Gilaberte Y, Fernández-Figueras M T
Servicio de Dermatología, Hospital Universitario Miguel Servet, IIS Aragón, Zaragoza, España.
Servicio de Anatomía Patológica, Hospital Universitari General de Catalunya, Grupo Quirón Salud, Sant Cugat del Vallès, Barcelona, España; Universitat Internacional de Catalunya, Sant Cugat del Vallès, Barcelona, España.
Actas Dermosifiliogr. 2022 Jan;113(1):58-66. doi: 10.1016/j.ad.2021.07.006. Epub 2021 Aug 2.
Actinic keratosis (AK) is a skin condition characterized by the proliferation of mutated keratinocytes that can develop into squamous cell carcinoma. Available therapies, although effective, are associated with a high frequency of severe local skin reactions. Tirbanibulin, one of the treatments for AK currently in development, is a new synthetic chemical entity with anti-proliferative and anti-tumor effects, both in vitro and in vivo, with proved efficacy in the treatment of AK, which has been recently demonstrated in two phase III clinical trials. In the present review, the tirbanibulin mechanism of action, based on the relevant literature and the results of several unpublished preclinical studies, is shown. In addition, the current scenario regarding the available treatments and how the novel tirbanibulin mechanism of action fits into the treatment of AK is raised.
光化性角化病(AK)是一种以突变角质形成细胞增殖为特征的皮肤疾病,这些细胞可发展为鳞状细胞癌。现有的治疗方法虽然有效,但会频繁引发严重的局部皮肤反应。替巴替尼是目前正在研发的AK治疗药物之一,它是一种新型合成化学实体,在体外和体内均具有抗增殖和抗肿瘤作用,已在两项III期临床试验中证明其对AK治疗有效。在本综述中,基于相关文献和多项未发表的临床前研究结果,阐述了替巴替尼的作用机制。此外,还提出了现有治疗方法的现状以及新型替巴替尼作用机制如何适用于AK治疗的问题。