Loramyc (miconazole muco-adhesive buccal tablet) / Valerio Therap, Nxera Pharma, Fuji Pharma, GALT Pharma - LARVOL DELTA

APTYS PHARMA (BIO 2022) - "Loramyc® and Testocream® are based on Aptys pharma technologies...Our clients come to us because we can solve formulation problems and make from a bright idea an industrial reality because our team is made of flexible and open mind scientists. At the end Aptys can deliver a ready-to-use package: formula + recipe + validated analytical methods + stability data."

Pain

Phytotherapy in the management of denture stomatitis: A systematic review and meta-analysis of randomized controlled trials. (PubMed, Phytother Res) - "There was no difference in the relief of clinical signs (odds ratio (OR) = 0.96; 95% confidence interval (CI): 0.43-2.15) and microbiological improvement (OR = 1.74; 95% CI: 0.55-5.45) between propolis and miconazole. Most of the included studies showed that phytomedicines had fewer side effects and more patient satisfaction than antifungals or disinfectants. However, further RCTs with more standardly prepared herbal formulations are required to verify the clinical efficacy of phytotherapy as an alternative or adjunctive therapy for denture stomatitis."

Journal • Retrospective data • Review • Dental Disorders • Infectious Disease • Stomatitis

Lead optimization generates selenium-containing miconazole CYP51 inhibitors with improved pharmacological profile for the treatment of fungal infections. (PubMed, Eur J Med Chem) - "In addition, molecular docking studies provide a model for the interaction between the compound B17 and the CYP51 protein. Overall, we believe that these selenium-containing miconazole compounds can be further developed for the potential treatment of fungal infections."

Journal • Hematological Disorders • Infectious Disease

Inhibitory Effect of Eugenol and Trans-Anethole Alone and in Combination with Antifungal Medicines on Candida albicans Clinical Isolates. (PubMed, Chem Biodivers) - "Achieved results indicated that eugenol showed synergistic and additive activities with miconazole and econazole against investigated clinical isolates, respectively. We tried to relate the results to changes in C. albicans cell sheaths under the influence of essential oils compounds (EOCs) performing the Fourier transform infrared spectra analysis to confirm the presence of particular chemical moieties in C. albicans cells. Nevertheless, no strong relationships was observed between synergistic and additive actions of used EOC-AMs combinations and chemical moieties in C. albicans cells."

Clinical • Combination therapy • Journal

Miconazole induces autophagic death in glioblastoma cells via reactive oxygen species-mediated endoplasmic reticulum stress. (PubMed, Oncol Lett) - "The inhibition of ER stress via treatment with 4-phenylbutyric acid or BiP knockdown reduced miconazole-induced autophagy and cell death. These findings suggest that miconazole induces autophagic cell death by inducing an ROS-dependent ER stress response in U251MG glioma cancer cells and provide new insights into the potential antiproliferative effects of miconazole."

Journal • Dermatology • Glioblastoma • Glioma • Oncology • Solid Tumor • ERN1

Antibacterial, Antifungal, Antioxidant, and Docking Studies of Potential Dinaphthodiospyrols from Diospyros lotus Linn Roots. (PubMed, ACS Omega) - "Among all the screened compounds, 7 exhibited good activity (30-49 mm), followed by compounds 5 and 6, (35-46 mm), while compounds 1-4 showed a moderate effect (8-28 mm) against the selected fungal strain against miconazole which showed potent effects (101-110.98 mm)...From the docking analysis, it was found that the docking results are well correlated with the experimental observations. In conclusion, the dinaphthodiospyrols exhibited excellent antibacterial, antifungal, and free radical scavenging potential."

Journal • Infectious Disease • Pneumonia • Respiratory Diseases

Design, Synthesis and Anticandidal Evaluation of Indazole and Pyrazole Derivatives. (PubMed, Pharmaceuticals (Basel)) - "Particularly, compound 10g, with N,N-diethylcarboxamide substituent, was the most active against C. albicans and both miconazole susceptible and resistant C. glabrata species. Therefore, the 3-phenyl-1H-indazole scaffold represents an opportunity for the development of new anticandidal agents with a new chemotype."

Journal • Candidiasis

Antifungal Activity of 1,4-Dialkoxynaphthalen-2-Acyl Imidazolium Salts by Inducing Apoptosis of Pathogenic Candida spp. (PubMed, Pharmaceutics) - "Among the tested compounds, NAIMS 7c showed strongest antifungal activity with 3.125 μg/mL MIC value compared with miconazole which showed 12.5 μg/mL MIC value against Candida spp., and more importantly >100 μg/mL MIC value against C.auris...The expression of apoptosis-related genes was induced in C. albicans by NAIMS 7c treatment. Taken together, the synthetic NAIMSs are of high interest as novel antifungal agents given further in vivo examination."

Journal • Candidiasis

Oceanapiside, a Marine Natural Product, Targets the Sphingolipid Pathway of Fluconazole-Resistant Candida glabrata. (PubMed, Mar Drugs) - "Oceanapiside (OPS), a marine natural product with a novel bifunctional sphingolipid structure, is fungicidal against fluconazole-resistant Candida glabrata at 10 μg/mL (15.4 μM). PHS concentration was elevated in extracts of cells treated with OPS when compared with cells treated with miconazole and amphotericin B. Elevated levels of PHS in OPS-treated cells confirms that OPS affects the pathway at a step downstream of PHS synthesis. These results also demonstrated that OPS has a mechanism of action different to those of miconazole and amphotericin B and interdicts fungal sphingolipid metabolism by specifically inhibiting the step converting PHS to phytoceramide."

Journal • Metabolic Disorders

Pharyngeal haematoma and partial airway obstruction caused by interaction between warfarin and topical miconazole gel. (PubMed, BMJ Case Rep) - "His international normalised ratio (INR) was reported initially as unreadable by the laboratory, then eventually came back as >20. After a thorough medication history, he said that he had recently been prescribed topical miconazole oromucosal gel by his dentist for oral candidiasis, which had interacted with the warfarin to cause this life-threatening haematoma."

Journal • Candidiasis • Critical care • Otorhinolaryngology

Surface morphology and in vitro leachability of soft liners modified by the incorporation of antifungals for denture stomatitis treatment. (PubMed, J Appl Oral Sci) - "The surface of the soft lining materials changed more significantly with the addition of Chx or It. Softone released a higher concentration of drugs than Trusoft did, guiding the future treatment of denture stomatitis."

Journal • Preclinical • Dental Disorders • Stomatitis

A Comparative Randomized, Open-label, Multicenter Study of the Efficacy and Safety of Miconazole Mucoadhesive Tablets and Miconazole Gel in the Treatment of Oropharyngeal Candidiasis [Translated Article]. (PubMed, Med Mycol J) - "The efficacy of SO-1105 was shown to be similar to that of miconazole gel. Meanwhile, SO-1105 is an adhesive tablet and is administered once-daily. For this, SO-1105 is expected to better compliance and useful drug for the elderly. Therefore, SO-1105 is considered to be widely used in clinical practice as one of the therapeutic drugs for oropharyngeal candidiasis."

Clinical • Journal • Candidiasis

Antifungal susceptibility profiles of otomycosis etiological agents in Ahvaz, Iran. (PubMed, Curr Med Mycol) - "Furthermore, epidemiological cutoff values (ECVs) were lower than those presented by the CLSI for itraconazole and caspofungin in 98.5% and 42.6% of Aspergillus species, respectively. Terbinafine exhibited a great activity against Aspergillus species, while fluconazole revealed a low activity against both Aspergillus species. Based on the results, 77.8% of Candida species were resistant to caspofungin; however, miconazole and econazole had low MIC ranges...In addition, terbinafine was identified as the best antifungal for both Aspergillus and Candida species. Moreover, tested azoles had relatively low MICs, whereas most of the isolates had the MIC values beyond the caspofungin ECVs."

Journal • Infectious Disease • Otorhinolaryngology

Sertaconazole induced toxicity in HeLa cells through mitotic arrest and inhibition of microtubule assembly. (PubMed, Naunyn Schmiedebergs Arch Pharmacol) - "Econazole, miconazole, and sertaconazole, the structurally related azoles with imidazole moiety, were evaluated for their cytotoxicity and their ability to bind to mammalian tubulin...Competitive tubulin-binding assay using colchicine and computational simulation studies showed that sertaconazole bound closer to the colchicine site and induced the tubulin dimer to adopt a "bent" conformation which is incompetent for the polymerization...Sertaconazole significantly inhibited the migration of HeLa cells and showed synergistic antiproliferative potential with vinblastine. Collectively, the results suggest that sertaconazole which is already in clinical practice could be useful as a topical chemotherapy agent for the treatment of skin cancers in combination with other systemic anticancer agents."

Journal • Genetic Disorders • Oncology • Skin Cancer

In vitro activity of ibrexafungerp and comparators against Candida albicans genotypes from vaginal samples and blood cultures. (PubMed, Clin Microbiol Infect) - "Ibrexafungerp shows good in vitro activity against Candida albicans from vaginal samples including phenotypically fluconazole non-wild type isolates. Furthermore, we found a certain population structure where some genotypes show reduced susceptibility to fluconazole."

Journal • Preclinical • Candidiasis • Vaginitis

A Case of Black Fungal Keratitis Caused by Biatriospora mackinnonii. (PubMed, Cornea) - "To the best of our knowledge, this is the first reported case of fungal keratitis caused by B. mackinnonii; however, in this case, PKP surgery resulted in a favorable outcome."

Clinical • Journal • Complement-mediated Rare Disorders • Dermatology • Immunology • Keratitis • Ocular Inflammation • Ophthalmology

Combining Miconazole and Domiphen Bromide Results in Excess of Reactive Oxygen Species and Killing of Biofilm Cells. (PubMed, Front Cell Dev Biol) - "Co-administration of the antioxidant ascorbic acid resulted in abolishment of the ROS generated by MCZ-DB combination as well as its fungicidal action. In conclusion, increased intracellular MCZ availability due to DB's action results in excess of ROS and enhanced fungal cell killing."

Journal

[VIRTUAL] Transport and permeability properties of dapivirine: understanding potential drug-drug interactions (HIVR4P 2021) - "A clinical study conducted by the International Partnership for Microbicides showed that concomitant use of DPV and vaginal miconazole (MIC), an antifungal treatment for Candidiasis, decreased DPV levels in the vaginal fluid while increasing DPV systemic exposure... Our findings suggest that the observed DPV-MIC interaction is not due to altered DPV transport or permeability. Studies on DPV metabolism are in progress to evaluate if altered enzymatic activities cause the DPV-MIC interaction."

Candidiasis • Human Immunodeficiency Virus • Infectious Disease

Synthesis, Spectroscopy, Single-Crystal Structure Analysis and Antibacterial Activity of Two Novel Complexes of Silver(I) with Miconazole Drug. (PubMed, Int J Mol Sci) - "In a previous article, we reported on the higher toxicity of silver(I) complexes of miconazole [Ag(MCZ)NO (1)] and [Ag(MCZ)ClO (2)] in HepG2 tumor cells compared to the corresponding salts of silver, miconazole and cisplatin. All Ag(I) complexes of miconazole resulted in much better inhibition of yeast growth than silver sulfadiazine, silver salts and miconazole. Moreover, the synthesized silver(I) complexes showed good or moderate activity against Gram-negative bacteria compared to the free ligand."

Journal • Oncology

Classification of polymorphic forms of fluconazole in pharmaceuticals by FT-IR and FT-NIR spectroscopy. (PubMed, J Pharm Biomed Anal) - "Based on the plots of Hotelling's T² vs Q residuals, pure compounds of miconazole and itraconazole, that were analyzed separately, were significantly considered outliers and rejected. Furthermore, binary mixtures consist of fluconazole form-II and monohydrate form with different ratios were used to test the suitability of each technique FT-IR and FT-NIR with PLS-DA to detect minimum contaminant or polymorphic conversion from a polymorphic form to another using also the plots of Hotelling's T² vs Q residuals."

Journal

Investigation of the Physiological, Biochemical and Antifungal Susceptibility Properties of Candida auris. (PubMed, Mycopathologia) - "Our data suggest a simple identification approach of C. auris based on its physiological and biochemical properties and highlight aspects of C. auris population from various clades."

Journal

Pharmaceuticals and personal care products in the seawater around a typical subtropical tourist city of China and associated ecological risk. (PubMed, Environ Sci Pollut Res Int) - "In addition, increased concentrations of ciprofloxacin, enrofloxacin, and erythromycin around aquaculture farms imply that aquaculture cannot be neglected as a source. The risk quotients calculated with the maximum concentrations of miconazole, triclosan, dehydronifedipine, and triclocarban exceeded 0.1, indicating potential moderate or high risks. Antibacterial agents in daily chemicals and azole broad-spectrum antifungals were associated with the highest risks in this study; this might be another significant pollution characteristic in the sea area around this subtropical tourist city."

Journal

Prevalence and antifungal susceptibility of gastrointestinal candidiasis among diabetic patients: A cross-sectional study. (PubMed, Afr J Lab Med) - "Resistance was observed with miconazole (48.65%), clotrimazole (18.92%) and fluconazole (8.11%). No resistance to itraconazole and nystatin was observed. Gastrointestinal candidiasis was associated with poor glucose control (p ≤ 0.001), prior use of antibiotics (p ≤ 0.001), antifungals (p ≤ 0.001) and corticosteroids (p ≤ 0.001) and was more common among female patients (p = 0.01). Occurrence of gastrointestinal candidiasis was relatively low among our participants, and infection was associated with poor glucose control, female sex and use of antifungals, antibiotics and corticosteroids."

Clinical • Journal • Observational data • Candidiasis • Dermatology • Diabetes • Gastrointestinal Disorder • Metabolic Disorders • Solid Tumor

Severe acute generalized exanthematous pustulosis (AGEP) induced by miconazole oral gel with overlapping features of drug reaction with eosinophilia and systemic symptoms (DRESS). (PubMed, Contact Dermatitis) - No abstract available

Journal • Eosinophilia • Epstein-Barr Virus Infection • Immunology

Management of recurrent aphthous ulcers exploiting polymer-based Muco-adhesive sponges: in-vitro and in-vivo evaluation. (PubMed, Drug Deliv) - "Additionally, histopathological examination showed faster healing with complete restoration of the normal oral histology in rats. The present study concludes that chitosan sponge loaded with a combination of tenoxicam and miconazole nitrate could improve healing of RAU cases."

Journal • Preclinical • Candidiasis • Immunology • Inflammation • Pain