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Skin Therapy Lett. 2022 Jul;27(4):4-7.

光化性角化病的局部药物治疗:聚焦于1%替拉替林软膏

Topical Pharmacological Treatment of Actinic Keratoses: Focus on Tirbanibulin 1% Ointment.

作者信息

Valenti Mario, Bianco Matteo, Narcisi Alessandra, Costanzo Antonio, Borroni Riccardo, Ardigò Marco

机构信息

Department of Biomedical Sciences, Humanitas University, Pieve Emanuele, Italy.

Dermatology Unit, IRCCS Humanitas Research Hospital, Rozzano, Italy.

出版信息

Dermatol Pract Concept. 2024 Jul 1;14(3 S1):e2024145S. doi: 10.5826/dpc.1403S1a145S.

DOI:10.5826/dpc.1403S1a145S
PMID:39133636
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11566729/
Abstract

Actinic keratosis (AK) is a frequent precancerous skin lesion that mostly affects chronically sun-exposed areas. Chronic sun damage leads to various mutations in onco-suppressor and oncogenic genes which cause an uncontrolled proliferation of atypical keratinocytes. Untreated AKs may evolve in cutaneous squamous cell carcinoma (cSCC), with the consequent need for dermato-surgical excision or even for systemic immunotherapy in case of invasive/metastatic cSCCs. Epidemiology data on AK prevalence are various, however, the literature unanimously reports an increasing prevalence due to the aging of the population. Clinically AKs appear as a scaly, erythematous macule or papule or hyperkeratotic plaque. Management of AKs and the field of cancerization is important to avoid the natural evolution into squamous cell carcinomas (SCCs). Both physical and topical treatments are approved for managing AKs. Patient compliance with topical regimens is usually low due to the length of the posology and frequent skin adverse events. A recently approved tirbanibulin-based ointment, showed potential for inhibiting cell proliferation and blocking SRC-kinases, implicated in the progression of AKs in SCCs. The advantage of this new treatment is the practical posology, with a daily application for 5 consecutive days on AKs of the face-scalp area. Local skin reactions are usually mild and do not require treatment discontinuation. The short course of this new therapy and its excellent tolerance massively increased patient compliance. This article reviews what is currently known about this new therapy from its mechanism of action to clinical trial outcomes regarding safety, effectiveness, and patient adherence to the treatment.

摘要

光化性角化病(AK)是一种常见的癌前皮肤病变,主要影响长期暴露于阳光下的区域。长期的阳光损伤会导致抑癌基因和致癌基因发生各种突变,从而引起非典型角质形成细胞的不受控制的增殖。未经治疗的AK可能会演变成皮肤鳞状细胞癌(cSCC),因此对于侵袭性/转移性cSCC可能需要进行皮肤外科切除甚至全身免疫治疗。关于AK患病率的流行病学数据各不相同,然而,文献一致报道由于人口老龄化患病率在上升。临床上,AK表现为鳞屑性、红斑性斑疹或丘疹或角化过度斑块。对AK和癌化区域的管理对于避免其自然演变成鳞状细胞癌(SCC)很重要。物理治疗和局部治疗都被批准用于管理AK。由于用药疗程长且皮肤不良事件频繁,患者对局部治疗方案的依从性通常较低。一种最近批准的基于替巴尼布林的软膏,显示出抑制细胞增殖和阻断SRC激酶的潜力,这些激酶与AK向SCC的进展有关。这种新治疗方法的优点是用药方案简便,在面部 - 头皮区域的AK上连续5天每日应用。局部皮肤反应通常较轻,不需要中断治疗。这种新疗法的短疗程及其良好的耐受性大大提高了患者的依从性。本文综述了目前关于这种新疗法的已知信息,从其作用机制到关于安全性、有效性和患者对治疗的依从性的临床试验结果。