Page last updated: 2024-12-08

albaconazole

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Description

albaconazole: UR-9825 is the (1R,2R)-isomer; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID208952
CHEMBL ID298817
SCHEMBL ID1262830
MeSH IDM0290738

Synonyms (37)

Synonym
7-chloro-3-((1r,2r)-2-(2,4-difluorophenyl)-2-hydroxy-1-methyl-3-(1h-1,2,4-triazol-1-yl)propyl)quinazolin-4(3h)-one
ur-9825
w-0027
albaconazole
7-chloro-3-[(1r,2r)-2-(2,4-difluorophenyl)-2-hydroxy-1-methyl-3-(1,2,4-triazol-1-yl)propyl]quinazolin-4-one
CHEMBL298817
w0027 ,
187949-02-6
7-chloro-3-[(2r,3r)-3-(2,4-difluorophenyl)-3-hydroxy-4-(1,2,4-triazol-1-yl)butan-2-yl]quinazolin-4-one
albaconazol
4(3h)-quinazolinone, 7-chloro-3-((1r,2r)-2-(2,4-difluorophenyl)-2-hydroxy-1-methyl-3-(1h-1,2,4-triazol-1-yl)propyl)-
ur 9825
7-chloro-3-(2-(2,4-difluorophenyl)-2-hydroxy-1-methyl-3-(1h-1,2,4-triazol-1-yl)propyl)quinazolin-4(3h)-one
albaconazole [usan:inn]
unii-ydw24y8iab
ydw24y8iab ,
albaconazol [inn-spanish]
albaconazole (usan/inn)
D09702
(1r,2r)-7-chloro-3-[2-(2,4-difluorophenyl)-2-hydroxy-1-methyl-3-(1h-1,2, 4-triazol-1-yl)propyl]quinazolin-4(3h)-one
(1r,2r)-7-chloro-3-[2-(2,4-difluorophenyl)-2-hydroxy-1-methyl-3-(1h-1,2,4-triazol-1-yl)propyl]quinazolin-4(3h)-one
UHIXWHUVLCAJQL-MPBGBICISA-N
albaconazole [usan]
7-chloro-3-[(1r,2r)-2-(2,4-difluorophenyl)-2-hydroxy-1-methyl-3-(1h-1,2,4-triazol-1-yl)propyl]quinazolin-4(3h)-one
albaconazole [inn]
SCHEMBL1262830
DTXSID3058244
bdbm50011477
AKOS027327579
J-012103
DB12073
Q4708967
7-chloro-3-((2r,3r)-3-(2,4-difluorophenyl)-3-hydroxy-4-(1h-1,2,4-triazol-1-yl)butan-2-yl)quinazolin-4(3h)-one
ur 9625; ur 9825
ur9825
w 0027
4(3h)-quinazolinone, 7-chloro-3-[(1r,2r)-2-(2,4-difluorophenyl)-2-hydroxy-1-methyl-3-(1h-1,2,4-triazol-1-yl)propyl]-

Research Excerpts

Overview

Albaconazole is an experimental triazole derivative with potent and broad-spectrum antifungal activity. It has a remarkably long half-life in dogs, monkeys, and humans.

ExcerptReferenceRelevance
"Albaconazole is an experimental triazole derivative with potent and broad-spectrum antifungal activity and a remarkably long half-life in dogs, monkeys, and humans. "( Activity of the new triazole derivative albaconazole against Trypanosoma (Schizotrypanum) cruzi in dog hosts.
Afonso, LC; Bahia, MT; Chiari, E; de Lana, M; Guedes, PM; Machado-Coelho, GL; Tafuri, WL; Urbina, JA; Veloso, VM, 2004
)
2.03

Effects

ExcerptReferenceRelevance
"Albaconazole has also shown very potent activity against species of Candida, Cryptococcus and Aspergillus."( New and emerging treatments for fungal infections.
Denning, DW; Pasqualotto, AC, 2008
)
1.07

Toxicity

ExcerptReferenceRelevance
" However, frequent repeated dosing is required, and hepatic and cardiac adverse events may occur."( A phase II, randomized, double-blind, placebo-controlled, parallel group, dose-ranging study to investigate the efficacy and safety of 4 dose regimens of oral albaconazole in patients with distal subungual onychomycosis.
Malahias, S; Raterink, K; Sigurgeirsson, B; van Rossem, K, 2013
)
0.59
" Most adverse events were mild or moderate, and treatment-related adverse events were all ≤3%."( A phase II, randomized, double-blind, placebo-controlled, parallel group, dose-ranging study to investigate the efficacy and safety of 4 dose regimens of oral albaconazole in patients with distal subungual onychomycosis.
Malahias, S; Raterink, K; Sigurgeirsson, B; van Rossem, K, 2013
)
0.59

Bioavailability

ExcerptReferenceRelevance
" Reduced toxicity, enhancement of bioavailability and counteraction of resistance are features desired by clinicians."( Newer antifungal agents.
Türel, O, 2011
)
0.37

Dosage Studied

ExcerptRelevanceReference
" Its extended half-life probably permits dosing less frequently than once a day."( New and emerging treatments for fungal infections.
Denning, DW; Pasqualotto, AC, 2008
)
0.35
" However, frequent repeated dosing is required, and hepatic and cardiac adverse events may occur."( A phase II, randomized, double-blind, placebo-controlled, parallel group, dose-ranging study to investigate the efficacy and safety of 4 dose regimens of oral albaconazole in patients with distal subungual onychomycosis.
Malahias, S; Raterink, K; Sigurgeirsson, B; van Rossem, K, 2013
)
0.59
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)34.86000.00091.901410.0000AID1138338
Sterol 14-alpha demethylaseTrypanosoma cruzi strain CL BrenerIC50 (µMol)0.00100.00101.707010.0000AID1915709
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (22)

Processvia Protein(s)Taxonomy
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (12)

Processvia Protein(s)Taxonomy
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (5)

Processvia Protein(s)Taxonomy
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (110)

Assay IDTitleYearJournalArticle
AID167736In vivo antifungal activity against systemic candidosis in rabbit kidney at a dose of 12.5 mg/kg, qd, po.1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
AID1651348Antifungal activity against fluconazole-resistant Candida albicans isolate 100 by NCCLS protocol based broth microdilution method2020Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4
Design, synthesis, and structure-activity relationship studies of novel triazole agents with strong antifungal activity against Aspergillus fumigatus.
AID562993Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 5 mg/kg, administered through oral gavage once daily for 5 days measured on day 6 post inoculation2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Efficacy of albaconazole against Candida albicans in a vaginitis model.
AID432803Antifungal activity against Sporothrix albicans after 72 hrs by microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro antifungal susceptibilities of five species of sporothrix.
AID725869Antifungal activity against Rhizomucor pusillus RHMI1 after 48 hrs by broth microdilution test2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a novel broad-spectrum antifungal agent derived from albaconazole.
AID165452In vivo antifungal activity against systemic candidosis in rabbit lung at a dose of 2.5 mg/kg, qd, po.1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
AID123517The compound was tested in vivo for anti-candida activity in mice model 1 (dose :0.5 mg/kg,fluconazole-treated group)1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
AID562989Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 20 mg/kg, administered through oral gavage once daily for 5 days measured on day 6 post inoculation2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Efficacy of albaconazole against Candida albicans in a vaginitis model.
AID1247371Antifungal activity against Candida parapsilosis 22019 after 24 hrs by serial dilution method2015European journal of medicinal chemistry, Sep-18, Volume: 102Design, synthesis, and structure-activity relationship studies of novel thienopyrrolidone derivatives with strong antifungal activity against Aspergillus fumigates.
AID307397Antifungal activity against Candida lusitaniae ATCC 42720 by broth microdilution assay2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery of novel indazole-linked triazoles as antifungal agents.
AID307400Antifungal activity against Aspergillus fumigatus ATCC 16424 by broth microdilution assay2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery of novel indazole-linked triazoles as antifungal agents.
AID118766In vivo antifungal activity against murine candidosis model after peroral administration with 0.5 mg/kg at various time intervals. (percent protection for 100% mortality with untreated group)1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
AID307398Antifungal activity against Candida tropicalis ATCC 750 by broth microdilution assay2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery of novel indazole-linked triazoles as antifungal agents.
AID307394Antifungal activity against Candida glabrata ATCC 34138 by broth microdilution assay2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery of novel indazole-linked triazoles as antifungal agents.
AID725871Antifungal activity against Scedosporium sp. SCSP1 after 48 hrs by broth microdilution test2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a novel broad-spectrum antifungal agent derived from albaconazole.
AID1651344Antifungal activity against Candida albicans Y0109 by NCCLS protocol based broth microdilution assay2020Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4
Design, synthesis, and structure-activity relationship studies of novel triazole agents with strong antifungal activity against Aspergillus fumigatus.
AID167735In vivo antifungal activity against systemic candidosis in rabbit kidney at a dose of 0.5 mg/kg, qd, po.1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
AID525140Antifungal activity against Fusarium moniliforme clade 2 by microdilution method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
In vitro antifungal susceptibility and molecular characterization of clinical isolates of Fusarium verticillioides (F. moniliforme) and Fusarium thapsinum.
AID725874Antifungal activity against Aspergillus fumigatus ASFU20 after 48 hrs by M38 method2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a novel broad-spectrum antifungal agent derived from albaconazole.
AID1138333Antimicrobial activity against fluconazole-resistant Candida albicans 100 after 24 hrs by serial dilution method2014Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility.
AID1247369Antifungal activity against Candida albicans SC5314 after 24 hrs by serial dilution method2015European journal of medicinal chemistry, Sep-18, Volume: 102Design, synthesis, and structure-activity relationship studies of novel thienopyrrolidone derivatives with strong antifungal activity against Aspergillus fumigates.
AID220226In vitro for antifungal activity against 10 yeasts1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
AID562994Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 40 mg/kg, administered through oral gavage twice daily for 5 days measured on day 1 post inoculation2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Efficacy of albaconazole against Candida albicans in a vaginitis model.
AID562990Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 10 mg/kg, administered through oral gavage twice daily for 5 days measured on day 6 post inoculation2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Efficacy of albaconazole against Candida albicans in a vaginitis model.
AID1247374Antifungal activity against Aspergillus fumigatus 7544 after 48 hrs by serial dilution method2015European journal of medicinal chemistry, Sep-18, Volume: 102Design, synthesis, and structure-activity relationship studies of novel thienopyrrolidone derivatives with strong antifungal activity against Aspergillus fumigates.
AID1138335Antimicrobial activity against fluconazole-resistant Candida albicans J18 after 24 hrs by serial dilution method2014Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility.
AID725882Antifungal activity against Candida krusei CAKR7 after 24 hrs by spectrofluorometric analysis2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a novel broad-spectrum antifungal agent derived from albaconazole.
AID563001Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 5 mg/kg, administered through oral gavage once daily for 5 days measured on day 1 post inoculation2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Efficacy of albaconazole against Candida albicans in a vaginitis model.
AID562987Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 40 mg/kg, administered through oral gavage once daily for 5 days measured on day 6 post inoculation2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Efficacy of albaconazole against Candida albicans in a vaginitis model.
AID307403Antifungal activity against Aspergillus niger ATCC 9042 by broth microdilution assay2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery of novel indazole-linked triazoles as antifungal agents.
AID1651345Antifungal activity against Candida parapsilosis 22019 by NCCLS protocol based broth microdilution assay2020Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4
Design, synthesis, and structure-activity relationship studies of novel triazole agents with strong antifungal activity against Aspergillus fumigatus.
AID26407Half-life in rats after iv administration1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
AID432799Antifungal activity against Sporothrix brasiliensis after 72 hrs by microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro antifungal susceptibilities of five species of sporothrix.
AID562998Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 10 mg/kg, administered through oral gavage twice daily for 5 days measured on day 1 post inoculation2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Efficacy of albaconazole against Candida albicans in a vaginitis model.
AID725881Antifungal activity against Candida krusei CAKR8 after 24 hrs by spectrofluorometric analysis2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a novel broad-spectrum antifungal agent derived from albaconazole.
AID307399Antifungal activity against Candida parapsilosis ATCC 21019 by broth microdilution assay2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery of novel indazole-linked triazoles as antifungal agents.
AID432801Antifungal activity against Sporothrix globosa after 72 hrs by microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro antifungal susceptibilities of five species of sporothrix.
AID195068In vivo activity against disseminated aspergillosis (liver) in immunocompromized rat model at a dose of 1 mg/kg, bid, po1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
AID73614In vitro antifungal activity against 6 filamentous fungi1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
AID562996Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 20 mg/kg, administered through oral gavage twice daily for 5 days measured on day 1 post inoculation2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Efficacy of albaconazole against Candida albicans in a vaginitis model.
AID563000Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 5 mg/kg, administered through oral gavage twice daily for 5 days measured on day 1 post inoculation2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Efficacy of albaconazole against Candida albicans in a vaginitis model.
AID118757In vivo antifungal activity against murine candidosis model after peroral administration with 0.25 mg/kg at various time intervals. (percent protection for 100% mortality with untreated group); not tested1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
AID1138336Antimicrobial activity against fluconazole-resistant Candida albicans J28 after 24 hrs by serial dilution method2014Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility.
AID725877Antifungal activity against Aspergillus fumigatus ASFU13 after 48 hrs by M38 method2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a novel broad-spectrum antifungal agent derived from albaconazole.
AID1651343Antifungal activity against Aspergillus fumigatus 7544 by NCCLS protocol based broth microdilution assay2020Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4
Design, synthesis, and structure-activity relationship studies of novel triazole agents with strong antifungal activity against Aspergillus fumigatus.
AID1138338Inhibition of human ERG expressed in CHO cells by whole-cell patch clamp assay2014Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility.
AID118756In vivo antifungal activity against murine candidosis model after peroral administration with 0.25 mg/kg at various time intervals. (percent protection for 100% mortality with fluconazole-treated group.); not tested1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
AID432800Antifungal activity against Sporothrix schenckii after 72 hrs by microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro antifungal susceptibilities of five species of sporothrix.
AID118758In vivo antifungal activity against murine candidosis model after peroral administration with 0.5 mg/Kg at various time intervals. (percent protection for 100% mortality with fluconazole-treated group.)1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
AID562995Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 40 mg/kg, administered through oral gavage once daily for 5 days measured on day 1 post inoculation2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Efficacy of albaconazole against Candida albicans in a vaginitis model.
AID307401Antifungal activity against Aspergillus flavus ATCC MYA-1004 by broth microdilution assay2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery of novel indazole-linked triazoles as antifungal agents.
AID1247373Antifungal activity against Candida glabrata 537 after 24 hrs by serial dilution method2015European journal of medicinal chemistry, Sep-18, Volume: 102Design, synthesis, and structure-activity relationship studies of novel thienopyrrolidone derivatives with strong antifungal activity against Aspergillus fumigates.
AID562988Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 20 mg/kg, administered through oral gavage twice daily for 5 days measured on day 6 post inoculation2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Efficacy of albaconazole against Candida albicans in a vaginitis model.
AID118893In vivo antifungal activity against murine candidosis model after peroral administration with 1 mg/kg at various time intervals. (percent protection for 100% mortality with untreated group)1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
AID123519The compound was tested in vivo for anti-candida activity in mice model 2(dose: 5 mg/kg, untreated group).1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
AID525139Antifungal activity against Fusarium moniliforme clade 1 by microdilution method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
In vitro antifungal susceptibility and molecular characterization of clinical isolates of Fusarium verticillioides (F. moniliforme) and Fusarium thapsinum.
AID1138337Antimicrobial activity against fluconazole-resistant Candida albicans J38 after 24 hrs by serial dilution method2014Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility.
AID1651341Antifungal activity against Candida albicans SC5314 by NCCLS protocol based broth microdilution assay2020Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4
Design, synthesis, and structure-activity relationship studies of novel triazole agents with strong antifungal activity against Aspergillus fumigatus.
AID525141Antifungal activity against Fusarium moniliforme clade 3 by microdilution method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
In vitro antifungal susceptibility and molecular characterization of clinical isolates of Fusarium verticillioides (F. moniliforme) and Fusarium thapsinum.
AID562992Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 5 mg/kg, administered through oral gavage twice daily for 5 days measured on day 6 post inoculation2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Efficacy of albaconazole against Candida albicans in a vaginitis model.
AID525142Antifungal activity against Fusarium thapsinum by microdilution method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
In vitro antifungal susceptibility and molecular characterization of clinical isolates of Fusarium verticillioides (F. moniliforme) and Fusarium thapsinum.
AID1138330Antimicrobial activity against Cryptococcus neoformans 32609 after 72 hrs by serial dilution method2014Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility.
AID195069In vivo activity against disseminated aspergillosis (liver) in immunocompromized rat model at a dose of 25 mg/kg, bid, po1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
AID725880Antifungal activity against Candida glabrata CAGL2 after 24 hrs by spectrofluorometric analysis2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a novel broad-spectrum antifungal agent derived from albaconazole.
AID1247372Antifungal activity against Cryptococcus neoformans 32609 after 72 hrs by serial dilution method2015European journal of medicinal chemistry, Sep-18, Volume: 102Design, synthesis, and structure-activity relationship studies of novel thienopyrrolidone derivatives with strong antifungal activity against Aspergillus fumigates.
AID123520The compound was tested in vivo for anti-candida activity in mice model 2(dose :5 mg/kg,fluconazole-treated group)1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
AID123518The compound was tested in vivo for anti-candida activity in mice model 1(dose: 0.5 mg/kg, untreated group).1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
AID725886Antifungal activity against fluconazole-resistant Candida albicans DSY735 after 24 hrs by spectrofluorometric analysis2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a novel broad-spectrum antifungal agent derived from albaconazole.
AID432802Antifungal activity against Sporothrix mexicana after 72 hrs by microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro antifungal susceptibilities of five species of sporothrix.
AID1138331Antimicrobial activity against Candida glabrata 537 after 24 hrs by serial dilution method2014Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility.
AID1651342Antifungal activity against Cryptococcus neoformans 32605 by NCCLS protocol based broth microdilution assay2020Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4
Design, synthesis, and structure-activity relationship studies of novel triazole agents with strong antifungal activity against Aspergillus fumigatus.
AID195070In vivo activity against disseminated aspergillosis (liver) in immunocompromized rat model at a dose of 5 mg/kg, bid, po1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
AID725878Antifungal activity against acquired-resistant Candida parapsilosis CAPA2 after 24 hrs by spectrofluorometric analysis2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a novel broad-spectrum antifungal agent derived from albaconazole.
AID1651347Antifungal activity against Microsporum gypseum CMCC by NCCLS protocol based broth microdilution assay2020Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4
Design, synthesis, and structure-activity relationship studies of novel triazole agents with strong antifungal activity against Aspergillus fumigatus.
AID725870Antifungal activity against Rhizomucor pusillus RHPU1 after 48 hrs by broth microdilution test2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a novel broad-spectrum antifungal agent derived from albaconazole.
AID307395Antifungal activity against Candida krusei ATCC 6528 by broth microdilution assay2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery of novel indazole-linked triazoles as antifungal agents.
AID1247370Antifungal activity against Candida albicans Y0109 after 24 hrs by serial dilution method2015European journal of medicinal chemistry, Sep-18, Volume: 102Design, synthesis, and structure-activity relationship studies of novel thienopyrrolidone derivatives with strong antifungal activity against Aspergillus fumigates.
AID307393Antifungal activity against Candida albicans ATCC 36082 by broth microdilution assay2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery of novel indazole-linked triazoles as antifungal agents.
AID1138340Aqueous solubility of the compound in hydrochloric acid solution at pH 1.22014Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility.
AID1651349Antifungal activity against fluconazole-resistant Candida albicans isolate 103 by NCCLS protocol based broth microdilution method2020Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4
Design, synthesis, and structure-activity relationship studies of novel triazole agents with strong antifungal activity against Aspergillus fumigatus.
AID195071In vivo activity against disseminated aspergillosis (liver) in immunocompromized rat model at a dose of 50 mg/kg, bid, po1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
AID165450In vivo antifungal activity against systemic candidosis in rabbit lung at a dose of 0.5 mg/kg, qd, po.1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
AID167737In vivo antifungal activity against systemic candidosis in rabbit kidney at a dose of 2.5 mg/kg, qd, po.1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
AID1138341Aqueous solubility of the compound in phosphate buffer at pH 7.42014Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility.
AID562991Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 10 mg/kg, administered through oral gavage once daily for 5 days measured on day 6 post inoculation2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Efficacy of albaconazole against Candida albicans in a vaginitis model.
AID562997Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 20 mg/kg, administered through oral gavage once daily for 5 days measured on day 1 post inoculation2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Efficacy of albaconazole against Candida albicans in a vaginitis model.
AID725876Antifungal activity against Aspergillus fumigatus ASFU7 after 48 hrs by M38 method2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a novel broad-spectrum antifungal agent derived from albaconazole.
AID725873Antifungal activity against Aspergillus fumigatus ASFU19 after 48 hrs by M38 method2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a novel broad-spectrum antifungal agent derived from albaconazole.
AID563002Antifungal activity against Candida albicans isolate 03-2718 after 48 hrs2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Efficacy of albaconazole against Candida albicans in a vaginitis model.
AID725875Antifungal activity against Aspergillus fumigatus ASFU17 after 48 hrs by M38 method2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a novel broad-spectrum antifungal agent derived from albaconazole.
AID165451In vivo antifungal activity against systemic candidosis in rabbit lung at a dose of 12.5 mg/kg, qd, po.1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
AID1138332Antimicrobial activity against Aspergillus fumigatus 7544 after 48 hrs by serial dilution method2014Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility.
AID1138328Antimicrobial activity against Candida albicans Y0109 after 24 hrs by serial dilution method2014Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility.
AID1138334Antimicrobial activity against fluconazole-resistant Candida albicans 103 after 24 hrs by serial dilution method2014Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility.
AID49099The compound was tested in vitro for antifungal activity against Candida albicans.1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
AID1138327Antimicrobial activity against Candida albicans SC5314 after 24 hrs by serial dilution method2014Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility.
AID562999Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 10 mg/kg, administered through oral gavage once daily for 5 days measured on day 1 post inoculation2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Efficacy of albaconazole against Candida albicans in a vaginitis model.
AID725885Antifungal activity against fluconazole-susceptible Candida albicans CAAL93 after 24 hrs by spectrofluorometric analysis2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a novel broad-spectrum antifungal agent derived from albaconazole.
AID1138329Antimicrobial activity against Candida parapsilosis 22019 after 24 hrs by serial dilution method2014Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility.
AID562986Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 40 mg/kg, administered through oral gavage twice daily for 5 days measured on day 6 post inoculation2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Efficacy of albaconazole against Candida albicans in a vaginitis model.
AID1915709Inhibition of Trypanosoma cruzi Sterol 14-alpha demethylase2021European journal of medicinal chemistry, Feb-05, Volume: 211Therapeutic progression of quinazolines as targeted chemotherapeutic agents.
AID725872Antifungal activity against Aspergillus fumigatus ASFU23 after 48 hrs by M38 method2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a novel broad-spectrum antifungal agent derived from albaconazole.
AID307402Antifungal activity against Aspergillus terreus ATCC 28301by broth microdilution assay2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery of novel indazole-linked triazoles as antifungal agents.
AID1651346Antifungal activity against Candida glabrata 537 by NCCLS protocol based broth microdilution assay2020Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4
Design, synthesis, and structure-activity relationship studies of novel triazole agents with strong antifungal activity against Aspergillus fumigatus.
AID118889In vivo antifungal activity against murine candidosis model after peroral administration with 1 mg/kg at various time intervals. (percent protection for 100% mortality with fluconazole-treated group.)1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
AID725883Antifungal activity against fluconazole-resistant Candida albicans DSY292 after 24 hrs by spectrofluorometric analysis2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a novel broad-spectrum antifungal agent derived from albaconazole.
AID725884Antifungal activity against fluconazole-susceptible Candida albicans CAAL97 after 24 hrs by spectrofluorometric analysis2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a novel broad-spectrum antifungal agent derived from albaconazole.
AID15872Log P value of the compound.1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
AID307396Antifungal activity against Cryptococcus neoformans ATCC 21019 by broth microdilution assay2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery of novel indazole-linked triazoles as antifungal agents.
AID725879Antifungal activity against acquired-resistant Candida parapsilosis CAPA1 after 24 hrs by spectrofluorometric analysis2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a novel broad-spectrum antifungal agent derived from albaconazole.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (33)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's2 (6.06)18.2507
2000's20 (60.61)29.6817
2010's9 (27.27)24.3611
2020's2 (6.06)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 34.35

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index34.35 (24.57)
Research Supply Index3.58 (2.92)
Research Growth Index5.15 (4.65)
Search Engine Demand Index42.51 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (34.35)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (2.94%)5.53%
Reviews7 (20.59%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other26 (76.47%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (3)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Phase 1, Randomized, Open-Label, Crossover Safety and Pharmacokinetic Study of 400 mg Albaconazole as a Tablet Formulation Versus a Capsule Formulation in Healthy Subjects [NCT01039883]Phase 140 participants (Actual)Interventional2009-11-23Completed
A Phase 2, Randomized, Double-blind, Placebo-controlled, Parallel-group, Dose-ranging Study to Investigate the Efficacy and Safety of 4 Dose Regimens of Oral Albaconazole in Subjects With Distal Subungual Onychomycosis [NCT00730405]Phase 2582 participants (Actual)Interventional2008-07-16Completed
A Single-Blind, Randomized, Dose-Finding Study Versus Fluconazole to Assess the Efficacy and Tolerability of Five Single Doses of Albaconazole in the Treatment of Acute Non-Recurrent Candida Spp Vulvovaginitis [NCT00199264]Phase 260 participants Interventional2004-06-30Terminated
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00730405 (6) [back to overview]Absolute Change in Unaffected Part of Target Nail From Baseline to Week 52
NCT00730405 (6) [back to overview]The Percentage of Participants Who Achieve Clinical Cure at Week 52
NCT00730405 (6) [back to overview]The Percentage of Participants Who Achieve Complete Cure at Week 52
NCT00730405 (6) [back to overview]The Percentage of Participants Who Achieve Effective Treatment at Week 52
NCT00730405 (6) [back to overview]The Percentage of Participants Who Achieve Mycological Cure at Week 52
NCT00730405 (6) [back to overview]The Percentage of Participants With a Global Change Score of Cleared or Much Improved at Week 52

Absolute Change in Unaffected Part of Target Nail From Baseline to Week 52

Length of the unaffected part of the target nail was measured in millimeters along the midpoint from the nail fold to the proximal border of the affected part (lowest point affected) along the midpoint of the target nail. It was assessed on Week 4, 8, 12, 16, 20, 24, 30, 36, 44 and 52. Baseline values were the observations at Week 0/Day 1 or before. Change from Baseline was a Baseline value subtracted from Week 52 value. P-value was based on analysis of variance (ANOVA) with treatment and pooled center. Statistics is provided for adjusted least square mean. (NCT00730405)
Timeframe: Baseline (Week 0/Day 1 or before) and up to Week 52

InterventionMillimeters (Mean)
Albaconazole 400 mg (36 Weeks) Oral Weekly6.47
Albaconazole 400 mg (24 Weeks) Oral Weekly6.21
Albaconazole 200 mg (36 Weeks) Oral Weekly4.75
Albaconazole 100 mg (36 Weeks) Oral Weekly3.78
Placebo0.40

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The Percentage of Participants Who Achieve Clinical Cure at Week 52

At each study visit, the investigator assessed the percentage of affected toenail on the target nail by estimating the percent affected nail in each quadrant, summing the percent affected in each quadrant and dividing the sum by 4. Clinical cure was defined as 100% clear nail. It was assessed on Week 4, 8, 12, 16, 20, 24, 30, 36, 44 and 52. (NCT00730405)
Timeframe: Week 52

InterventionPercentage of participants (Number)
Albaconazole 400 mg (36 Weeks) Oral Weekly34
Albaconazole 400 mg (24 Weeks) Oral Weekly32
Albaconazole 200 mg (36 Weeks) Oral Weekly30
Albaconazole 100 mg (36 Weeks) Oral Weekly16
Placebo1

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The Percentage of Participants Who Achieve Complete Cure at Week 52

At each study visit, the investigator assessed the percentage of affected toenail on the target nail by estimating the percent affected nail in each quadrant, summing the percent affected in each quadrant and dividing the sum by 4. Complete cure was defined as mycological cure plus clinical cure. It was assessed on Week 4, 8, 12, 16, 20, 24, 30, 36, 44 and 52. (NCT00730405)
Timeframe: Week 52

InterventionPercentage of participants (Number)
Albaconazole 400 mg (36 Weeks) Oral Weekly33
Albaconazole 400 mg (24 Weeks) Oral Weekly26
Albaconazole 200 mg (36 Weeks) Oral Weekly21
Albaconazole 100 mg (36 Weeks) Oral Weekly12
Placebo0

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The Percentage of Participants Who Achieve Effective Treatment at Week 52

At each study visit, the investigator assessed the percentage of affected toenail on the target nail by estimating the percent affected nail in each quadrant, summing the percent affected in each quadrant and dividing the sum by 4. Effective treatment was defined as a mycological cure and clear or almost clear nail (distal subungual hyperkeratosis and/or onycholysis leaving less than 10% of nail plate effected). Comparisons were carried out in a sequential step-down fashion, combined with the Holm procedure at step 2. P-value was based on a sequential step-down combined with the Holm procedure. It was assessed on Week 4, 8, 12, 16, 20, 24, 30, 36, 44 and 52. (NCT00730405)
Timeframe: Week 52

InterventionPercentage of participants (Number)
Albaconazole 400 mg (36 Weeks) Oral Weekly54
Albaconazole 400 mg (24 Weeks) Oral Weekly38
Albaconazole 200 mg (36 Weeks) Oral Weekly29
Albaconazole 100 mg (36 Weeks) Oral Weekly21
Placebo1

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The Percentage of Participants Who Achieve Mycological Cure at Week 52

At each study visit, the investigator assessed the percentage of affected toenail on the target nail by estimating the percent affected nail in each quadrant, summing the percent affected in each quadrant and dividing the sum by 4. Mycological cure was defined as negative potassium hydroxide (KOH) and negative cultures for dermatophytes. It was assessed on Week 12, 16, 20, 24, 30, 36, 44 and 52. (NCT00730405)
Timeframe: Week 52

InterventionPercentage of participants (Number)
Albaconazole 400 mg (36 Weeks) Oral Weekly71
Albaconazole 400 mg (24 Weeks) Oral Weekly54
Albaconazole 200 mg (36 Weeks) Oral Weekly43
Albaconazole 100 mg (36 Weeks) Oral Weekly34
Placebo6

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The Percentage of Participants With a Global Change Score of Cleared or Much Improved at Week 52

A count of the number of toenails affected, using visual examination, was performed at all study visits (Week 12, 24, 30, 36, 44 and 52). The investigator given a global evaluation of the toenails condition, based on the investigator's assessment of the reduction in extent of nail involvement and improvement in clinical signs as compared with the status at the Baseline visit. The 0-5 rating scale was used: 0: cleared, 1: much improved, 2: minimally improved, 3: unchanged, 4: minimally worse and 5: much worse; where higher score indicates worse condition and lower score indicates clear toenail. (NCT00730405)
Timeframe: Week 52

InterventionPercentage of participants (Number)
Albaconazole 400 mg (36 Weeks) Oral Weekly71
Albaconazole 400 mg (24 Weeks) Oral Weekly62
Albaconazole 200 mg (36 Weeks) Oral Weekly61
Albaconazole 100 mg (36 Weeks) Oral Weekly45
Placebo10

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