Delving into the Latest Updates on Fenticonazole Nitrate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Fenticonazole, Fenticonazole nitrate (USAN)

+ [3]

Target

Ergosterol

Mechanism

Ergosterol biosynthesis inhibitors

Therapeutic Areas

Infectious DiseasesUrogenital DiseasesSkin and Musculoskeletal Diseases

Active Indication

MycosesCandidiasis, VulvovaginalTinea Pedis+ [1]

Inactive Indication-

Originator Organization-

Active Organization

Kaifeng Pharmaceutical (Group) Co., Ltd.

Beijing Meidi Kangxin Pharmaceutical Technology Co.,Ltd.

Nanjing Haina Pharmaceutical Technology Co Ltd.

+ [1]

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date-

Regulation-

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Structure

Molecular FormulaC24H20Cl2N2OS

InChIKeyZCJYUTQZBAIHBS-UHFFFAOYSA-N

CAS Registry72479-26-6

View All Structures (2)

Candida onychomycosis is a common fungal infection affecting the nails, primarily caused by Candida (C.) species. Regarding the increasing trend of Candida onychomycosis and the antifungal resistant phenomenon in recent years, this study aims to evaluate the epidemiological characteristics of Candida onychomycosis, the distribution of emerging species, and the antifungal susceptibility profiles of isolates. Onychomycosis caused by yeast species was confirmed through direct examination and culture of nail scraping among all individuals suspected to have onychomycosis and referred to a medical mycology laboratory between June 2019 and March 2022. Species of yeast isolates were identified using the multiplex PCR and PCR-RFLP methods. The antifungal susceptibility of isolates to common antifungal agents and imidazole drugs was evaluated according to the M-27-A3 CLSI protocol. Among 101 yeast strains isolated from onychomycosis, Candida parapsilosis complex (50.49%) was the most common species, followed by C. albicans (20.79%) and C. tropicalis (10.89%). Rare species of yeasts such as C. guilliermondii and Saccharomyces cerevisiae were also identified by molecular methods. Results obtained from antifungal susceptibility testing showed significant differences in MIC values of isoconazole, fenticonazole, and sertaconazole among different species. Overall, a fluconazole-resistant rate of 3% was found among Candida species. Moreover, there was a statistically significant difference in MICs of fenticonazole and clotrimazole between the two most prevalent causative species, C. parapsilosis complex and C. albicans. Correct identification of the causative agents of onychomycosis and performing susceptibility testing could be helpful in choosing the most appropriate antifungal therapy.

17 Jan 2023·FEMS Microbiology Letters

Therapeutic effects of fenticonazole on bacterial vaginosis in mice

Article

Author: Peng, Peiran ; Dai, Hongbo ; Mei, Ru ; Zhu, Jun ; Yao, Chao ; Yu, Jinfen

AbstractBacterial vaginitis (BV) is a syndrome of increased vaginal discharge, fishy smelling leucorrhea, and itching and burning vulva caused by the microecological imbalance in the vagina induced by mixture of Gardnerella vaginalis (GV) and some anaerobic bacteria. Fenticonazole, an imidazole derivative and antimicrobial compound, has been demonstrated to exert effective therapeutic effects in mixed vaginitis. Accordingly, our study was designed to explore the potential role of fenticonazole in GV-infected BV mouse models. Female C57/BL6 mice were injected intraperitoneally with β-estradiol 3 days before and on the day of GV infection to maintain a pseudoestrus state. On the day of infection, mice were intravaginally inoculated with 20 µl of a suspension of GV (6 × 106 CFU/ml). Fenticonazole was administered as 2% vaginal cream (0.2 mg each mouse) by intravaginal application once a day for 3 days beginning the day of infection. At day 3 postinfection, the mice were sacrificed and vaginal washes were harvested. GV proliferation and Lactobacillus content were calculated in the vaginal lavage. Neutrophil counts in the vaginal lavage were observed through Pap staining. Myeloperoxidase (MPO) activity and proinflammatory cytokine (TNF-α, IL-1β, IL-6, iNOS, COX2, and NF-κB) levels in vaginal tissues were measured by ELISA and western blotting. Vaginal tissues were stained by hematoxylin and eosin (H&E) to examine the exfoliation of vaginal epithelial cells. GV infection increased GV proliferation and neutrophil counts but reduced Lactobacillus content in the vaginal lavage, as well as enhanced MPO activity, proinflammatory cytokine levels, and the exfoliation of vaginal epithelial cells in vaginal tissues of BV mouse models. However, administration of fenticonazole significantly ameliorated the above phenomena. Fenticonazole greatly improves the symptoms of GV-induced BV in mouse models.

31 Dec 2022·Drug Delivery

Corneal targeted fenticonazole nitrate-loaded novasomes for the management of ocular candidiasis: Preparation, in vitro characterization, ex vivo and in vivo assessments

Article

Author: Amin, Maha M. ; Ahmed, Sadek ; Sayed, Sinar ; El-Korany, Sarah Mohamed

The purpose of this manuscript was to develop and optimize Fenticonazole Nitrate (FTN)-loaded novasomes aiming to enhance drug corneal penetration and to improve its antifungal activity. Ethanol injection was used to formulate FTN-loaded novasomes adopting a central composite design. The researched factors were: stearic acid concentration (g%) (A), span 80: drug ratio (B) and cholesterol amount (mg) (C), and their effects on percent entrapment efficiency (EE%), particle size (PS), poly-dispersity index (PDI), zeta potential (ZP), and in vitro drug release after 8 hours (Q8h) were studied. Numerical optimization by Design-Expert® software was employed to select the optimum formula in respect to highest EE%, ZP (as absolute value), and Q8h >80% and lowest PS and PDI. Additional evaluation of the optimum formula was accomplished by short term stability study, effect of gamma sterilization, determination of Minimal Inhibitory Concentration and ex vivo corneal permeation study. The in vivo evaluation of the optimum formula was done to ensure its safety via in vivo ocular irritancy and in vivo corneal tolerance studies. Also, the efficacy was confirmed through in vivo corneal uptake study and susceptibility test. The optimum formula with the highest desirability value (0.738) showed EE% (94.31%), PS (197.05 nm), ZP (-66.95 mV) and Q8h (85.33%). It revealed to be safe, with augmented corneal permeation (527.98 µg/cm²) that leads to higher antifungal activity. The above results confirmed the validity of novasomes to improve the corneal permeation and antifungal activity of Fenticonazole Nitrate.

100 Deals associated with Fenticonazole Nitrate

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External Link

KEGG	Wiki	ATC	Drug Bank
D02583	Fenticonazole Nitrate	D01AC12 G01AF12	DB13434

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Mycoses	-	-	-

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Candidiasis, Vulvovaginal	Phase 3	CN	Shandong Teruilin Medicine Technology Development Co., Ltd.	09 Aug 2016
Tinea Pedis	Phase 2	CN	Kaifeng Pharmaceutical (Group) Co., Ltd.	12 Apr 2019
Dermatomycoses	Phase 1	CN	Nanjing Haina Pharmaceutical Technology Co Ltd.	17 Aug 2015