scholarly journals In Vitro Activities of Novel Azole Compounds ATTAF-1 and ATTAF-2 against Fluconazole-Susceptible and -Resistant Isolates of Candida Species

2016 ◽  
Vol 61 (1) ◽  
Author(s):  
Hamed Fakhim ◽  
Saeed Emami ◽  
Afsane Vaezi ◽  
Seyedeh Mahdieh Hashemi ◽  
Leila Faeli ◽  
...  
Keyword(s):  
Candida Species ◽  
Antifungal Agents ◽  
Synergistic Effects ◽  
Geometric Mean ◽  
The Novel ◽  
Content Type ◽  
Fluconazole Resistant ◽  
Dose Dependent

ABSTRACT The in vitro activities of two novel azole compounds (aryl-1,2,4-triazol-3-ylthio analogues of fluconazole [ATTAFs]) and five comparator antifungal agents against 52 clinical Candida isolates from 5 different species were determined. The novel azole compounds had the lowest geometric mean MICs, followed by fluconazole. Moreover, combinations of these compounds with fluconazole exhibited synergistic effects against fluconazole-susceptible (22 of 23 isolates), fluconazole-susceptible dose-dependent (10 of 13 isolates), and fluconazole-resistant (1 of 16 isolates) Candida isolates.

scholarly journals The Investigational Fungal Cyp51 Inhibitor VT-1129 Demonstrates PotentIn VitroActivity against Cryptococcus neoformans and Cryptococcus gattii

2016 ◽  
Vol 60 (4) ◽  
pp. 2528-2531 ◽  
Author(s):  
Shawn R. Lockhart ◽  
Annette W. Fothergill ◽  
Naureen Iqbal ◽  
Carol B. Bolden ◽  
Nina T. Grossman ◽  
...  
Keyword(s):  
Cryptococcus Neoformans ◽  
Geometric Mean ◽  
Cryptococcus Gattii ◽  
The Novel ◽  
Content Type ◽  
Large Panel

ABSTRACTThein vitroactivities of the novel fungal Cyp51 inhibitor VT-1129 were evaluated against a large panel ofCryptococcus neoformansandCryptococcus gattiiisolates. VT-1129 demonstrated potent activities against bothCryptococcusspecies as demonstrated by low MIC50and MIC90values. ForC. gattii, thein vitropotency was maintained against all genotypes. In addition, significantly lower geometric mean MICs were observed for VT-1129 than for fluconazole againstC. neoformans, including isolates with reduced fluconazole susceptibility.

scholarly journals In Vitro Susceptibility of Thai Pythium insidiosum Isolates to Antibacterial Agents

2020 ◽  
Vol 64 (4) ◽  
Author(s):  
Navaporn Worasilchai ◽  
Ariya Chindamporn ◽  
Rongpong Plongla ◽  
Pattama Torvorapanit ◽  
Kasama Manothummetha ◽  
...  
Keyword(s):  
Antibacterial Agents ◽  
Antifungal Agents ◽  
Radical Surgery ◽  
Synergistic Effects ◽  
In Vitro Susceptibility ◽  
Pythium Insidiosum ◽  
Content Type ◽  
Life Threatening ◽  
Report Data

ABSTRACT Human pythiosis is a life-threatening human disease caused by Pythium insidiosum. In Thailand, vascular pythiosis is the most common form and carries a mortality rate of 10 to 40%, despite aggressive treatment with radical surgery, antifungal agents, and immunotherapy. Itraconazole and terbinafine have been the mainstay of treatment, until recently, based on case report data showing potential synergistic effects against Brazilian P. insidiosum isolates. However, the synergistic effects of itraconazole and terbinafine against Thai P. insidiosum isolates were not observed. This study tested the in vitro susceptibilities of 27 Thai human P. insidiosum isolates (clade II, n = 17; clade IV, n = 10), 12 Thai environmental P. insidiosum isolates (clade II, n = 4; clade IV, n = 8), and 11 non-Thai animal P. insidiosum isolates (clade I, n = 9; clade II, n = 2) to antibiotics in eight antibacterial classes to evaluate alternative effective treatments. Tetracycline and macrolide antibiotics demonstrated in vitro activity against Thai P. insidiosum isolates, with doxycycline MICs (1 to 16 μg/ml), minocycline MICs (1 to 4 μg/ml), tigecycline MICs (1 to 4 μg/ml), azithromycin MICs (1 to 16 μg/ml), and clarithromycin MICs (0.125 to 8 μg/ml) being the lowest, on average. Synergistic effects of tetracyclines and macrolides were also observed.

scholarly journals In VitroInteractions between Target of Rapamycin Kinase Inhibitor and Antifungal Agents against Aspergillus Species

2016 ◽  
Vol 60 (6) ◽  
pp. 3813-3816 ◽  
Author(s):  
Lujuan Gao ◽  
Xiaozhen Ding ◽  
Zhun Liu ◽  
Qingzhi Wu ◽  
Tongxiang Zeng ◽  
...  
Keyword(s):  
Amphotericin B ◽  
Aspergillus Flavus ◽  
Antifungal Agents ◽  
Kinase Inhibitor ◽  
Synergistic Effects ◽  
Target Of Rapamycin ◽  
Broth Microdilution ◽  
Content Type ◽  
Tor Kinase

In vitrointeractions of INK128, a target of rapamycin (TOR) kinase inhibitor, and antifungals, including itraconazole, voriconazole, posaconazole, amphotericin B, and caspofungin, againstAspergillusspp. were assessed with the broth microdilution checkerboard technique. Our results suggested synergistic effects between INK128 and all azoles tested, against multipleAspergillus fumigatusandAspergillus flavusisolates. However, no synergistic effects were observed when INK128 was combined with amphotericin B or caspofungin. No antagonism was observed for any combination.

scholarly journals In Vitro Antifungal Activity of Luliconazole, Efinaconazole, and Nine Comparators Against Aspergillus and Candida Strains Isolated from Otomycosis

2021 ◽  
Vol 14 (4) ◽  
Author(s):  
Gholamreza Shokoohi ◽  
Reza Rouhi ◽  
Mohammad Etehadnezhad ◽  
Bahram Ahmadi ◽  
Javad Javidnia ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Candida Species ◽  
Fungal Pathogens ◽  
Antifungal Agents ◽  
Geometric Mean ◽  
Antifungal Drugs ◽  
High Recurrence Rate ◽  
Broth Microdilution ◽  
In Vitro Antifungal Activity

Background: Aspergillus and Candida species are the most commonly identified fungal pathogens in otomycosis. However, we usually encounter some difficulties in its treatment because many patients show resistance to antifungal agents and present a high recurrence rate. Objectives: The current research was conducted to compare the in vitro activities of luliconazole (LUL), and efinaconazole (EFN) and the nine comparators on Aspergillus and Candida strains isolated from otomycosis. Methods: The in vitro activities of nine common antifungal drugs (amphotericin B (AMB), voriconazole (VRC), fluconazole (FLU), itraconazole (ITC), ketoconazole (KTO), clotrimazole (CLO), nystatin (NYS), terbinafine (TRB), and caspofungin (CAS)) and two novel new azoles (LUL and EFN) against of 108 clinical isolates of Aspergillus and Candida species obtained from otomycosis were assessed according to the CLSI broth microdilution document. Results: The LUL and EFN had the geometric mean minimum inhibitory concentrations (GM MICs) of 0.098 and 0.109 μg/mL against all Aspergillus strains, respectively. Furthermore, the GM MICs of all Candida isolates for LUL, EFN, CAS, CLO, VRC, AMB, ITC, KTO, FLU, NYS, and TRB were calculated to be 0.133, 0.144, 0.194, 0.219, 0.475, 0.537, 0.655, 1.277, 4.905, 9.372, and 13.592 μg/mL, respectively. Additionally, 6 (35.29%), 2 (11.7%), and 1 (5.88%) Candida isolates were resistant to FLU, CAS, and VRC, respectively. Conclusions: As the findings indicated, LUL and EFN showed the lowest GM MIC values against the examined species. Accordingly, these novel imidazole and triazole antifungal agents can be regarded as proper candidates for the treatment of otomycosis caused by Aspergillus and Candida strains.

scholarly journals In VitroActivity of Isavuconazole against Rasamsonia Species

2016 ◽  
Vol 60 (11) ◽  
pp. 6890-6891 ◽  
Author(s):  
J. Steinmann ◽  
S. Dittmer ◽  
J. Houbraken ◽  
J. Buer ◽  
P.-M. Rath
Keyword(s):  
Species Complex ◽  
Antifungal Agents ◽  
Effective Concentration ◽  
Antifungal Drugs ◽  
The Novel ◽  
Large Collection ◽  
Minimum Effective Concentration ◽  
Content Type

ABSTRACTThein vitrosusceptibilities to the novel triazole isavuconazole and six other antifungal agents of a large collection ofRasamsoniaisolates (n= 47) belonging to seven species were determined. Isavuconazole and voriconazole had noin vitroactivity (MIC, >32 mg/liter) against isolates of theRasamsoniaargillaceaspecies complex. The echinocandins were the most potent antifungal drugs against all of the isolates tested (minimum effective concentration, ≤0.19 mg/liter).

Susceptibility of uncommon Candida species to systemic antifungals by the EUCAST methodology

2019 ◽  
Vol 58 (6) ◽  
pp. 848-851 ◽  
Author(s):  
Judith Díaz-García ◽  
Luis Alcalá ◽  
Pablo Martín-Rabadán ◽  
Aina Mesquida ◽  
Carlos Sánchez-Carrillo ◽  
...  
Keyword(s):  
Point Mutation ◽  
Candida Species ◽  
Antifungal Agents ◽  
Wild Type ◽  
In Vitro Susceptibility ◽  
Susceptibility Data ◽  
Fluconazole Resistant ◽  
Type C

Abstract The incidence of infections by uncommon Candida species has increased in recent years, however, in vitro susceptibility data are scarce. Here we assess the susceptibility of C. krusei, C. dubliniensis, C. lusitaniae, and C. guilliermondii complex isolates (n = 120) to antifungal agents by the EUCAST methodology. C. dubliniensis proved to be the most susceptible species, similar to that of C. albicans (P < .05), whereas C. guilliermondii was the least susceptible. Two C. krusei isolates were echinocandin-resistant and harbored a point mutation (L701M) in the FKS1. Some isolates were either fluconazole-resistant (C. lusitaniae, n = 2) or fluconazole non-wild type (C. guilliermondii, n = 3).

scholarly journals In Vitro Antifungal Activity of Novel Triazole Efinaconazole and Five Comparators against Dermatophyte Isolates

2018 ◽  
Vol 62 (5) ◽  
Author(s):  
Ali Rezaei-Matehkolaei ◽  
Sadegh Khodavaisy ◽  
Mohamad Mahdi Alshahni ◽  
Takashi Tamura ◽  
Kazuo Satoh ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Trichophyton Rubrum ◽  
Geometric Mean ◽  
Clinical Isolates ◽  
The Novel ◽  
Large Collection ◽  
Content Type ◽  
Trichophyton Interdigitale ◽  
In Vitro Antifungal Activity

ABSTRACT The objective of this study was to assess the in vitro activity of the novel triazole antifungal drug, efinaconazole, and five comparators (luliconazole, lanoconazole, terbinafine, itraconazole, and fluconazole) against a large collection of Trichophyton interdigitale and Trichophyton rubrum clinical isolates. The geometric mean MICs were the lowest for luliconazole (0.0005 μg/ml), followed by lanoconazole (0.002 μg/ml), efinaconazole (0.007 μg/ml), terbinafine (0.011 μg/ml), itraconazole (0.095 μg/ml), and fluconazole (12.77 μg/ml). It appears that efinaconazole, lanoconazole, and luliconazole are promising candidates for the treatment of dermatophytosis due to T. interdigitale and T. rubrum .

scholarly journals Antifungal Susceptibility of Emerging Dimorphic Pathogens in the Family Ajellomycetaceae

2017 ◽  
Vol 62 (1) ◽  
Author(s):  
Karolina Dukik ◽  
Abdullah M. S. Al-Hatmi ◽  
Ilse Curfs-Breuker ◽  
Dirk Faro ◽  
Sybren de Hoog ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Antifungal Agents ◽  
Geometric Mean ◽  
Antifungal Susceptibility ◽  
Effective Concentration ◽  
Dimorphic Fungi ◽  
Minimum Effective Concentration ◽  
Content Type ◽  
The Family

ABSTRACT The in vitro susceptibilities of 24 molecularly identified dimorphic fungi belonging to the genera Adiaspiromyces, Blastomyces, and Emergomyces within the family Ajellomycetaceae were tested against 8 standard antifungal agents using CLSI document M38-A2. Amphotericin B and posaconazole had the lowest geometric mean MICs (<0.05 μg/ml) followed by itraconazole (<0.07 μg/ml), voriconazole (<0.15 μg/ml), and isavuconazole (<0.42 μg/ml) while fluconazole was not active. Micafungin demonstrated good in vitro antifungal activity against Emergomyces (geometric mean minimum effective concentration [GM MEC] 0.1 μg/ml) and Blastomyces (GM MEC <0.017 μg/ml).

scholarly journals In VitroActivities of Hexaazatrinaphthylenes against Leishmania spp.

2015 ◽  
Vol 59 (5) ◽  
pp. 2867-2874 ◽  
Author(s):  
Atteneri López-Arencibia ◽  
Daniel García-Velázquez ◽  
Carmen M. Martín-Navarro ◽  
Ines Sifaoui ◽  
María Reyes-Batlle ◽  
...  
Keyword(s):  
Therapeutic Agents ◽  
Content Type ◽  
Inhibition Effect ◽  
Intracellular Amastigotes ◽  
Dependent Inhibition ◽  
Leishmania Spp ◽  
Dose Dependent Inhibition ◽  
Dose Dependent ◽  
Potential Use

ABSTRACTThein vitroactivity of a novel group of compounds, hexaazatrinaphthylene derivatives, against two species ofLeishmaniais described in this study. These compounds showed a significant dose-dependent inhibition effect on the proliferation of the parasites, with 50% inhibitory concentrations (IC50s) ranging from 1.23 to 25.05 μM against the promastigote stage and 0.5 to 0.7 μM against intracellular amastigotes. Also, a cytotoxicity assay was carried out to in order to evaluate the possible toxic effects of these compounds. Moreover, different assays were performed to determine the type of cell death induced after incubation with these compounds. The obtained results highlight the potential use of hexaazatrinaphthylene derivatives againstLeishmaniaspecies, and further studies should be undertaken to establish them as novel leishmanicidal therapeutic agents.

scholarly journals Fluconazole MIC and the Fluconazole Dose/MIC Ratio Correlate with Therapeutic Response among Patients with Candidemia

2005 ◽  
Vol 49 (8) ◽  
pp. 3171-3177 ◽  
Author(s):  
Cornelius J. Clancy ◽  
Victor L. Yu ◽  
Arthur J. Morris ◽  
David R. Snydman ◽  
M. Hong Nguyen
Keyword(s):  
Therapeutic Response ◽  
Geometric Mean ◽  
Therapeutic Failure ◽  
Response To Therapy ◽  
Success Rates ◽  
Therapeutic Success ◽  
Data Set ◽  
In Vitro Susceptibility ◽  
Dose Dependent

ABSTRACT We tested 32 Candida isolates recovered in the early 1990s from the bloodstreams of patients with candidemia for in vitro susceptibility to fluconazole and determined if MIC and/or the daily dose of fluconazole/MIC ratio correlated with the response to therapy. This is a unique data set since 87.5% (28/32) of patients were treated with fluconazole doses now considered to be inadequate (≤200 mg), which contributed to high therapeutic failure rates (53% [17/32]). The geometric mean MIC and dose/MIC ratio for isolates associated with therapeutic failure (11.55 μg/ml and 14.3, respectively) differed significantly from values associated with therapeutic success (0.95 μg/ml and 219.36 [P = 0.0009 and 0.0004, respectively]). The therapeutic success rates among patients infected with susceptible (MIC ≤ 8 μg/ml), susceptible-dose dependent (S-DD) (MIC = 16 or 32 μg/ml), and resistant (MIC ≥ 64 μg/ml) isolates were 67% (14/21), 20% (1/5), and 0% (0/6), respectively. A dose/MIC ratio >50 was associated with a success rate of 74% (14/19), compared to 8% (1/13) for a dose/MIC ratio ≤50 (P = 0.0003). Our data suggest that both fluconazole MIC and dose/MIC ratio correlate with the therapeutic response to fluconazole among patients with candidemia. In clinical practice, dose/MIC ratio might prove easier to interpret than breakpoint MICs, since it quantitates the effects of increasing fluconazole doses that are alluded to in the S-DD designation.

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