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

Sep 24, 2026

Actinic keratosis (AK) is a common precancerous skin lesion arising in chronically sun-exposed areas, driven by UV-induced mutations in tumor-suppressor and oncogenic pathways that lead to atypical keratinocyte proliferation. Without treatment, AK can progress to cutaneous squamous cell carcinoma (cSCC), requiring excision or systemic immunotherapy for advanced disease. The review highlights approved physical and topical AK treatments and focuses on tirbanibulin 1% ointment. Its mechanism targets cell proliferation via SRC-kinase inhibition, offering a practical 5-day regimen with mainly mild local reactions, improving adherence.

LanguageEnglish

CategoryHealthcare

FormatPDF

Pages9

Reading Time23 min

AccessFree to download

Abstract

Introduction

Epidemiology and Clinical Presentation

Histopathology and Pathogenesis

Treatment Options and Adherence Challenges

Mechanism and Clinical Evidence for Tirbanibulin

Topical Pharmacological Treatment of Actinic Keratoses: Focus on Tirbanibulin 1% Ointment Mario Valenti1,2, Matteo Bianco1,2, Alessandra Narcisi1,2, Antonio Costanzo1,2, Riccardo Borroni1,2, Marco Ardigò1,2 1 Department of Biomedical Sciences, Humanitas University, Pieve Emanuele, Italy 2 Dermatology Unit, IRCCS Humanitas Research Hospital, Rozzano, Italy Key words: tirbanibulin, actinic keratoses, field of cancerization, local adverse events Citation: Valenti M, Bianco M, Narcisi A, Costanzo A, Borroni RG, Ardigò M. Topical Pharmacological Treatment of Actinic Keratoses: Focus on Tirbanibulin 1% Ointment. Dermatol Pract Concept. 2024;14(3)S1:e2024145S. DOI: [https://doi.org/10.5826/dpc.1403S1a145S](https://doi.org/10.5826/dpc.1403S1a145S)[ ](https://doi.org/10.5826/dpc.1403S1a145S)[Accepted:](Accepted: April 22)[ April 22](Accepted: April 22), [2024](2024); Published: July 2024 Copyright: ©2024 Valenti et al. This is an open-access article distributed under the terms of the Creative Commons AttributionNonCommercial License (BY-NC-4.0), [https://creativecommons.org/licenses/by-nc/4.0/](https://creativecommons.org/licenses/by-nc/4.0/), which permits unrestricted noncommercial use, distribution, and reproduction in any medium, provided the original authors and source are credited. Funding: None. Competing Interests: None. Authorship: All authors have contributed significantly to this publication. Corresponding Author: Mario Valenti, MD, Department of Biomedical Sciences, Humanitas University, Pieve Emanuele; Dermatology Unit, IRCCS Humanitas Research Hospital, Rozzano, [Italy. Email: mario.valenti@hunimed.eu](Italy. Email: mario.valenti@hunimed.eu) ABSTRACT Actinic keratosis (AK) is a frequent precancerous skin lesion that mostly affects chronically sunexposed 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. Review | Dermatol Pract Concept. 2024;14(3)S1:e2024145S 1 Introduction Actinic keratoses (or solar keratoses) are the clinical manifestation of a common, chronic disease of the skin of adults [1], which develops in areas exposed to sunlight [2] . Risk factors for the development of actinic keratoses and SCCare I-II phototypes according to Fitzpatrick’s scale, male sex, age, and immunodepression [3-5] . The incidence of AKs is likely underestimated, as they are not recorded routinely in cancer registries. Unsurprisingly, the prevalence of AKs shows

FAQs

What is actinic keratosis and why is it important to treat it?

Actinic keratosis is a frequent precancerous skin lesion in chronically sun-exposed areas. Untreated AK may evolve into cutaneous squamous cell carcinoma (cSCC), increasing the need for more invasive or systemic treatment.

What causes actinic keratosis at the biological level?

Chronic sun damage produces UV-induced mutations in key genes, including tumor-suppressor TP53, which promote uncontrolled proliferation of atypical keratinocytes. AKs share histopathological similarities with squamous cell carcinoma due to common multi-stage pathogenesis.

How does tirbanibulin 1% ointment fit into AK treatment and what is its practical regimen?

The review describes tirbanibulin-based ointment as inhibiting cell proliferation and blocking SRC-kinases implicated in AK progression toward SCC. The key advantage is practical posology: once-daily application for 5 consecutive days on AKs of the face-scalp area, with usually mild local skin reactions that do not require discontinuation.

Sep 24, 2026

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