Potent Activities of Novel Imidazoles Lanoconazole and Luliconazole against a Collection of Azole-Resistant and -Susceptible Aspergillus fumigatus Strains

Abastabar, Mahdi; Rahimi, Nooshin; Meis, Jacques F.; Aslani, Narges; Khodavaisy, Sadegh; Nabili, Mojtaba; Rezaei‐Matehkolaei, Ali; Makimura, Koichi; Badali, Hamid

doi:10.1128/aac.01193-16

Cited by 38 publications

(20 citation statements)

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“…Luliconazole and lanoconazole are novel topical FDA-approved imidazoles for treatment of superficial mycoses. These drugs have proven in vitro activity against most clinically important molds and yeasts, e.g., Aspergillus fumigatus (including strains with acquired itraconazole resistance) (19), Aspergillus terreus species complex (20), dermatophytes (21), black fungi and relatives (22), Malassezia species (23), and Candida species (24). No in vitro susceptibility data of luliconazole and lanoconazole against Fusarium species have been published.…”

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confidence: 99%

Potent Activities of Luliconazole, Lanoconazole, and Eight Comparators against Molecularly Characterized Fusarium Species

Abastabar

Al‐Hatmi

Moghaddam

et al. 2018

Antimicrob Agents Chemother

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A collection of clinical ( = 47) and environmental ( = 79) isolates were tested against 10 antifungal drugs, including 2 novel imidazoles. Luliconazole and lanoconazole demonstrated very low geometric mean MIC values of 0.005 and 0.013 μg/ml, respectively, compared with 0.51 μg/ml for micafungin, 0.85 μg/ml for efinaconazole, 1.12 μg/ml for natamycin, 1.18 μg/ml for anidulafungin, 1.31 μg/ml for voriconazole, 1.35 μg/ml for caspofungin, 1.9 μg/ml for amphotericin B, and 4.08 μg/ml for itraconazole. Results show that these drugs are potential candidates for (topical) treatment of skin and nail infections due to species.

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confidence: 99%

Potent Activities of Luliconazole, Lanoconazole, and Eight Comparators against Molecularly Characterized Fusarium Species

Abastabar

Al‐Hatmi

Moghaddam

et al. 2018

Antimicrob Agents Chemother

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“…Moreover, new imidazoles, such as lanoconazole and luliconazole, strongly inhibit the growth of Aspergillus spp. [4,5]. An additional challenge is the presence of Aspergillus biofilms, which are thought to contribute to virulence in IA and aspergilloma [6].…”

Section: Introductionmentioning

confidence: 99%

Synergistic effects of vorinostat (SAHA) and azoles against Aspergillus species and their biofilms

Yin

2020

BMC Microbiol

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Background: Invasive aspergillosis is a fungal infection that occurs mainly in immunocompromised patients. It is responsible for a high degree of mortality and is invariably unresponsive to conventional antifungal treatments. Histone deacetylase inhibitors can affect the cell cycle, apoptosis and differentiation. The histone deacetylase inhibitor vorinostat (SAHA) has recently received approval for the treatment of cutaneous T cell lymphoma. Here, we investigated the interactions of SAHA and itraconazole, voriconazole, and posaconazole against Aspergillus spp. in vitro using both planktonic cells and biofilms. Results: We investigated 20 clinical strains using broth microdilution checkerboard methods. The results showed synergy between SAHA and itraconazole, voriconazole, and posaconazole against 60, 40, and 25% of tested isolates of planktonic Aspergillus spp., respectively. Similar synergy was also observed against Aspergillus biofilms. The expression of the azole-associated multidrug efflux pumps MDR1, MDR2, MDR3 and MDR4, as well as that of HSP90, was measured by RT-PCR. The results indicated that the molecular mechanism of the observed synergistic effects in Aspergillus fumigatus may be partly associated with dampened expression of the efflux pump genes and, furthermore, that HSP90 suppression may be a major contributor to the observed synergistic effects of the drugs.Conclusions: SAHA has potential as a secondary treatment to enhance the effects of azoles against both biofilm and planktonic cells of Aspergillus spp. in vitro. This effect occurs mostly by inhibition of HSP90 expression.

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“…Luliconazole, (-)-(E)-[(4R)-4-(2, 4-dichlorophenyl)-1, 3-dithiolan-2-ylidene] (1H63imidazol-1-yl) acetonitrile, is a new synthetic imidazole antifungal. Luliconazole was firstly synthesized by Nihon Nohyaku Co Ltd in Japan in 2005 and similar to other common azoles, it is effective on ergosterol biosynthesis with fewer side effects and greater potency (1,2). Luliconazole initially available as topical cream (LUZU) 1% for dermatophytosis and solution 10% for onychomycosis (1,3,4).…”

Section: Introductionmentioning

confidence: 99%

“…Luliconazole initially available as topical cream (LUZU) 1% for dermatophytosis and solution 10% for onychomycosis (1,3,4). A very low minimum inhibitory concentration (MIC) of luliconazole for dermatophytes, Candida, Fusarium and Aspergillus species has been reported (2,(5)(6)(7).…”

Section: Introductionmentioning

confidence: 99%

“…In addition, A. flavus is one of the most important otomycosis agents (18). On the other hand, intrinsic and acquired azole -resistance have predominantly been reported for several Aspergillus species comprise A. fumigatus, A. flavus, A. niger, A. terreus and A. lentulus in vitro (2,13,19,20). Moreover, resistant to amphotericin B in invasive aspergillosis has been reported for different Aspergillus species including A. flavus (21,22).…”

Section: Introductionmentioning

confidence: 99%

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The high efficacy of luliconazole against environmental and otomycosis Aspergillus flavus strains

Moslem

Mahmoudabadi

2020

IJM

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Background and Objectives: Luliconazole is currently confirmed for the topical therapy of dermatophytosis. Moreover, it is found that luliconazole has in vitro activity against some molds and yeast species. The aim of the present study was to evaluate the efficacy of luliconazole in comparison to routine used antifungals on clinical and environmental isolates of Aspergillus flavus. Materials and Methods: Thirty eight isolates of A. flavus (18 environmental and 20 clinical isolates) were detected based on morphological and microscopic features and also PCR-sequencing of β-tubulin ribosomal DNA gene. All the isolates were tested against luliconazole, voriconazole, amphotericin B and caspofungin. Minimum inhibitory concentration (MIC), 90 MIC50, MIC isolates. and MIC Geometric (GM) were calculated using CLSI M38-A2 protocol for both environmental and clinical GM Results: Luliconazole with extremely low MIC range, 0.00049-0.00781 μg/mL and MIC 0.00288 μg/mL showed very strong activity against both clinical and environmental A. flavus isolates. Moreover, voriconazole inhibited 100% of isolates at defined epidemiological cutoff values (ECV ≤ 2 µg/ml). 50% and 27.8% of clinical and environmental isolates of A. flavus, were resistant to caspofungin, respectively. Whereas, all the isolates were found to be resistant to amphotericin B. GM Conclusion: The analysis of our data clearly indicated that luliconazole (with MIC 0.00244 µg/ml for clinical and 0.00336 μg/ml for environmental isolates) had the highest in vitro activity against A. flavus strains.

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Potent Activities of Novel Imidazoles Lanoconazole and Luliconazole against a Collection of Azole-Resistant and -Susceptible Aspergillus fumigatus Strains

Cited by 38 publications

References 20 publications

Potent Activities of Luliconazole, Lanoconazole, and Eight Comparators against Molecularly Characterized Fusarium Species

Potent Activities of Luliconazole, Lanoconazole, and Eight Comparators against Molecularly Characterized Fusarium Species

Synergistic effects of vorinostat (SAHA) and azoles against Aspergillus species and their biofilms

The high efficacy of luliconazole against environmental and otomycosis Aspergillus flavus strains

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