tirbanibulin oral (KX-01 oral) / Athenex - LARVOL DELTA

Non-surgical therapies for localized non-melanoma skin cancer in older adults: A review. (PubMed, J Geriatr Oncol) - "Specifically, topical agents such as 5-fluorouracil, imiquimod, tirbanibulin, retinoids, and trichloroacetic acid offer effective, less-invasive options for superficial lesions but rely heavily on adherence, which may be compromised in cognitively impaired or functionally-limited individuals. Intralesional therapies (including 5-fluorouracil and methotrexate), on the other hand, provide high clearance rates with minimal systemic toxicity, while also reducing patient responsibility and daily application...Furthermore, this review emphasizes that across all modalities, NST selection must prioritize geriatric principles, balancing efficacy with safety, comfort, functional status, cognitive capacity, support systems, and patient preferences. As the aging population grows and NMSC numbers expand in parallel, individualized, patient-centered care and expanded older adult-focused research are essential to optimizing treatment outcomes for older adults."

Journal • Review • Alzheimer's Disease • Basal Cell Carcinoma • Cognitive Disorders • Dermatology • Genetic Disorders • Non-melanoma Skin Cancer • Skin Cancer • Solid Tumor • Squamous Cell Carcinoma

Fractional CO2 laser as a priming strategy for tirbanibulin in actinic keratoses – a prospective intra-individual comparative study (ADO 2026) - No abstract available

Clinical • Actinic Keratosis • Dermatology

Efficacy and tolerability of topically applied tirbanibulin on actinic keratoses with downward-directed proliferation patterns (EADV 2026) - No abstract available

Clinical • Actinic Keratosis • Dermatology

Tirbanibulin 1% for cutaneous eyelid actinic keratosis: a consecutive five-case series with periocular protection (EADV 2026) - No abstract available

Clinical • Actinic Keratosis • Dermatology

4% 5-Fluorouracil Cream for Actinic Keratoses: First Report of Efficacy and Tolerability in a Person Living With Human Immunodeficiency Virus Infection. (PubMed, Clin Case Rep) - "The patient had previously undergone several treatments, including cryotherapy, diclofenac gel, and tirbanibulin, with only temporary improvement. Given the increased oncologic risk in immunocompromised patients, timely and effective treatment of AK is essential. Nevertheless, the limited evidence available in this specific population underscores the need for further prospective studies to better define management strategies and long-term outcomes."

Journal • Actinic Keratosis • Dermatology • Human Immunodeficiency Virus • Infectious Disease • Oncology • Pruritus • Skin Cancer • Squamous Cell Carcinoma • Squamous Cell Skin Cancer

Fractional CO2 laser as a priming strategy for tirbanibulin in actinic keratoses – a prospective intra-individual comparative study (ADO 2026) - No abstract available

Clinical • Actinic Keratosis • Dermatology

Clinical Clearance of Actinic Keratoses with Tirbanibulin 1% Ointment: Evidence from a Meta-Analysis. (PubMed, Life (Basel)) - "This led to an overall pooled PC rate of 71.96% (95% CI: 64.89-78.09%). In conclusion, tirbanibulin 1% ointment has shown clinical effectiveness and should be considered a promising treatment for AKs."

Journal • Retrospective data • Actinic Keratosis • Dermatology • Oncology • Squamous Cell Carcinoma • Squamous Cell Skin Cancer

Predictors of outcomes and satisfaction with tirbanibulin in actinic keratosis: a multicenter real-world study. (PubMed, Ital J Dermatol Venerol) - "Tirbanibulin 1% achieved high clearance with favorable tolerability and satisfaction, supporting its use in individualized management of field cancerization."

Biomarker • Journal • Real-world evidence • Actinic Keratosis • Dermatology • Oncology

Repurposing tirbanibulin as an orally active E2-targeting entry inhibitor against Chikungunya virus. (PubMed, Br J Pharmacol) - "Tirbanibulin is a novel, orally bioavailable entry-stage inhibitor that directly targets the E2 glycoprotein. Multiple preclinical and clinical studies have confirmed its favourable oral bioavailability and safety. Given its established clinical safety profile, it represents a promising repurposing candidate for clinical evaluation against Chikungunya fever."

Journal • Chikungunya • Immunology • Infectious Disease • Rheumatology

Potential role of tirbanibulin in the management of superficial basal cell carcinoma. (PubMed, J Eur Acad Dermatol Venereol) - No abstract available

Journal • Basal Cell Carcinoma • Non-melanoma Skin Cancer • Oncology

Berbamine improves behavioral impairments in Huntington's disease mice models through inhibiting Src/AKT1/NFκB signaling pathway and attenuating Src-mediated mitophagy suppression. (PubMed, Int Immunopharmacol) - "BBM ameliorates motor and cognitive impairments in HD model mice through inhibition of neuroinflammation and mHTT expression, maintenance of mitochondrial function, which was mediated by inhibiting Src/AKT1/NFκB signaling pathway and attenuating Src-mediated mitophagy suppression."

Journal • Preclinical • Alzheimer's Disease • CNS Disorders • Cognitive Disorders • Huntington's Disease • Inflammation • Movement Disorders • AKT1 • NLRP3 • PINK1

A single-center prospective observational study evaluating the efficacy and safety of tirbanibulin 1% in actinic keratoses in immunosuppressed patients: the ESTIMATE study. (PubMed, J Dtsch Dermatol Ges) - "This study demonstrates that tirbanibulin is a safe, well-tolerated, and effective option for AK management in OTRs, addressing a critical need in this high-risk population."

Journal • Observational data • Actinic Keratosis • Dermatology • Oncology • Squamous Cell Carcinoma • Transplantation

Sequential Keratolytic Pre-Treatment Followed by Tirbanibulin in Hyperkeratotic Actinic Keratoses: A Retrospective Comparative Study. (PubMed, Pharmaceuticals (Basel)) - "Tirbanibulin 1% ointment is an effective short-course field therapy for AK, but its efficacy in hyperkeratotic lesions (Olsen grade II-III) may be limited by reduced drug penetration through a thickened stratum corneum. This retrospective study suggests that keratolytic pretreatment may represent a useful adjunctive strategy in hyperkeratotic AK treated with tirbanibulin. Prospective randomized studies are warranted to confirm these findings and to define standardized treatment protocols."

Journal • Retrospective data • Actinic Keratosis • Dermatology • Non-melanoma Skin Cancer • Oncology • Skin Cancer • Squamous Cell Carcinoma • Squamous Cell Skin Cancer

Sequential Field Therapy in Actinic Keratosis: A Mechanism-Based Rationale for Complementary Treatment Strategies. (PubMed, J Clin Med) - " This narrative review summarizes the rationale, mechanisms of action, efficacy profile, tolerability, and practical limitations of currently available field-directed therapies for actinic keratosis, including 5-fluorouracil, imiquimod, diclofenac, photodynamic therapy, and tirbanibulin. Mechanism-based sequential field therapy may represent a rational strategy to optimize long-term control of actinic keratosis and field cancerization. Prospective comparative studies are needed to define optimal sequences, treatment intervals, patient selection criteria, and clinically meaningful endpoints, including sustained field clearance, recurrence reduction, tolerability, adherence, and prevention of progression to invasive cutaneous squamous cell carcinoma."

Journal • Review • Actinic Keratosis • Dermatology • Oncology • Squamous Cell Carcinoma • Squamous Cell Skin Cancer

Comprehensive multi-omics analysis identifies cancer subtypes and prognostic signatures of hepatitis B virus-associated hepatocellular carcinoma. (PubMed, NPJ Precis Oncol) - "In vitro assays confirmed that KX2-391 dose-dependently induces apoptosis in high-MLPS HBV-HCC cell lines, and in vivo xenograft models demonstrated its superior efficacy in inhibiting tumor growth compared to lenvatinib, without significant organ toxicity. Mechanistically, we discovered that F9 acts as a tumor suppressor by interacting with SERPINC1 to inhibit the Wnt/β-catenin signaling pathway. Collectively, our study provides a novel HBV-HCC classification system, a high-performance prognostic tool, and identifies both KX2-391 and F9 as promising avenues for precision therapy."

Journal • Hepatitis B • Hepatocellular Cancer • Infectious Disease • Oncology • Solid Tumor

KXV01 Injection in Patients With Advanced Solid Tumor (Including Osteosarcoma and Sarcoma) (clinicaltrials.gov) - P1 | N=30 | Recruiting | Sponsor: TCRx Therapeutics Co.Ltd

New P1 trial • Oncology • Osteosarcoma • Sarcoma • Solid Tumor

Structure-based design and synthesis of KX-01 analogs as potent antitumor agents targeting the tubulin colchicine binding site. (PubMed, Eur J Med Chem) - "The cocrystal of 8h-tubulin complex revealed that it simultaneously occupies the colchicine site in β-tubulin and a cavity in α-tubulin. In the HT29 xenograft model, orally administered 8h (5 mg/kg, once daily) showed marginally superior in vivo antitumor efficacy than KX-01."

Journal • Oncology

Pigmented Actinic Keratoses on the Face: Dermoscopic Features and Therapeutic Response to Tirbanibulin — A Biopsy-Confirmed Case Series (EADO 2026) - "Tirbanibulin appears to be an effective and well-tolerated therapeutic option for biopsy-confirmed PAK, contributing to both clinical and dermoscopic improvement. Further prospective studies with larger cohorts are warranted to better define diagnostic criteria and long-term outcome."

Biopsy • Clinical • Actinic Keratosis • Basal Cell Carcinoma • Dermatology • Melanoma • Pruritus • Solid Tumor

Sequential keratolytic pretreatment enhances tirbanibulin efficacy in field cancerization assessed by line-field confocal optical coherence tomography: a pilot study (EADO 2026) - "Treatment consisted of topical 5% salicylic petrolatum for 2 weeks, followed by tirbanibulin 1% ointment once daily for 5 consecutive days on a maximum treatment area of 25 cm². This combination approach may enhance tirbanibulin effectiveness and potentially extend its applicability to higher-grade AK. Larger, controlled studies are warranted to confirm these findings and to define standardized LC-OCT–based response criteria."

Clinical • Actinic Keratosis • Oncology

Efficacy and safety of tirbanibulin 1% ointment in elderly patients with actinic keratosis: a pooled analysis of Phase 3 clinical trials (EADO 2026) - P3 | "LTS at Day 8 were consistent across groups, with mostly mild-to-moderate reactions; severe reactions were infrequent and similar: erythema (≥80 years: 9.3% vs <80 years: 7.4%), flaking/scaling (9.3% vs 7.2%), crusting (2.8% vs 1.7%), swelling (0.9% vs 0.4%), and vesiculation (0% vs 0.2%).Conclusions Tirbanibulin has shown efficacy and favorable safety/tolerability in very elderly patients. These outcomes support 5-day tirbanibulin treatment as a suitable field-directed therapy for AK in these high-risk patients."

P3 data • Retrospective data • Actinic Keratosis • Dermatology

Real-World Experience with Tirbanibulin 1% in Actinic Keratosis: Does Polypharmacy Influence Therapeutic Outcomes? (EADO 2026) - "Tirbanibulin 1% ointment, a tubulin polymerization inhibitor with Src signaling antagonism, demonstrates efficacy through cell cycle arrest and apoptosis induction. These findings support tirbanibulin use in elderly, polypharmacy populations with actinic keratosis, while recommending clinical awareness of potential increased local tolerability events. Regional variation in efficacy between facial and scalp lesions suggests skin thickness and drug penetration differences warrant further investigation."

Clinical • Real-world • Real-world evidence • Actinic Keratosis • Dermatology

Evaluation of long-term of therapeutic response in real-world clinical practice following tirbanibulin treatment. (EADO 2026) - "In this study, long-term effectiveness in real-world clinical practice was also evaluated, demonstrating sustained complete response rates exceeding 60%, compared with the 53% reported in the study by Brian Berman et al. Based on these findings, tirbanibulin is positioned as an effective and well-tolerated treatment with a convenient dosing regimen that improves patient adherence and provides favorable long-term outcomes."

Clinical • Real-world • Real-world evidence • Actinic Keratosis

Sustained real-world effectiveness of tirbanibulin 1% for actinic keratoses in solid organ transplant recipients (EADO 2026) - "This study aimed to evaluate real-world longitudinal effectiveness and safety of tirbanibulin 1% ointment in SOTR with AKs.Methods We conducted a retrospective observational study including SOTR with AKs treated with tirbanibulin 1% in standard 5-day cycles. Treatment was well tolerated, with no severe local skin reactions reported.Conclusions In SOTR with AKs, tirbanibulin 1% demonstrated sustained real-world effectiveness with a favorable safety profile over extended follow-up. Stability of ORR across time points supports its role as a well-tolerated option for repeated field therapy in this high-risk population requiring long-term management."

Clinical • Real-world • Real-world effectiveness • Real-world evidence • Actinic Keratosis • Dermatology • Solid Organ Transplantation • Squamous Cell Carcinoma • Squamous Cell Skin Cancer • Transplantation

Relationship between efficacy and cosmetic outcome in tirbanibulin-treated patients with actinic keratosis over a field up to 100 cm²: subanalysis from TirbAKare study (EADO 2026) - P3 | "This analysis aimed to evaluate the relationship between lesion clearance and cosmetic outcome in patients treated with tirbanibulin 1% ointment.Methods This post-hoc analysis of the phase III TirbAKare study (NCT06135415) included 280 patients randomized 2:1 to tirbanibulin or vehicle. Similar results were observed at D113 (-0.26; 95%CI: -0.44, -0.08).Conclusions These results suggest a clinical relationship between AK lesion clearance and cosmetic outcome in tirbanibulin-treated patients at both, D57 and D113. Most of tirbanibulin treated patients appeared to achieve both, ≥ 75% reduction in lesion count and good/excellent cosmetic outcome, aligning with treatment expectations of both, patients and investigators."

Clinical • Actinic Keratosis • Dermatology

Comments on "Randomized comparative study of 5-Fluorouracil 4 %, tirbanibulin, and photodynamic therapy for relapsing actinic keratoses". (PubMed, Photodiagnosis Photodyn Ther) - No abstract available

Journal • Actinic Keratosis • Dermatology