School of Medicine, Baylor College of Medicine, Houston, TX, USA.
Department of Dermatology, Perelman School of Medicine at the University of Pennsylvania, Philadelphia, PA, USA.
Expert Opin Emerg Drugs. 2021 Dec;26(4):433-434. doi: 10.1080/14728214.2021.2004694. Epub 2021 Nov 15.
Resiquimod is a Toll-like receptor (TLR)-7 and TLR-8 agonist that, like imiquimod, belongs to the class of imidazoquinolines, small organic molecules with potent antiviral and anticancer activity. Resiquimod activates myeloid and plasmacytoid dendritic cells while also promoting release of cytokines as interleukin-6, tumor necrosis factor-α and interferon-γ more effectively than imiquimod. Given these immunologic effects, resiquimod is emerging as a new topical pharmacotherapy for actinic keratosis (AK). In the pivotal trial by Stockfleth et al. complete clinical clearance in all the resiquimod-treated arms was more significant than placebo varying from 56% to 74%. Partial clinical clearance, or disappearance of >75% of AKs, was also significantly higher in the resiquimod arms varying from 75% to 87%. Overall, resiquimod is a new molecule that remains a promising therapy for AK, although additional studies are needed to further evaluate its efficacy.
瑞喹莫德是 Toll 样受体(TLR)-7 和 TLR-8 的激动剂,与咪喹莫特一样,属于咪唑并喹啉类,是一类具有强大抗病毒和抗癌活性的小分子有机化合物。瑞喹莫德激活髓样和浆细胞样树突状细胞,同时比咪喹莫特更有效地促进白细胞介素 6、肿瘤坏死因子-α 和干扰素-γ 的释放。鉴于这些免疫效应,瑞喹莫德作为一种新的光化性角化病(AK)局部治疗药物正在出现。在 Stockfleth 等人的关键试验中,所有瑞喹莫德治疗组的完全临床清除率均明显高于安慰剂组,从 56%到 74%不等。瑞喹莫德组的部分临床清除率(或 AK 消失>75%)也明显更高,从 75%到 87%不等。总体而言,瑞喹莫德是一种新的分子,仍然是 AK 有前途的治疗药物,尽管需要进一步的研究来进一步评估其疗效。