Actinic keratosis (AK), a skin condition characterized by the proliferation of atypical keratinocytes, can progress to squamous cell carcinoma. Existing treatments are effective but cause high rates of local skin reactions. Tirbanibulin, one of the treatments under development for AK, is a novel synthetic drug with powerful in vitro and in vivo antiproliferative and antitumor effects. Its efficacy in this setting was recently demonstrated in 2 phase 3 clinical trials. We review tirbanibulin’s mechanism of action based on the current literature and several unpublished preclinical studies. We also review treatments available for AK and discuss how tirbanibulin, with its novel mechanism of action, fits into the therapeutic landscape.
