Safety and efficacy of imiquimod 5% cream in the treatment of penile genital warts in uncircumcised men when applied three times weekly or once per day

Gollnick, Harald; Barasso, R; Jappe, Uta; Ward, Kristen M.; Eul, A.; Carey-Yard, M; Milde, K.

doi:10.1177/095646240101200105

Cited by 67 publications

(58 citation statements)

References 15 publications

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“…Lower clearance rates in men have been linked to greater keratinization of the skin along the penile shaft, affecting drug penetration. 22 A case study demonstrating progressive resolution and clearance of vulvar condyloma after topical therapy with Polyphenon E 15% ointment appear in Figure 4. Table 4 lists the properties, activity, and side effects associated with green tea catechins and the 2 other patient-administered topical agents approved by the FDA for treatment of anogenital warts: podofilox and imiquimod.…”

Section: Wwwajogorgmentioning

confidence: 99%

Green tea catechins for treatment of external genital warts

Meltzer

Monk

Tewari

2009

American Journal of Obstetrics and Gynecology

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This review evaluates the antiviral, antioxidant, and immunostimulatory properties of green tea catechins. Two randomized trials evaluating the activity and efficacy of green tea catechins in the management of external genital warts are presented, and the reported side effects associated with this topical treatment modality are outlined. Finally, the mechanism of action, percent of wart clearance, time to clearance, and toxicity profile of green tea catechins are compared with those of podofilox and imiquimod, 2 other patient-administered topical agents approved for treatment of anogenital warts.

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Section: Wwwajogorgmentioning

confidence: 99%

Green tea catechins for treatment of external genital warts

Meltzer

Monk

Tewari

2009

American Journal of Obstetrics and Gynecology

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“…The small size of imiquimod, its hydrophobicity and ability to penetrate the epidermal barrier on the one hand, and, on the other hand, considerable unwanted side effects when the compound is applied systemically, led to the development of a topical formulation (Aldara 5% cream) for the treatment of viral lesions (HPV papillomas) and malignant tumors of the skin. Imiquimod was first approved for the treatment of genital warts and is usually well tolerated (Gollnick et al, 2001). In addition, several controlled clinical trials as well as many smaller series of cases and case reports have demonstrated that imiquimod is also effective against a variety of primary skin cancers as well as cutaneous metastases of some malignancies.…”

Section: Antitumoral Efficacy Of Tlr7/8 Agonists In Clinical Trialsmentioning

confidence: 99%

TLR7 and TLR8 as targets in cancer therapy

2008

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Small-molecule agonists at Toll-like receptor 7 (TLR7) and TLR8 have sparked a vivid interest in cancer research owing to their profound antitumoral activity. The lead compound of the imidazoquinoline family, imiquimod, is marketed as a topical formulation. It is efficacious against many primary skin tumors and cutaneous metastases. Using different imidazoquinoline species, distinct functions of TLR7 and TLR8 have been discovered. The predominant antitumoral mode of action of these agents is TLR7/ 8-mediated activation of the central transcription factor nuclear factor-jB, which leads to induction of proinflammatory cytokines and other mediators. Cutaneous dendritic cells are the primary responsive cell type and initiate a strong Th1-weighted antitumoral cellular immune response. Recent research has shown that dendritic cells themselves acquire direct antitumoral activity upon stimulation by imiquimod. In addition, there are a number of secondary effects on the molecular and cellular level that can be explained through the activation of TLR7/8. The proinflammatory activity of imiquimod, but not resiquimod, appears to be augmented by suppression of a regulatory mechanism, which normally limits inflammatory responses. This is achieved independently of TLR7/8 through interference with adenosine receptor signaling pathways. Finally, at higher concentrations imiquimod exerts Bcl-2-and caspase-dependent proapoptotic activity against tumor cells.

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“…In addition, it has been reported that there are adverse side effects resulting from the treatments. Patients most frequently complained of itch and to a lesser extent of a burning sensation, but rarely of pain (19)(20)(21)(22).…”

mentioning

confidence: 99%

Analysis of cellular and behavioral responses to imiquimod reveals a unique itch pathway in transient receptor potential vanilloid 1 (TRPV1)-expressing neurons

Kim

Park

Kim

et al. 2011

Proc. Natl. Acad. Sci. U.S.A.

102

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Despite its clinical importance, the mechanisms that mediate or generate itch are poorly defined. The identification of pruritic compounds offers insight into understanding the molecular and cellular basis of itch. Imiquimod (IQ) is an agonist of Toll-like receptor 7 (TLR7) used to treat various infectious skin diseases such as genital warts, keratosis, and basal cell carcinoma. Itch is reportedly one of the major side effects developed during IQ treatments. We found that IQ acts as a potent itch-evoking compound (pruritogen) in mice via direct excitation of sensory neurons. Combined studies of scratching behavior, patch-clamp recording, and Ca 2+ response revealed the existence of a unique intracellular mechanism, which is independent of TLR7 as well as different from the mechanisms exploited by other well-characterized pruritogens. Nevertheless, as for other pruritogens, IQ requires the presence of transient receptor potential vanilloid 1 (TRPV1)-expressing neurons for itchassociated responses. Our data provide evidence supporting the hypothesis that there is a specific subset of TRPV1-expressing neurons that is equipped with diverse intracellular mechanisms that respond to histamine, chloroquine, and IQ.

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Safety and efficacy of imiquimod 5% cream in the treatment of penile genital warts in uncircumcised men when applied three times weekly or once per day

Cited by 67 publications

References 15 publications

Green tea catechins for treatment of external genital warts

Green tea catechins for treatment of external genital warts

TLR7 and TLR8 as targets in cancer therapy

Analysis of cellular and behavioral responses to imiquimod reveals a unique itch pathway in transient receptor potential vanilloid 1 (TRPV1)-expressing neurons

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