tirbanibulin
Regulatory sources consulted
Approved indications
- Treatment in adults of nonhyperkeratotic, nonhypertrophic Olsen grade 1 actinic keratosis on the face or scalp.
Contraindications
Absolute
- Hypersensitivity to tirbanibulin or any excipient.
Clinical warnings
- Avoid the eyes, lips, inside the nose or ears, ingestion, and open, lacerated, or unhealed skin. Local reactions may require assessment. — CIMA/AEMPS, ficha técnica 1211558001
- Major warning · Minimize ultraviolet exposure. Assess use individually in immunosuppression. Reassess lesions suspicious for progression to squamous cell carcinoma. — CIMA/AEMPS, ficha técnica 1211558001
Adverse events
Common (≥1%)
Local erythema, flaking, crusting, swelling, or erosion · Local vesicles, itching, or pain
Pregnancy and lactation
Do not use during pregnancy or in women of childbearing potential not using contraception. During breastfeeding, decide whether to stop breastfeeding or stop treatment.
Recent literature (PubMed)
We review here the pharmacology, pharmacokinetics, efficacy, dosage and administration, and place in therapy of tirbanibulin for the treatment of actinic keratosis (AK). A literature search using PubMed was conducted using the terms tirbanibulin (tirbanibulin) and actinic keratosis from September 2014 to February 2021. All English-language articles evaluating tirbanibulin were analyzed for this review. Tirbanibulin was granted approval for the treatment of AK of the face or scalp as a first-line therapy. It is administered at a dose of 2.5 mg in 250 mg of white or off-white ointment for a 25 cm2 contiguous treatment surface for 5 consecutive days. Adverse effects include flaking/scaling, crusting, swelling, vesiculation/pustulation, and erosion/ulceration. This article discusses the clinical trials that led to the approval of tirbanibulin and comparison with other approved topical ointments indicated for the treatment of AK. In the clinical trials, all participants experienced a decrease in lesion size or saw complete clearance with minimal adverse effects.
Cutaneous field cancerization in dermatology describes the anatomic region of photodamaged skin with actinic keratoses (AKs) or cutaneous squamous cell carcinoma (cSCC) that is surrounded by cellular atypia, forming a dysplastic field. The concept of field cancerization is especially relevant in dermatology, as actinic keratoses and the surrounding dysplastic region can progress to carcinomas, necessitating the treatment of the field. Recent research has focused on field-directed therapy using topical agents. This study aims to systematically review randomized controlled trials on topical treatments for actinic keratosis field cancerization, following the PRISMA guidelines. Clinical recommendations were based on the Oxford Centre for Evidence-Based Medicine. We identified 20 original randomized controlled trials for topical cutaneous field therapy. 0.5% 5-Fluorouracil/salicylic acid and 0.5% 5-fluorouracil received a clinical recommendation grade of A, while diclofenac sodium received a clinical recommendation grade of B. Calcipotriol/5-fluorouracil, Imiquimod, sunscreen combination therapies, and tirbanibulin received a recommendation grade of C. This review provides a framework for clinicians when considering topical treatments for patients with field cancerization.
Tirbanibulin is a topical medication approved in 2020 as a 5 day topical treatment for actinic keratosis, a precancerous skin lesion characterized by the hyperproliferation of atypical keratinocytes. Tirbanibulin exerts its effects through dual mechanisms: microtubule inhibition, which disrupts cell division, and Src kinase inhibition, which interferes with cancer-associated signaling pathways. Although its primary use is in AK, these mechanisms suggested potential therapeutic applications in a broader range of epithelial cancers. In this literature review, we explored tirbanibulin's application in not only actinic keratosis, but also in squamous cell carcinoma and basal cell carcinoma. We addressed the relevant findings obtained in recent papers to evaluate tirbanibulin's safety, efficacy, side effects, real-life clinical experiences, and its potential in anti-aging and skin lightening therapies on patients. In summary, we highlighted the preclinical and clinical evidence on the use of tirbanibulin as an effective and safe treatment option beyond AK. Graphical Abstract.
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 downregulates 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.