Imiquimod for the treatment of skin cancer

Topical Administration of Anticancer Drugs for Skin Cancer Treatment

“…Imiquimod is an immune response modifier that directly and indirectly interacts with the immune system (Perrotta et al, 2011). It was initially approved by the FDA in 1997 for genital and perianal wart treatment but has been used off-label for neoplastic skin treatments (Burns & Brown, 2005). In 2004, the FDA approved the use of imiquimod 5% cream for the treatment of actinic keratosis and superficial BCC in patients for whom surgery is not an option (Perrota et al, 2011).…”

“…Moreover, response rates differ for superficial and invasive cancers. For example, Burns (2005) reported that imiquimod was more effective in treating superficial BCC than for nodular BCC. This is likely because nodular BCC occurs deep in the dermis and the drug may not reach the full depth of the tumor invasion.…”

“…Studies have revealed that almost all patients treated with imiquimod exhibit some degree of local inflammation at the application site. In FDA studies, patients presented some degree of erythema, edema, ulceration or erosion (Burns & Brown, 2005). The formulation of 3% diclofenac gel has been used for the topical treatment of actinic keratosis.…”

Development of TLR9 agonists for cancer therapy

“…Consistent with the hypothesis that TLRs are an important component of immune defenses, mice deficient for TLR4 have an increased susceptibility to infection with Gram-negative bacteria (2,3). A synthetic agonist for TLR4, monophosphoryl lipid A, has been developed as a vaccine adjuvant (4), and a synthetic agonist for TLR7, imiquimod, has been developed in a topical formulation approved by the FDA for treatment of genital warts, actinic keratosis, and basal cell carcinoma, but it is also widely used in other conditions (5). This Review focuses on TLR9, which is the only TLR for which a systemically administered specific agonist has shown substantial evidence of antitumor activity in human clinical trials.…”

Cancer and the microbiome: potential applications as new tumor biomarker

“…PF-3512676 has been also tested in advanced renal cell carcinoma [115] and advanced cutaneous T cell lymphoma [116]. Imiquimod is a TLR7 agonist that seems to have some activity when it is used topically for the treatment of several premalignant and malignant skin diseases [117], but it is not effective when given by systemic injection, despite some encouraging results obtained in mouse models [118]. These new agents are currently being used in conjunction with other treatments to enhance the anti-tumor immune response.…”