ketoconazole / Generic mfg. - LARVOL DELTA

Targeted inhibition of FBXL2 confers susceptibility of HER2-negative breast cancer to trastuzumab deruxtecan. (PubMed, Nat Cancer) - "Strikingly, GGTi-2418@LNP or ketoconazole@LNP combined with T-DXd induced robust and durable tumor regression in HER2-IHC 0 TNBC xenograft models in female mice. Together, this study highlights that targeted inhibition of FBXL2 combined with T-DXd may be a viable therapeutic strategy for treating HER2-IHC 0 solid tumors."

Journal • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • Targeted Protein Degradation • Triple Negative Breast Cancer • FBXL2 • HER-2

Protein covalent modification and hepatic cytotoxicity of atorvastatin resulting from its metabolic activation. (PubMed, Arch Toxicol) - "Atorvastatin calcium (ATV) is a statin drug that reduces low-density lipoprotein cholesterol and is widely used for the prevention and treatment of hyperlipidemia and cardiovascular and cerebrovascular diseases. Pre-treatment with CYP3A inhibitor ketoconazole (KTC) significantly reduced both ATV-derived protein adduction and hepatocyte susceptibility to ATV cytotoxicity. The findings facilitate the understanding of the mechanisms involved in ATV's idiosyncratic toxicity through systematic characterization of a CYP3A-mediated bioactivation process."

Journal • Cardiovascular • CNS Disorders • Dyslipidemia • Hepatology • Liver Failure • Vascular Neurology

Molecularly Imprinted Polymer‒Solid-Phase Extraction Coupled With High-Performance Liquid Chromatography-Ultraviolet Detection for Selective Determination of Ketoconazole in Cosmetic Shampoo. (PubMed, J Sep Sci) - "The method demonstrated excellent precision (relative standard deviation ≤ 6.06%) and high recovery rates (80.41%-98.86%) in real samples. Consequently, this study establishes a cost-effective, selective, and highly efficient approach for the determination of trace levels of KCZ in cosmetic products."

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Unveiling the impact of atmospheric temperature on antifungal resistance and virulence factors in Candida spp. isolated from forest ecosystem. (PubMed, Microb Pathog) - "Antifungal susceptibility was assessed using the Kirby-Bauer disk diffusion method, testing the efficacy of amphotericin B, fluconazole, ketoconazole, and voriconazole. The stability of phospholipase and esterase activity indicates that not all virulence factors are temperature-sensitive, emphasizing the complexity of fungal adaptation. This study highlights the critical need for further research on the influence of climate change on fungal pathogenicity and treatment efficacy."

Journal • Infectious Disease

Engineering micro- and nanosized pharmaceutical salt crystals using high-pressure homogenization. (PubMed, Int J Pharm) - "Using ketoconazole (KTZ) and oxalic acid (OA) as a model system, salt formation was successfully achieved through HPH processing in the presence of various stabilizers (Pharmacoat® 606, Pluronic® F127, Soluplus®, and TPGS) at different concentrations and process temperatures...Dissolution studies performed at pH 4.4 showed up to an 80% drug release within 15 min for HPH-processed KTZ:OA salts, a substantial improvement over bulk KTZ. The findings establish HPH as a versatile, solvent-free, and continuous manufacturing platform for the production of high-purity pharmaceutical salts with superior dissolution performance, highlighting its potential to transform solid-state drug formulation and process intensification strategies in pharmaceutical development."

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Molecular Identification and Evaluation of Resistance to Antifungal Drugs in Candida Species Isolated From Diaper Rash of Neonates. (PubMed, Health Sci Rep) - "Nystatin, posaconazole, voriconazole, amphotericin B, ketoconazole, and clotrimazole showed high activity against all species (Minimum Inhibitory Concentration ≤ 0.125 µg/mL). The treatment of recurrent invasive candidiasis, needing repeated course of fluconazole or itraconazole, could be a risk factor for selecting resistant isolates. In addition, as the liposomal amphotericin B is no more commercialized in our country, a higher drug selection pressure for azoles may be expected in the future."

Journal • Candidiasis • Contact Dermatitis • Dermatitis • Dermatology • Immunology • Infectious Disease • Pediatrics

Cutaneous Syncephalastrum racemosum infection in an immunocompetent patient successfully treated with oral ketoconazole: case report and ten-year literature review (ESCMID Global 2026) - No abstract available

Case report • Clinical • Review • Infectious Disease

Endocrine consequences of antifungal therapy: A missed entity. (PubMed, World J Clin Cases) - "Adrenal and gonadal dysfunctions with ketoconazole, and mineralocorticoid excess with posaconazole and itraconazole, are well-documented. Uncommon manifestations, such as voriconazole-induced syndrome of inappropriate antidiuretic hormone secretion or salt-losing nephropathy, and fluoride-related periostitis associated with voriconazole and itraconazole, have also been reported...Echinocandins differ from azoles and polyenes in that they rarely affect endocrine pathways, making them a safer option when endocrine toxicity is a concern. Clinicians must remain vigilant to the endocrine adverse effects and pharmacological interactions of antifungal agents to enable timely recognition and management."

Journal • Review • Endocrine Disorders • Infectious Disease • Nephrology • Renal Disease

Emergence of Fusarium oxysporum infection in farmed Labeo rohita: Isolation, growth requirements, antifungal response, and pathogenic potential. (PubMed, Vet Res Commun) - "Antifungal susceptibility testing indicated that none of amphotericin B, ketoconazole, itraconazole, clotrimazole, and nystatin produced zones of inhibition against the fungal isolate. In contrast, the fungus exhibited sensitivity to sodium chloride and copper sulfate, with reduced radial growth at salinity levels exceeding 0.5% and CuSO4 concentrations above 25 ppm. Our findings confirm that the F. oxysporum strain is virulent to L. rohita, and highlights the potential utility of salinity and copper sulfate-based management strategies for control of this fungus in aquaculture."

Journal • Infectious Disease

Insights into Transport Function of the Murine Organic Anion-Transporting Polypeptide OATP1B2 by Comparison with Its Rat and Human Orthologues. (PubMed, Toxics) - "Cyclosporine A, ritonavir, odevixibat, rosuvastatin, and rifampicin markedly inhibited uptake...A comparison of the rodent data with the human orthologues revealed similar inhibition patterns but distinct substrate selectivity: hOATP1B1 showed high affinity for E1S but negligible TCA uptake, while hOATP1B3 transported TCA weakly but not E1S. This study provides insights into species-specific differences in OATP-mediated hepatic uptake and is therefore valuable for the interpretation of preclinical studies and their transfer to human pharmacology."

Journal • Preclinical

Species Identification, Virulence Factors, and Antifungal Resistance in Clinical Candida Isolates from ICU Patients. (PubMed, Microorganisms) - "Antifungal susceptibility to fluconazole, ketoconazole, and amphotericin B was determined only by the agar disk diffusion method, and virulence was assessed through esterase, DNase, protease, and hemolytic activity assays. Oral isolates were more frequent than tracheal isolates and demonstrated a higher prevalence of antifungal resistance and virulence traits. These findings underscore the epidemiological importance of characterizing Candida species in hospitals to better understand the yeast profile and to support adequate clinical management."

Journal • Critical care

Overcoming Candida albicans biofilm drug resistance via azole-sophorolipid synergy. (PubMed, Sci Rep) - "This study explores a novel approach combining sophorolipids (SLs), a glycolipid biosurfactant, with clinical azoles, including fluconazole (FLZ), itraconazole (ITZ), and ketoconazole (KCZ), against C. albicans biofilms. Quantitative real-time polymerase chain reaction analysis revealed significant downregulation of essential biofilm-associated genes such as BCR1, EFG1, and CDC28, demonstrating SLs's ability to inhibit various stages of biofilm development and stability. Thus, the synergy observed with azole drugs, particularly ITZ and SLs, was highly effective in biofilm removal, highlighting the compatibility of anti-biofilm biosurfactant SLs with some antifungal agents."

Journal • BCR

P versicolor: Comparison of the Efficacy of Topical Luliconazole 2% Cream vs Topical Ketoconazole 1% Cream in the Treatment of Pityriasis Versicolor. (clinicaltrials.gov) - P4 | N=86 | Not yet recruiting | Sponsor: PAEC General Hospital, Islamabad

New P4 trial

Antioxidant, Antimicrobial, and Molecular Binding Affinity Applications of Green-Synthesized Nickel Oxide Nanoparticles. (PubMed, Chem Biodivers) - "Molecular docking revealed strong binding affinities of NiO NPs with P. aeruginosa (-9.9 kcal/mol) and A. niger endoglucanase (-8.5 kcal/mol), comparable to streptomycin (-11.1 kcal/mol) and ketoconazole (-10.0 kcal/mol). These findings highlight the promising antioxidant and antimicrobial potential of NiO NPs for biomedical applications."

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Synthesis of Enduracididine Free Linear Teixobactin Analogs: Molecular Docking, DFT Calculations, and Their Antimicrobial Activities, Bacterial Cell Wall Lysis and Glucose Assay. (PubMed, Curr Med Chem) - "Mass, 1H NMR, and HPLC analysis characterized the synthesized fine TX analogs (TX1-TX5). The DFT and docking studies' electronic characteristic calculations predicted that halogenated (TX1, TX2, and TX4) and methoxy (TX3) substituted analogs have higher stability and electrophilicity, making them suitable agents for antimicrobial activity."

Journal • Infectious Disease

Exploring the potential of postbiotic Limosilactobacillus fermentum as a novel therapeutic agent for Candida albicans. (PubMed, J Microbiol Methods) - "The antifungal drugs used were found to be effective against Candida isolates; however, two isolates, belonging to C. albicans and C. tropicalis, showed significant resistance to the tested antifungal agents, fluconazole 10 μg and ketoconazole 10 μg. The postbiotic of L. fermentum GD5MG inhibited the growth of antifungal drug-resistant Candida sp., significantly reducing the number of planktonic Candida cells and inhibiting Candida biofilm formation, thereby showcasing its potential to suppress dental caries. These observations underscore that, despite the promising probiotic potency, the postbiotic of L. fermentum GD5MG remains a novel and alternative therapeutic candidate for dental prophylaxis."

Journal • Dental Disorders

​Temporal proteomic profiling of iPSC-derived human liver organoids reveals optimal maturation for drug metabolism and toxicology. (PubMed, Sci Rep) - "Functional validation of CYP3A4 activity through rifampicin induction and ketoconazole inhibition demonstrated metabolic competence comparable to existing in vitro liver models, including HepaRG cells and primary human hepatocytes. Interestingly, Day 45 organoids exhibited a shift toward a mesenchymal cell profile, with increased markers of hepatic stellate cells, suggesting utility for disease modeling applications. These findings indicate Day 30 of liver organoids as the optimal stage for drug metabolism and toxicological investigations, providing a proteomic framework that enhances their utility of iHLOs as physiologically relevant liver models."

Journal • CYP3A4

Phytochemical composition and antimicrobial efficacy of Nigerian polyherbal formulations against antibiotic-resistant micro-organisms. (PubMed, Sci Rep) - "The Kruskal-Wallis' test results indicated significant differences among the groups, with gentamicin demonstrating a notably higher mean rank. Ultimately, the findings suggest that although gentamicin and ketoconazole exhibited superior activity, both plant extract formulations hold promise as potential alternative antimicrobial sources, thereby contributing to the combat against antibiotic resistance."

Journal • Infectious Disease

Enhancing bioavailability of a weakly basic drug through cocrystallization: PBPK modeling of ketoconazole-succinic acid. (PubMed, Eur J Pharm Biopharm) - "The model successfully captured the reduced exposure to KTZ when administered with omeprazole. This model-based approach has demonstrated the potential of KTZ-SA cocrystal to enhance bioavailability in populations with achlorhydria-related disparities, effectively addressing the challenges posed by variable gastric acidity. The findings support the development of pharmaceutical cocrystals to optimize drug delivery and maximize therapeutic outcomes."

Journal • Gastrointestinal Disorder • Metabolic Disorders

Drug Release, Entrapment Efficacy, and Drug Loading Capacity of Taxanes Loaded Solid Lipid Nanoparticles (SLNs). (PubMed, Anticancer Agents Med Chem) - "Multiple formulation and environmental factors influence EE%, DLC%, and the drug release behavior of Taxane-loaded SLNs. Understanding these variables is not just important, but it is the key to rationalizing effective and stable nano-lipid formulations in cancer therapy. It is a fascinating and crucial area of study that demands our attention."

Journal • Oncology

In vitro antifungal and antibiofilm evaluation of reduction-responsive ketoconazole-loaded nanoparticles based on cystamine-modified poly (isobutene-alt-maleic anhydride) polymer. (PubMed, Pharm Dev Technol) - "Interestingly, MPEG-P-KET demonstrated higher ability to inhibit biofilm formation and disrupt mature biofilms than KET. The polymeric nanoparticles with disulfide bonds could be used for the encapsulation and controlled delivery of antifungal drugs in the field of fungal infection treatment."

Journal • Preclinical • Infectious Disease

Characterization of EpiIntestinal Duodenum Microtissue as an In Vitro Model for Studying Intestinal Drug Permeability, Transport, and Metabolism. (PubMed, Pharm Res) - "These findings suggest that the EpiIntestinal duodenum microtissue can effectively replicate the complex interplay of permeability, metabolism, and transport in the gut, thereby improving the prediction of oral drug absorption."

Journal • Preclinical • CYP2C19 • CYP3A4 • UGT1A1

Epidemiology of Fungal Bloodstream Infections and Antifungal Susceptibility in a Tertiary Care Hospital in Riyadh, Saudi Arabia: A Rare Candida Co-Infection Case. (PubMed, Pathogens) - "The high prevalence of NAC, including tolerant isolates of C. parapsilosis and C. glabrata, along with multi-azole-resistant C. albicans and unique coinfection scenarios, urgently requires robust antifungal resistance surveillance."

Journal • Candidiasis • Infectious Disease

Carbonized NiFeP-MOF porous nanoflowers via in-situ LDH-to-MOF conversion on Fe3O4@SiO2 for vortex-assisted magnetic dispersive μSPE and LC-MS/MS analysis of antifungals in blood samples. (PubMed, Talanta) - "In this study, an efficient analytical method based on vortex-assisted magnetic dispersive micro solid phase extraction (VA-MD-μSPE) was developed for the extraction, cleanup and preconcentration of trace quantities of antifungal drugs-including ketoconazole (KZ), clotrimazole (CZ) and miconazole (MZ)-in blood samples, using a novel carbonized magnetic sorbent NiFeP-MOF@SiO2@Fe3O4, followed by quantification using LC-MS/MS...The method demonstrated Greenness and Blueness metrics of 0.64 and 55.0, respectively, reflecting its good sustainability and practical applicability. In light of the simplicity and aforementioned figures of merit, this method demonstrates strong potential as a streamlined strategy for extracting target analytes from complex biological matrices."

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Impact of cocrystal dissolution-supersaturation-precipitation (DSP) behaviour on drug permeation across the PermeaPad® biomimetic barrier. (PubMed, Eur J Pharm Sci) - "Our findings with the 1:1 ketoconazole (KTZ) -p-aminobenzoic acid (PABA) cocrystal indicate the existence of an optimal SA value (7), where KTZ-PABA dissolution performance resulted in 8-fold AUC increase, translating to a 7-fold increase in cumulative KTZ permeation after 6 hours...The strategy presented in this work can be readily applied during the pre-formulation stage of cocrystal development, enabling targeted selection of coformer concentrations for formulation development. Overall cocrystals offer unique flexibility as a formulation strategy for poorly water-soluble drugs, allowing for tailored DSP behaviour and drug transport over biological barriers based on mechanistic understanding, as demonstrated in this study."

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