Tirbanibulin for Actinic Keratosis: Insights into the Mechanism of Action

Actinic keratosis (AK) is a common pre-neoplastic skin lesion constituted by uncontrolled proliferation of atypical keratinocytes that may evolve to squamous cell carcinoma. With global prevalence increasing, AK is expected to be the most common carcinoma of the skin. Tirbanibulin is a reversible tu...

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Bibliographic Details
Published inClinical, cosmetic and investigational dermatology Vol. 15; pp. 2495 - 2506
Main Authors Schlesinger, Todd, Stockfleth, Eggert, Grada, Ayman, Berman, Brian
Format Journal Article
LanguageEnglish
Published Auckland Dove Medical Press Limited 01.01.2022
Taylor & Francis Ltd
Dove
Dove Medical Press
Subjects
Actinic keratosis
Apoptosis
Cancer
Cancer therapies
Care and treatment
Cell cycle
Cell division
Cell growth
Drug resistance
Gene expression
Immune system
Kinases
Medical research
Medicine, Experimental
microtubules
Mutation
Nonsteroidal anti-inflammatory drugs
Patient compliance
Polymerization
Review
Skin
Squamous cell carcinoma
src kinase inhibitor
tirbanibulin
Tubulins
Vincristine
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Summary:Actinic keratosis (AK) is a common pre-neoplastic skin lesion constituted by uncontrolled proliferation of atypical keratinocytes that may evolve to squamous cell carcinoma. With global prevalence increasing, AK is expected to be the most common carcinoma of the skin. Tirbanibulin is a reversible tubulin polymerization inhibitor with potent anti- proliferative and anti-tumoral effects. In-vivo and in-vitro studies have shown that tirbanibulin significantly inhibits cell proliferation, tumor growth and down-regulates Src signaling with no overt toxicity. Early phase and Phase III trials have shown high lesion clearance, compliance, and few side effects of once daily tirbanibulin treatment. This review discusses tirbanibulin anti-cancer activity, focusing on tubulin polymerization and Src signaling inhibitory effects, highlighting relevant literature and novel preclinical results from the ATNXUS- KX01 -001 study. Furthermore, we address the relevant findings obtained in recent clinical trials to evaluate the safety, efficacy, pharmacokinetics, clearance efficacy, and side effects of the 1% tirbanibulin ointment applied once daily. In summary, we highlight preclinical and clinical evidence on the use of tirbanibulin as an effective and safe treatment option for AK. Keywords: actinic keratosis, tirbanibulin, microtubules, Src kinase inhibitor
Bibliography:ObjectType-Article-2
SourceType-Scholarly Journals-1
ObjectType-Feature-3
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ObjectType-Review-1
ISSN:1178-7015
1178-7015
DOI:10.2147/CCID.S374122