to cutaneous melanoma

et al. 2016

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Abstract. Cutaneous melanoma is a life-threatening skin cancer. Its incidence is rapidly increasing, and early diagnosis is the main factor able to improve its poor prognosis. Toll-like receptors (TLRs) are transmembrane glycoproteins that recognize pathogen-and damage-associated molecular patterns, against which TLRs activate the innate immune response and initiate the adaptive immune response. Genetic variations of these receptors may alter the immune system, and are involved in evolution and susceptibility to various diseases, including cancer. The aim of the present study was to evaluate whether the presence of TLR7 glutamine (Gln) 11 leucine (Leu) polymorphism confers an increased susceptibility to cutaneous melanoma. For that purpose, a case-control study was performed with 182 melanoma cases and 89 controls. To highlight the possible association between the aforementioned polymorphism and the susceptibility to melanoma, 93 cases of single melanoma and 89 cases of multiple primary melanoma (MPM) were compared in the present study. Since the TLR7 gene is localized on the chromosome X, the allelic frequency of the Gln11Leu polymorphism was analyzed separately in males and females. The distribution of allele frequencies between melanoma cases and controls (P=0.245) and between single melanoma and MPM cases (P=0.482) was not significant. Therefore, the present results do not suggest an association between TLR7 Gln11Leu polymorphism and susceptibility to cutaneous melanoma. Further studies are required to analyze the influence of other TLR polymorphisms on the susceptibility to malignant melanoma and the involvement of innate immunity in this malignancy.

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“…Several studies reported high efficacy of imiqimod for the treatment of superficial BCC with a cure rate ranging from 43-94% (42-45), whereas it is less efficacious for nodular BCC with a cure rates of 50-65% (43,46). Imiquimod has also been used in the treatment of warts, actinic keratosis, Bowen's disease and lentigo maligna melanoma (17,18). In addition to imiquimod, other topical agents, such as nicotinamide, all-trans retinoic acid, adapalene, zinc and sodium tosylchloramide have also been reported to act through TLRs (47).…”

Section: Discussionmentioning

confidence: 99%

“…Furthermore, their role in tumor development and progression has attracted increasing attention recently (11). Imiquimod, an agonist of TLR7 (16) has been shown to induce the expression of several cytokines such as IFN-α, IL-12 and TNF-α, which mediate its anticancer effects (pro-apoptotic, anti-invasive and anti-angiogenic) (17). It may be applied topically in the treatment of premalignant and malignant skin disorders, in particular BCC (17,18).…”

Section: Introductionmentioning

confidence: 99%

“…Imiquimod, an agonist of TLR7 (16) has been shown to induce the expression of several cytokines such as IFN-α, IL-12 and TNF-α, which mediate its anticancer effects (pro-apoptotic, anti-invasive and anti-angiogenic) (17). It may be applied topically in the treatment of premalignant and malignant skin disorders, in particular BCC (17,18). The high efficacy of this TLR7 agonist toward BCC supports a possible role of this receptor in the induction of BCC, and consequently, polymorphisms of this receptor could be responsible for a greater or lesser susceptibility to BCC.…”

Section: Introductionmentioning

confidence: 99%

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Association between Toll-like receptor 7 Gln11Leu single-nucleotide polymorphism and basal cell carcinoma

et al. 2016

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Abstract. Non-melanoma skin cancers (NMSC) are the most common form of human skin cancer. The majority of NMSC are basal cell carcinoma (BCC) and squamous cell carcinoma (SCC) with a BCC:SCC incidence ratio of 4:1 in immunocompetent patients. Toll-like receptors (TLRs) are transmembrane glycoproteins that recognize pathogen-associated molecular patterns and damage-associated molecular patterns, against which they activate the innate immune response and initiate the adaptive immune response. Genetic variations of these receptors can alter the immune system and are involved in evolution and susceptibility of various diseases, including cancer. Imiquimod, an agonist of TLR7, is applied topically in the treatment of premalignant and malignant skin disorders, in particular BCC. The high efficacy of this TLR7 agonist toward BCC supports a possible role of this receptor in the induction of BCC and, consequently, polymorphisms of this receptor could be responsible for a greater or lesser susceptibility to BCC. The aim of the present study was to evaluate whether the presence of the functional TLR7 rs179008/Gln11Leu promoter polymorphism conferred an increased susceptibility to BCC. A case-control study with 177 BCC cases and 158 controls was performed to highlight the possible association between this polymorphism and the susceptibility to BCC. As the TLR7 gene is localized on chromosome X, the allelic frequency of this polymorphism was analyzed separately in males and females. The analysis of the distribution of frequencies of wild-type TLR7 and variant TLR7 carrying the single-nucleotide polymorphism (SNP) rs179008 in patients with BCC and healthy subjects did not reveal any statistically significant difference between cases and controls. This study does not suggest the involvement of the SNP rs179008 of TLR7 in the susceptibility to BCC, but cannot exclude a role for TLR7 in BCC carcinogenesis considering the high efficacy of the TLR7 agonist, imiquimod, in the treatment of this neoplastic disorder.

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Viral and Nonviral Uses of Imiquimod: A Review

Abstract: Imiquimod has been shown to be a safe and effective treatment for a variety of skin conditions.

Cited by 93 publications

References 94 publications

Advances in the use of topical imiquimod to treat dermatologic disorders

Advances in the use of topical imiquimod to treat dermatologic disorders

TLR7 Gln11Leu single nucleotide polymorphism and susceptibility to cutaneous melanoma

Association between Toll-like receptor 7 Gln11Leu single-nucleotide polymorphism and basal cell carcinoma

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