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. 2022 Oct;15(10 Suppl 1):S3-S10.

Profile of Tirbanibulin for the Treatment of Actinic Keratosis

Brian Berman  1 , Ayman Grada  2 , Daniela K Berman  3
Affiliations

Profile of Tirbanibulin for the Treatment of Actinic Keratosis

Brian Berman et al. J Clin Aesthet Dermatol. 2022 Oct.

Abstract

Actinic keratosis (AK) is a chronic disease resulting from deleterious effects of long-term, cumulative, epidermal exposure to ultraviolet (UV) light. UV-induced mutations in p53, ras, and p16 genes lead to the emergence of abnormal epidermal actinic keratosis (AKs) cells, which proliferate while avoiding apoptosis and may lead to invasive squamous cell carcinoma. There are both lesion-targeted and field-directed topical treatments. This review is of new and emerging information on tirbanibulin and tirbanibulin 1% ointment, which is approved for topical field treatment of actinic keratosis on the face and scalp. Potent antiproliferative and proapoptotic activities result from tirbanibulin's inhibition tubulin polymerization and disruption of microtubule formation and Src kinase signaling. Tirbanibulin 1% ointment is an effective treatment of facial and scalp AK after five consecutive once-daily applications, as measured by complete and partial clearance and percent reduction in the number of lesions. Localized skin reactions are usually mild to moderate, resolving within a month. The short and well-tolerated course of therapy results in very high patient adherence to the treatment regimen.

Keywords: Tirbanibulin ointment; actinic keratosis; field therapy.

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Conflict of interest statement

FINANCIAL DISCLOSURES: Dr. B. Berman is an advisory board member, investigator, consultant, and/or speaker for Biofrontera, SUN Pharmaceuticals, Inc., LEO Pharma, and Almirall LLC. Dr. Grada is a former Almirall LLC employee. Ms. D. Berman has no conflicts of interest relevant to the content of this article.

Figures

FIGURE 1.
FIGURE 1.
Molecular structure of tirbanibulin
FIGURE 2.
FIGURE 2.
Mechanism of action of tirbanibulin (T),
FIGURE 3.
FIGURE 3.
Percent of patients with complete clearance of actinic keratosis (AK) lesions after treatment with tirbanibulin 1% ointment vs. vehicle control treatment, once daily for 5 days—Data are from the intent-to treat population and included both face and scalp treatment areas. Patients who discontinued before the Day 57 assessment were considered treatment failures. Significance determined by Cochran-Mantel-Haenszel method stratified by treatment group. D: difference between treatment groups; n/N: number of patients with 100% clearance/total number of patients
FIGURE 4.
FIGURE 4.
Percent of patients with at least 75% clearance of actinic keratosis (AK) lesions after treatment with tirbanibulin 1% ointment vs. vehicle control treatment once daily for 5 days—Data are from the intent-to treat population and included both face and scalp treatment areas. Patients who discontinued before the Day 57 assessment were considered treatment failures. Significance determined by Cochran-Mantel-Haenszel method stratified by treatment group. D: difference between treatment groups; n/N: number of patients with ≥75% clearance/total number of patients
FIGURE 5.
FIGURE 5.
Composite local skin reaction (LSR) scores to tirbanibulin 1% ointment once-daily treatment (Days 1–5) over time; composite score is the sum of all six LSR grades with a possible range of 0–18.; pooled results from 2 Phase III studies
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References

    1. Uhlenhake EE. Optimal treatment of actinic keratoses. Clin Interv Aging. 2013;8:29. - PMC - PubMed
    1. Drake LA, Ceilley RI, Cornelison RL et al. Guidelines of care for actinic keratoses. J Am Acad Dermatol. 1995;32(1):95–98. - PubMed
    1. https://www.lewin.com/content/dam/Lewin/Resources/Site_Sections/Publicat... Society for Investigative Dermatology, American Academy of Dermatology Association. The burden of skin diseases, 2005. Accessed 2 Feb 2022. - PubMed
    1. Cockerell CJ, Wharton JR. New histopathological classification of actinic keratosis (incipient intraepidermal squamous cell carcinoma). J Drug Dermatol. 2005;4(4):462–467. - PubMed
    1. Berman B, Bienstock L, Kuritzky L et al. Actinic keratosis: sequelae and treatments: recommendations from a consensus panel. J Fam Pract. 2006;55(5):S1–S1. - PubMed

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