Kerydin (tavaborole) / Pfizer - LARVOL DELTA

Boron-Based Bioisosteres in Medicinal Chemistry: Advances in Heterocycles and Therapeutic. (PubMed, ChemMedChem) - "Benzoxaboroles have reached clinical relevance, including antifungal drugs such as tavaborole and crisaborole, as well as late-stage candidates like epetraborole and acoziborole. Benzoxaborinines and olaparib isosteres exhibit activity against carbonic anhydrases and PARP enzymes, while boronic acid drugs such as bortezomib and ixazomib are established proteasome inhibitors used in cancer therapy...Despite these advances, challenges remain regarding potency, pharmacokinetics, and mechanistic understanding of boron-target interactions. Overall, boron-based bioisosteres represent a versatile platform for developing new therapeutics across diverse disease areas."

Journal • Review • Oncology • PARP1

Boron-Containing Drug Candidates in Clinical Trials. (PubMed, Handb Exp Pharmacol) - "The agents reviewed include borofalan, delanzomib, flovagatran, dutogliptin, talabostat, numidargistat, OATD-02, AN0128, epetraborole, ganfeborole, acoziborole, taniborbactam, xeruborbactam, and sodium borocaptate, as well as the five FDA-approved boroncontaining drugs (bortezomib, ixazomib, crisaborole, tavaborole, vaborbactam). The review also highlights how clinical success depends on matching pharmacology with unmet need, feasible administration, competitive differentiation, and durable development partnerships. Ongoing advances in scaffold design, delivery, combination therapy, and indication selection are expected to broaden the therapeutic impact of boron-containing medicines."

Journal • Cardiovascular • Head and Neck Cancer • Hematological Disorders • Infectious Disease • Oncology • Pulmonary Disease • Respiratory Diseases • Solid Tumor • Thrombosis • Tuberculosis

TiO2-Catalyzed Borylation of Haloarenes under Visible Light and Synthesis of Benzoxaboroles. (PubMed, J Org Chem) - "The familiar boron-bearing drug molecules are tavaborole, crisaborole, bortezomib, ganfeborole, and ixazomib. A new reaction mechanism was proposed, and the radical intermediate was trapped by 2,2,6,6-tetramethyl-1-piperidinyloxy. This method was successfully applied for one-pot borylation and reduction of aldehydes, followed by cyclization under an acidic medium for the synthesis of benzoxaboroles."

Journal

Molecular modeling of 7-propanamide benzoxaboroles as CPSF3 inhibitors through docking-based 3D-QSAR and molecular dynamics simulations. (PubMed, RSC Adv) - "Benzoxaboroles are boron-based heterocycles with broad therapeutic potential, including two FDA-approved drugs, tavaborole and crisaborole. Among them, compounds 50 and 51 show enhanced pIC50 values compared to compound 32. In conclusion, this study explores SARs of benzoxaborole compounds through docking-based 3D-QSAR and MD simulations, offering valuable theoretical guidance for the rational design of new benzoxaborole derivatives as anti-cancer agents via inhibiting CPSF3."

Journal • Oncology

A targeted drug-repurposing strategy identifies Tavaborole (Kerydin) as a potent fungistatic agent against Candida auris. (PubMed, Front Microbiol) - "Shared alterations in glycogen metabolism and amino acid biosynthesis suggest conserved antifungal adaptation mechanisms. Altogether, this study highlights Tavaborole as a promising antifungal candidate against C. auris, sheds novel insights into drug resistance mechanisms employed by the pathogen and delivers a drug-repurposing procedure highly customizable to target other microorganisms."

Journal

Response to Reich and Lipner, "Defining an onychomycosis cohort: The importance of mycologic sampling". (PubMed, JAAD Int) - No abstract available

Journal • Infectious Disease

On the mode of anti-C. albicans activity of a bis(benzoxaborole) analogue of tavaborole. (PubMed, Future Sci OA) - "Benzoxaboroles exhibited a similar resistance to azoles, which is associated with increased MDR1 and IDH6 levels. Efflux inhibitors for benzoxaboroles were crucial for treating candidiasis and may inspire future antifungal research."

Journal • Candidiasis • ABCB1

Activity of Topical Antifungals Against the Terbinafine-Resistant Dermatophyte Trichophyton indotineae: In Vivo Analysis (AAD 2026) - "These results were confirmed in this in vivo model of T. indotineae dermatophytosis, in which efinaconazole demonstrated clinical efficacy 1.6- and ~3-fold higher than tavaborole and ciclopirox, respectively. These findings suggest efinaconazole may be effective in treatment of onychomycosis from terbinafine-resistant T. indotineae."

Preclinical • Infectious Disease

Zn2+-Driven Tavaborole-Adenosine Hydrogel: A Strategy for Enhanced Solubility, Sustained Release, and Antifungal Efficacy. (PubMed, Mol Pharm) - "Cytotoxicity assays on RAW 264.7 cells indicated good biocompatibility with >85% cell viability. These findings suggest that the AT-Zn2+ hydrogel holds significant potential as a clinically effective antifungal agent."

Journal • Infectious Disease

Telemedicine visits for new onychomycosis diagnoses result in fewer antifungal prescriptions than in-person care: A retrospective cohort study. (PubMed, JAAD Int) - No abstract available

Journal • Retrospective data • Infectious Disease

Decoding iNOS Inhibition: A Computational Voyage of Tavaborole Toward Restoring Endothelial Homeostasis in Venous Leg Ulcers. (PubMed, Pharmaceuticals (Basel)) - "MD trajectories for 1 ns showed stable structural configurations with negligible deviations (RMSD ≈ 0.44 ± 0.10 nm) and hydrogen bonding, and MM-PBSA analysis confirmed energetically favorable complex formation (ΔG_binding ≈ 18.38 ± 63.24 kJ/mol) similar to the control systems (L-arginine and 1400W). Taken together, these computational findings indicate that tavaborole can stably occupy the iNOS active site and interact with key catalytic residues, providing a mechanistic basis for further in vitro and ex vivo validation of its potential as an iNOS inhibitor to reduce nitrosative stress and restore endothelial homeostasis in venous leg ulcers, rather than direct therapeutic proof."

Journal • Cardiovascular • Inflammation • Venous Ulcer

Recent advances in the synthesis and applications of oxaborole derivatives. (PubMed, Org Biomol Chem) - "This property has led to the successful development of FDA-approved therapeutics such as tavaborole (antifungal) and crisaborole (anti-inflammatory), sparking widespread research interest. Emphasis is placed on the development of sustainable and efficient routes, such as photocatalytic, mechanochemical, and continuous-flow processes. Along with the synthesis, the review also covers the expanding applications of these compounds in different fields."

Journal • Review

Benzoxaborole and Beyond: The Emergence of Cyclic Hemiboronic Acids as a Versatile Chemotype in Medicine, Catalysis, and Materials. (PubMed, Chem Rev) - "Inspired by the recent success of the benzoxaborole ring system in drug discovery, highlighted by the approved products tavaborole and crisaborole, the last two decades have seen a continuous rise in interest toward other classes of nonaromatic and pseudoaromatic hemiboronic heterocycles. Preparative methods, structural characteristics, and important physical properties such as the open-closed equilibrium, acidity (pKa), and molecular interactions are discussed and compared between different structural subtypes. Ring size and the nature of heteroatoms within the ring often exert dramatic differences in acidity, reactivity, and aromatic character of the heterocycle, which in turn enable their methodical application."

Journal • Review

Recent Advancements in the Diversification and Applications of Boron-Containing Compounds in Medicinal Chemistry. (PubMed, Pharmaceuticals (Basel)) - "Boron-containing compounds have made a significant impact on the field of medicinal chemistry since the discovery of Bortezomib (Velcade®), a dipeptide boronic acid approved by the FDA in 2003 for the treatment of multiple myeloma. Since then, over the last two decades, four more boron-containing drugs have been approved by the FDA: Tavaborole (Kerydin®), Ixazomib (Ninlaro®), Crisaborole (Eucrisa®), and Vaborbactam (in Vabomere®). These compounds are approved for treating conditions such as onychomycosis, multiple myeloma, and atopic dermatitis, as well as an Aβ-lactamase inhibitor approved in combination with meropenem for treating infections...This review aims to highlight the recent advances made in the last decade in the drug design of boron-containing compounds and their therapeutic applications. Here, in this work, we have focused on the recent diversification and progress of boron-containing compounds in medicinal chemistry applications."

Journal • Review • Atopic Dermatitis • Dermatitis • Dermatology • Hematological Malignancies • Immunology • Infectious Disease • Multiple Myeloma • Oncology

Inhibition of Mandelate Racemase by Boron-Based Inhibitors: Different Binding Modes for Benzoxaboroles Versus Boronic Acids. (PubMed, Biochemistry) - "Interestingly, 11B NMR spectroscopy and X-ray crystallography revealed that aryl boronic acids and benzoxaboroles interact with MR via different binding modes. Unlike phenylboronic acid, which forms an Nε2-B bond with His 297 at the active site, the 1.8-Å resolution structure of the MR-tavaborole adduct revealed the presence of an Nζ-B bond between the bound tavaborole and Lys 166 at the active site."

Journal

Combination of Low White Blood Cell Count and Impaired Renal Function Is a Risk Factor for Higher Concentrations of Venetoclax and Prolonged Neutropenia in AML Patients with Venetoclax Combined Regimen: Real World Experience in the Japanese Cohort (ASH 2024) - "Aim : Severe and prolonged neutropenia is one of the most critical adverse events associated with venetoclax (VEN) in combination with azacitidine (Aza)...Patients with WBC < 3000/ul and estimated GFR (eGFR) <60ml/min showed higher VEN AUC values compared to others (Low WBC and low eGFR : mean 38935 h・ug/l vs others : mean 26901 h・ug/l, p = 0.020)...And importantly, we discovered patients with low WBC count and low renal function could be risk factors for higher concentrations of VEN and, eventually, prolonged neutropenia. VEN intensity-guided adjustment might be worth considering to manage neutropenia for Asian AML populations, especially patients with low WBC and impaired renal function."

Clinical • Real-world • Real-world evidence • Acute Myelogenous Leukemia • Hematological Disorders • Neutropenia

Clinical Application of Single-Cell MRD By Genotype and Phenotype in AML (ASH 2024) - "The majority of patients (61.9%) received induction with cytarabine and anthracycline, while 28.6% received hypomethylating agents and venetoclax while 9.5% received other therapies...A total of 61,858 cells were called (mean 2690 cells/sample)...In conclusion, we report that single-cell MRD multi-omics in AML was feasible in clinical practice and offered additional information above that received from MFC- and NGS-based MRD assays, either alone or in combination. Updated results from clinical outcomes will be presented."

Clinical • Acute Myelogenous Leukemia • Chronic Myelomonocytic Leukemia • Hematological Malignancies • Leukemia • Oncology • CD34 • CDKN2A • DNMT3A • FLT3 • IDH1 • IDH2 • KIT • NPM1 • TP53 • U2AF1

Benzoxaboroles in medicinal chemistry: A structure-guided perspective on next-generation therapeutics. (PubMed, Eur J Med Chem) - "Special attention is given to translationally relevant examples, including FDA-approved drugs such as Tavaborole, investigational clinical candidates, and novel hybrid scaffolds that exploit BBZ's covalent and reversible binding capabilities. Distinguishing features of this review include (a) a residue-level analysis of target-ligand interactions, particularly for LeuRS and β-carbonic anhydrase enzymes, (b) a critical discussion of physicochemical parameters such as pKa modulation for activity tuning, (c) an exploration of hybrid chemotypes (e.g., Amp-B-BBZ conjugates), for overcoming resistance and toxicity, and (d) future opportunities for targeting neglected pathogens. By consolidating dispersed literature and integrating structure-guided design principles, this review not only serves as a reference for the current state of BBZ-based therapeutics but also outlines rational strategies for the next generation of boron-based drugs, thereby addressing gaps in scope..."

Journal • Review • Oncology

Onychomycosis in Diabetics: A Common Infection with Potentially Serious Complications. (PubMed, Life (Basel)) - "Systemic antifungals such as terbinafine and itraconazole are considered first-line therapies, particularly for moderate to severe onychomycosis...For patients with mild to moderate disease, or contraindications to oral therapy, topical agents such as efinaconazole or tavaborole offer viable alternatives. Adjunctive measures, including education on foot hygiene, prompt treatment of tinea pedis, and environmental sanitization, are important in preventing recurrence and reinfection. This review summarizes the epidemiology, diagnosis, and treatment considerations for onychomycosis in diabetic patients, emphasizing the need for individualized care to improve outcomes in this high-risk population."

Journal • Review • Cardiovascular • Dermatology • Diabetes • Infectious Disease • Metabolic Disorders • Mood Disorders • Pain • Peripheral Arterial Disease

Broad-spectrum antifungal activity of aniline-modified tavaborole derivatives: insights from molecular docking and bioassays. (PubMed, Pest Manag Sci) - "This study establishes substituted aniline-tavaborole hybrids as highly promising candidates for next-generation agricultural fungicides. The unique LeuRS inhibition mechanism of the designed molecules presents an innovative and effective strategy to counter fungal pathogens, demonstrating substantial potential for crop protection."

Journal

Onychomycosis in special populations. (PubMed, Future Microbiol) - "Topical antifungals such as efinaconazole, tavaborole, and ciclopirox can be considered for mild to moderate onychomycosis. This review provides an in-depth overview of the epidemiology, diagnosis, and management of onychomycosis in special populations, underscoring the importance of individualized care to improve outcomes and reduce recurrence."

Journal • Review • Dermatology • Diabetes • Hepatology • Immunology • Infectious Disease • Metabolic Disorders • Psoriasis • Transplantation

Comprehending the Potential of Topical Therapies for the Treatment of Onychomycosis. (PubMed, Recent Adv Drug Deliv Formul) - "The main challenge associated with topical therapy was found to be the unique structure of the nails, hampering drug penetration to the infection site and inducing fungal drug resistance. Conventional treatment methods, as well as novel techniques developed for topical therapy, like microporation, ionotophoresis, laser, and photodynamic therapy, have also been explored. Oral antifungals are most commonly used for moderate to severe onychomycosis as they provide greater cure rates, whereas topical application of antifungals is advocated for mild to moderate infections as it possesses a better safety profile. Efinaconazole solution (10%), tavaborole solution (5%), and ciclopirox nail lacquer (8%) for topical use are accepted by the Food and Drug Administration (FDA) for the management of onychomycosis. Laser treatment is approved in the United States for the short-term improvement of clear nails in fungal infections, but the clinical outcomes have not yet reached optimal..."

Journal • Infectious Disease

Transfersome enhances nail penetration of antifungal drug and photosensitizer for chemo-photodynamic therapy of onychomycosis in a novel rat model. (PubMed, J Control Release) - "Here, a transfersome (termed THT) capable of penetrating nails to deliver a photosensitizer (hematoporphyrin monomethyl ether, HMME) and an antifungal chemotherapeutic drug (tavaborole) has been developed, achieving a chemo-photodynamic synergistic treatment of onychomycosis...It is accumulated around and deformed to enter the physiological pores of the nail plate, effectively penetrating to deeper layers at the nail bed. THT, with its high nail penetration efficiency and potent synergistic antifungal activity, represents a promising topical treatment for onychomycosis."

Journal • Preclinical • Infectious Disease

Styrene-Maleic Acid Copolymer-Based Nanoprobes for Enhanced Boron Neutron Capture Therapy. (PubMed, Pharmaceutics) - " Two SMA-based BNCT nanoprobes, SMA-glucosamine conjugated Borax (SG@B) and SMA-conjugated aminophenylboronic acid encapsulating tavaborole (S-APB@TB), were designed and synthesized... These findings highlight the tumor-targeting potential of SMA-based BNCT nanoprobes. Further investigations are warranted to advance their clinical development as BNCT agents."

Journal • Colon Cancer • Colorectal Cancer • Oncology • Sarcoma • Solid Tumor

Antifungal agent tavaborole as a potential broad-spectrum serine and metallo-β-lactamases inhibitor. (PubMed, EBioMedicine) - "Tavaborole shows good potential as an agent for use in combination with β-lactam antibiotics for treating multidrug-resistant Gram-negative bacterial infections."

Journal • Infectious Disease