Page last updated: 2024-11-12

tavaborole

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

tavaborole: has antifungal activity; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

tavaborole : A member of the class of benzoxaboroles that is 1,3-dihydro-1-hydroxy-2,1-benzoxaborole substituted at position 5 by a fluoro group. A topical antifungal agent used for the treatment of onychomycosis (fungal infection of the toenails and fingernails). [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID11499245
CHEMBL ID443052
CHEBI ID77942
SCHEMBL ID500016
MeSH IDM0501305

Synonyms (66)

Synonym
tavaborole
an-2690 ,
sch-900340
2,1-benzoxaborole, 5-fluoro-1,3-dihydro-1-hydroxy-
5-fluoro-1-hydroxy-3h-2,1-benzoxaborole
CHEMBL443052
an2690
chebi:77942 ,
tavaborole (usan)
D10169
kerydin (tn)
AKOS006303927
bdbm50370987
HY-10980
CS-1058
k124a4euq3 ,
hsdb 8342
174671-46-6
5-fluoro-1,3-dihydro-1-hydroxy-2,1-benzoxaborole
kerydin
an 2690
tavaborole [usan:inn]
unii-k124a4euq3
NCGC00264110-01
5-fluoro-2,1-benzoxaborol-1(3h)-ol
tavaborole [who-dd]
tavaborole [usan]
tavaborole [vandf]
tavaborole [orange book]
tavaborole [inn]
tavaborole [mi]
S4996
5-fluoro-1,3-dihydro-2,1-benzoxaborol-1-ol
MB08883
5-fluorobenzo[c][1,2]oxaborol-1(3h)-ol
LFQDNHWZDQTITF-UHFFFAOYSA-N
1,3-dihydro-5-fluoro-1-hydroxy-2,1-benzoxaborole
5-fluoro-3h-benzo[c][1,2)oxaborol-1-ol
5-fluoro-3h-benzo[c][1,2]oxaborol-1-ol
SCHEMBL500016
T3775
AC-30887
FT-0697827
DTXSID00169888 ,
DB09041
mfcd10699483
EX-A1086
an-2690(tavaborole)
p-fluorbenzoxaborole
DS-8392
SY038332
5-fluoro-1-hydroxy-2,1-benzoxaborolane
Z1198279578
Q21011226
BCP08730
EN300-125084
5-fluoro-1-hydroxyl-1,3-dihydrobenzo[c][1,2]oxaborole
CCG-266215
NCGC00264110-02
tavaborole (an-2690)
F11396
d01ae24
tavaborol
tavaborolum
dtxcid5092379
tavaborole topical solution, 5%

Research Excerpts

Overview

Tavaborole is a broad-spectrum oxaborole antifungal agent with low molecular weight. It is approved by the US Food and Drug Administration for the treatment of toenail onychomycosis.

ExcerptReferenceRelevance
"Tavaborole is a topical treatment option for onychomycosis."( Planimetric Post-hoc Analysis of Women With Onychomycosis from Tavaborole 5% Phase III Studies: Evidence of Greater Improvements in Patients With >50% Baseline Infection.
Gellings Lowe, N; Lipner, SR; Pariser, DM; Rycerz, AM; Wendelken, ME; Yost, JM, 2018
)
1.44
"Tavaborole is a novel small-molecule antifungal agent recently approved in the United States for the topical treatment of toenail onychomycosis."( Examining the Benefits of the Boron-Based Mechanism of Action and Physicochemical Properties of Tavaborole in the Treatment of Onychomycosis.
Ghannoum, M; Gupta, AK; Markinson, B; Rock, F; Rycerz, A; Winter, T, 2018
)
1.42
"Tavaborole is a broad-spectrum oxaborole antifungal agent with low molecular weight, permitting optimal nail plate penetration."( Tavaborole for the treatment of onychomycosis.
Elewski, BE; Tosti, A, 2014
)
2.57
"Tavaborole is a novel, topical antifungal pharmaceutical agent pending FDA approval for the treatment of toenail onychomycosis due to dermatophytes. "( Tavaborole for the treatment of onychomycosis.
Elewski, BE; Tosti, A, 2014
)
3.29
"Tavaborole is a novel, low-molecular weight oxaborole antifungal drug under development by Anacor Pharmaceuticals Inc. "( Tavaborole: first global approval.
Markham, A, 2014
)
3.29
"Tavaborole is a novel, boron-based anti-fungal agent with greater nail plate penetration than its predecessors, due to its smaller molecular weight."( Spotlight on tavaborole for the treatment of onychomycosis.
Finch, J; Jinna, S, 2015
)
1.51
"Tavaborole is a topical antifungal agent approved by the US Food and Drug Administration for the treatment of toenail onychomycosis. "( Tavaborole, a Novel Boron-Containing Small Molecule Pharmaceutical Agent for Topical Treatment of Onychomycosis: I. Reproductive and Developmental Toxicity Studies.
Chanda, S; Ciaravino, V; Coronado, D; Hoberman, A; Lanphear, C, 2016
)
3.32
"Tavaborole is a topical antifungal agent approved by the US Food and Drug Administration for the treatment of toenail onychomycosis. "( Tavaborole, a Novel Boron-Containing Small Molecule Pharmaceutical Agent for Topical Treatment of Onychomycosis: II. Prenatal and Postnatal Developmental Toxicity and Maternal Function Study.
Chanda, S; Ciaravino, V; Coronado, D; Hoberman, A; Lanphear, C, 2016
)
3.32
"Tavaborole is a new drug that addresses the unmet needs of currently available treatments."( Tavaborole - a treatment for onychomycosis of the toenails.
Gupta, AK; Versteeg, SG, 2016
)
2.6

Effects

ExcerptReferenceRelevance
"Tavaborole has a unique mechanism of action against fungal organisms and retains antifungal properties in the presence of keratin."( Tavaborole (AN-2690) for the treatment of onychomycosis of the toenail in adults.
Daigle, D; Gupta, AK, 2014
)
2.57

Treatment

Tavaborole is a topical treatment option for onychomycosis. Tavaborole-treated polished nails showed no polish discoloration.

ExcerptReferenceRelevance
"Tavaborole is a topical treatment option for onychomycosis."( Planimetric Post-hoc Analysis of Women With Onychomycosis from Tavaborole 5% Phase III Studies: Evidence of Greater Improvements in Patients With >50% Baseline Infection.
Gellings Lowe, N; Lipner, SR; Pariser, DM; Rycerz, AM; Wendelken, ME; Yost, JM, 2018
)
1.44
"Tavaborole-treated polished nails showed no polish discoloration, and tavaborole applicators did not change in appearance during treatment. "( Evaluation of the Appearance of Nail Polish Following Daily Treatment of Ex Vivo Human Fingernails With Topical Solutions of Tavaborole or Efinaconazole.
Chanda, S; Coronado, D; Merchant, T; Vlahovic, TC; Zane, LT, 2016
)
2.08

Toxicity

ExcerptReferenceRelevance
" In rabbit embryo-fetal development toxicity studies dosed via oral or dermal administration, the no observable adverse effect level for maternal toxicity and embryo-fetal toxicity was 50 mg/kg/d (16 times the MRHD) and 5% (26 times the MRHD), respectively."( Tavaborole, a Novel Boron-Containing Small Molecule Pharmaceutical Agent for Topical Treatment of Onychomycosis: I. Reproductive and Developmental Toxicity Studies.
Chanda, S; Ciaravino, V; Coronado, D; Hoberman, A; Lanphear, C, 2016
)
1.88
" The no observed adverse effect level (NOAEL) for maternal toxicity (F0 generation) was 60 mg/kg/d, based on the decreased activity observed in the 100 mg/kg/d dose group."( Tavaborole, a Novel Boron-Containing Small Molecule Pharmaceutical Agent for Topical Treatment of Onychomycosis: II. Prenatal and Postnatal Developmental Toxicity and Maternal Function Study.
Chanda, S; Ciaravino, V; Coronado, D; Hoberman, A; Lanphear, C, 2016
)
1.88
" There are limited data on adverse events associated with the newer topical onychomycosis drugs."( Retrospective analysis of adverse events with topical onychomycosis medications reported to the United States Food and Drug Administration.
Lipner, SR; Wang, Y, 2020
)
0.56

Dosage Studied

One double-blind, randomized, vehicle-controlled study (study 1) and two open-label studies (studies 2 and 3) examined the efficacy, safety, and optimal dosing concentration of tavaborole topical solution applied once daily or three times weekly for 180 days.

ExcerptRelevanceReference
"To assess the potential efficacy, safety, and optimal dosing concentration of tavaborole, a novel, boron-based pharmaceutical agent with broad-spectrum antifungal activity, for the treatment of onychomycosis of the toenail due to dermatophytes."( The efficacy and safety of tavaborole, a novel, boron-based pharmaceutical agent: phase 2 studies conducted for the topical treatment of toenail onychomycosis.
Bucko, A; Herz-Ruelas, ME; Jarratt, MT; Jones, TM; Ocampo-Candiani, J; Pollak, RA; Toledo-Bahena, ME; Zane, LT, 2014
)
0.93
"5%, were generally mild to moderate, and resolved with treatment discontinuation and/or a reduction in dosing frequency."( The efficacy and safety of tavaborole, a novel, boron-based pharmaceutical agent: phase 2 studies conducted for the topical treatment of toenail onychomycosis.
Bucko, A; Herz-Ruelas, ME; Jarratt, MT; Jones, TM; Ocampo-Candiani, J; Pollak, RA; Toledo-Bahena, ME; Zane, LT, 2014
)
0.7
"In study 1, tavaborole penetration was evaluated over 20 days of dosing using the Franz finite dose technique and modified Franz diffusion cells."( In Vitro Nail Penetration of Tavaborole Topical Solution, 5%, Through Nail Polish on Ex Vivo Human Fingernails.
Chanda, S; Coronado, D; MPharm, TM; Vlahovic, T; Zane, LT, 2015
)
1.09
" Nail polish appearance after application of tavaborole (dropper) or efinaconazole (brush); respective applicator appearance; presence of color transfer from respective applicators; and color transfer to remaining solutions after dosing of polished nails were evaluated."( Evaluation of the Appearance of Nail Polish Following Daily Treatment of Ex Vivo Human Fingernails With Topical Solutions of Tavaborole or Efinaconazole.
Chanda, S; Coronado, D; Merchant, T; Vlahovic, TC; Zane, LT, 2016
)
0.9
" Dropper and brush applicators were applied to white watercolor paper immediately after dosing to evaluate color transfer from polished nails."( Evaluation of the Appearance of Nail Polish Following Daily Treatment of Ex Vivo Human Fingernails With Topical Solutions of Tavaborole or Efinaconazole.
Chanda, S; Coronado, D; Merchant, T; Vlahovic, TC; Zane, LT, 2016
)
0.64
" In rabbit embryo-fetal development toxicity studies dosed via oral or dermal administration, the no observable adverse effect level for maternal toxicity and embryo-fetal toxicity was 50 mg/kg/d (16 times the MRHD) and 5% (26 times the MRHD), respectively."( Tavaborole, a Novel Boron-Containing Small Molecule Pharmaceutical Agent for Topical Treatment of Onychomycosis: I. Reproductive and Developmental Toxicity Studies.
Chanda, S; Ciaravino, V; Coronado, D; Hoberman, A; Lanphear, C, 2016
)
1.88
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
antifungal agentAn antimicrobial agent that destroys fungi by suppressing their ability to grow or reproduce.
protein synthesis inhibitorA compound, usually an anti-bacterial agent or a toxin, which inhibits the synthesis of a protein.
EC 6.1.1.4 (leucine--tRNA ligase) inhibitorAn EC 6.1.1.* (ligases forming aminoacyl tRNA and related compounds) inhibitor that inhibits the action of leucine--tRNA synthetase (EC 6.1.1.4).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
organofluorine compoundAn organofluorine compound is a compound containing at least one carbon-fluorine bond.
benzoxaboroleAny organic heterobicyclic compound that consists of an oxoborole ring that is ortho-fused to a benzene ring.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (5)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Carbonic anhydrase 1Homo sapiens (human)Ki2.01500.00001.372610.0000AID1504709
Carbonic anhydrase 2Homo sapiens (human)Ki0.46200.00000.72369.9200AID1504710; AID1726062
Leucine--tRNA ligase, cytoplasmicSaccharomyces cerevisiae S288CIC50 (µMol)2.10002.10002.10002.1000AID289193
Leucine--tRNA ligase, cytoplasmicSaccharomyces cerevisiae S288CKi16.62501.85001.85001.8500AID289191; AID289192
Carbonic anhydrase Cryptococcus neoformans var. grubiiKi0.08900.01000.73648.3470AID1504707
Carbonic anhydrase Nakaseomyces glabratus CBS 138Ki0.07200.00701.21749.1700AID1504708
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (12)

Processvia Protein(s)Taxonomy
one-carbon metabolic processCarbonic anhydrase 1Homo sapiens (human)
morphogenesis of an epitheliumCarbonic anhydrase 2Homo sapiens (human)
positive regulation of synaptic transmission, GABAergicCarbonic anhydrase 2Homo sapiens (human)
positive regulation of cellular pH reductionCarbonic anhydrase 2Homo sapiens (human)
angiotensin-activated signaling pathwayCarbonic anhydrase 2Homo sapiens (human)
regulation of monoatomic anion transportCarbonic anhydrase 2Homo sapiens (human)
secretionCarbonic anhydrase 2Homo sapiens (human)
regulation of intracellular pHCarbonic anhydrase 2Homo sapiens (human)
neuron cellular homeostasisCarbonic anhydrase 2Homo sapiens (human)
positive regulation of dipeptide transmembrane transportCarbonic anhydrase 2Homo sapiens (human)
regulation of chloride transportCarbonic anhydrase 2Homo sapiens (human)
carbon dioxide transportCarbonic anhydrase 2Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (6)

Processvia Protein(s)Taxonomy
arylesterase activityCarbonic anhydrase 1Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 1Homo sapiens (human)
protein bindingCarbonic anhydrase 1Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 1Homo sapiens (human)
hydro-lyase activityCarbonic anhydrase 1Homo sapiens (human)
cyanamide hydratase activityCarbonic anhydrase 1Homo sapiens (human)
arylesterase activityCarbonic anhydrase 2Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 2Homo sapiens (human)
protein bindingCarbonic anhydrase 2Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 2Homo sapiens (human)
cyanamide hydratase activityCarbonic anhydrase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (6)

Processvia Protein(s)Taxonomy
cytosolCarbonic anhydrase 1Homo sapiens (human)
extracellular exosomeCarbonic anhydrase 1Homo sapiens (human)
cytoplasmCarbonic anhydrase 2Homo sapiens (human)
cytosolCarbonic anhydrase 2Homo sapiens (human)
plasma membraneCarbonic anhydrase 2Homo sapiens (human)
myelin sheathCarbonic anhydrase 2Homo sapiens (human)
apical part of cellCarbonic anhydrase 2Homo sapiens (human)
extracellular exosomeCarbonic anhydrase 2Homo sapiens (human)
cytoplasmCarbonic anhydrase 2Homo sapiens (human)
plasma membraneCarbonic anhydrase 2Homo sapiens (human)
apical part of cellCarbonic anhydrase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (65)

Assay IDTitleYearJournalArticle
AID289206Antifungal activity against Cladosporium cladosporioides ATCC 160222007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID1504708Inhibition of Candida glabrata Nce103 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay2017ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11
Benzoxaboroles as Efficient Inhibitors of the β-Carbonic Anhydrases from Pathogenic Fungi: Activity and Modeling Study.
AID289208Antifungal activity against Trichophyton rubrum ATCC 187592007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID289207Antifungal activity against Fusarium solani ATCC 360312007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID1297994Inhibition of Trypanosoma brucei LeuRS assessed as formation of stable tRNA(Leu)-compound adduct in editing site of enzyme2016Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
Repurposing strategies for tropical disease drug discovery.
AID1569289Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Design, Synthesis, and Structure-Activity Relationship of 7-Propanamide Benzoxaboroles as Potent Anticancer Agents.
AID289192Inhibition of Saccharomyces cerevisiae cytoplasmic leucyl-tRNA synthetase after 20 mins2007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID1504707Inhibition of Cryptococcus neoformans Can2 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay2017ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11
Benzoxaboroles as Efficient Inhibitors of the β-Carbonic Anhydrases from Pathogenic Fungi: Activity and Modeling Study.
AID289210Antifungal activity against Epidermophyton floccosum ATCC 5250662007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID1850491Antifungal activity against Aspergillus niger assessed as fungal growth inhibition incubated for 48 hrs by agar diffusion method2022Bioorganic & medicinal chemistry, 06-01, Volume: 63Boron-Containing heterocycles as promising pharmacological agents.
AID289216Antimicrobial activity against AN2690-resistant Saccharomyces cerevisiae ANA323 with CDC60 G405V mutation2007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID289214Antimicrobial activity against AN2690-resistant Saccharomyces cerevisiae ANA321 with CDC60 R316I mutation2007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID289196Antifungal activity against Candida glabrata ATCC 900302007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID1504709Inhibition of human carbonic anhydrase-1 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay2017ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11
Benzoxaboroles as Efficient Inhibitors of the β-Carbonic Anhydrases from Pathogenic Fungi: Activity and Modeling Study.
AID266927Antifungal activity against Candida albicans2006Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
Discovery of a new boron-containing antifungal agent, 5-fluoro-1,3-dihydro-1-hydroxy-2,1- benzoxaborole (AN2690), for the potential treatment of onychomycosis.
AID289209Antifungal activity against Trichophyton mentagrophytes ATCC 281852007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID1726065Selectivity index, ratio of Ki for human carbonic anhydrase 2 to Ki for Vibrio cholerae gamma carbonic anhydrase
AID289213Antimicrobial activity against AN2690-resistant Saccharomyces cerevisiae ANA320 with CDC60 N415D mutation2007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID289193Inhibition of Saccharomyces cerevisiae cytoplasmic leucyl-tRNA synthetase assessed as tRNA amino-acylation2007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID289202Antifungal activity against Aspergillus fumigatus ATCC 130732007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID289198Antifungal activity against Candida tropicalis ATCC 138032007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID1569288Antiproliferative activity against human SKOV3 cells after 72 hrs by MTT assay2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Design, Synthesis, and Structure-Activity Relationship of 7-Propanamide Benzoxaboroles as Potent Anticancer Agents.
AID1863505Inhibition of full length DENV2 NS2B-NS3 protease in human HeLa cells expressing luciferase reporter gene at 12.5 uM incubated for 24 hrs by luminescence analysis relative to control
AID289199Antifungal activity against Cryptococcus neoformans F2852007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID1864430Inhibition of NLRP3 inflammasome activation in LPS-primed mouse J774.A1 cells assessed as reduction in IL-1beta secretion at 1 uM2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of a Novel Oral Proteasome Inhibitor to Block NLRP3 Inflammasome Activation with Anti-inflammation Activity.
AID289190Inhibition of protein synthesis in Saccharomyces cerevisiae S288C after 15 mins2007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID289215Antimicrobial activity against AN2690-resistant Saccharomyces cerevisiae ANA322 with CDC60 C326F mutation2007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID289212Antifungal activity against Microsporum gypseum ATCC 241032007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID289211Antifungal activity against Microsporum audouinii ATCC 425582007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID1726062Inhibition of human carbonic anhydrase 2 incubated for 30 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay
AID266926Antifungal activity against Trichophyton mentagrophytes2006Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
Discovery of a new boron-containing antifungal agent, 5-fluoro-1,3-dihydro-1-hydroxy-2,1- benzoxaborole (AN2690), for the potential treatment of onychomycosis.
AID289189Inhibition of Saccharomyces cerevisiae cytoplasmic leucyl-tRNA synthetase assessed as [3H]IleutRNA-Leu hydrolysis by post-transfer editing assay2007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID289195Antifungal activity against Candida albicans ATCC 900282007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID1726064Selectivity index, ratio of Ki for human carbonic anhydrase 2 to Ki for Vibrio cholerae beta carbonic anhydrase
AID1863504Inhibition of full length DENV2 NS2B-NS3 protease in human HeLa cells expressing luciferase reporter gene incubated for 24 hrs by luminescence analysis
AID289204Antifungal activity against Alternaria alternata ATCC 66632007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID1726063Selectivity index, ratio of Ki for human carbonic anhydrase 2 to Ki for Vibrio cholerae alpha carbonic anhydrase
AID1504706Inhibition of Malassezia globosa beta-carbonic anhydrase incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay2017ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11
Benzoxaboroles as Efficient Inhibitors of the β-Carbonic Anhydrases from Pathogenic Fungi: Activity and Modeling Study.
AID1726059Inhibition of Vibrio cholerae alpha carbonic anhydrase incubated for 30 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay
AID289219Antimicrobial activity against AN2690-resistant Saccharomyces cerevisiae ANA327 with CDC60 T314M mutation2007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID289221Antimicrobial activity against AN2690-resistant Saccharomyces cerevisiae ANA360 with CDC60 T319I mutation2007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID289194Antimicrobial activity against Saccharomyces cerevisiae ATCC 2013882007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID1504710Inhibition of human carbonic anhydrase-2 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay2017ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11
Benzoxaboroles as Efficient Inhibitors of the β-Carbonic Anhydrases from Pathogenic Fungi: Activity and Modeling Study.
AID266925Antifungal activity against Trichophyton rubrum2006Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
Discovery of a new boron-containing antifungal agent, 5-fluoro-1,3-dihydro-1-hydroxy-2,1- benzoxaborole (AN2690), for the potential treatment of onychomycosis.
AID266928Antifungal activity against Cryptococcus neoformans2006Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
Discovery of a new boron-containing antifungal agent, 5-fluoro-1,3-dihydro-1-hydroxy-2,1- benzoxaborole (AN2690), for the potential treatment of onychomycosis.
AID289222Antimicrobial activity against Saccharomyces cerevisiae in synthetic defined media without leucine2007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID1569291Cytotoxicity against human WI38 cells after 72 hrs by MTT assay2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Design, Synthesis, and Structure-Activity Relationship of 7-Propanamide Benzoxaboroles as Potent Anticancer Agents.
AID289191Inhibition of Saccharomyces cerevisiae cytoplasmic leucyl-tRNA synthetase after 2 mins2007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID289218Antimicrobial activity against AN2690-resistant Saccharomyces cerevisiae ANA326 with CDC60 L315V mutation2007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID289220Antimicrobial activity against AN2690-resistant Saccharomyces cerevisiae ANA358 with CDC60 S416L mutation2007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID289197Antifungal activity against Candida krusei ATCC 445072007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID289223Binding affinity to Saccharomyces cerevisiae cytoplasmic leucyl-tRNA synthetase in presence of AMP2007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID289205Antifungal activity against Penicillium chrysogenum ATCC 101082007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID1863503Inhibition of C-terminal His tagged SARS CoV-2 main protease transfected in Escherichia coli BL21 (DE3) using 2-Abz-Ser-AlaVal-Leu-Gln-Ser-Gly-Tyr(3-NO2)-Arg-OH as substrate at 50 uM preincubated for 15 mins followed by substrate addition and measured aft
AID289201Antifungal activity against Malassezia pachydermatis ATCC 967462007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID1726061Inhibition of Vibrio cholerae gamma carbonic anhydrase incubated for 30 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay
AID1569290Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Design, Synthesis, and Structure-Activity Relationship of 7-Propanamide Benzoxaboroles as Potent Anticancer Agents.
AID289200Antifungal activity against Malassezia furfur ATCC 443442007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID289203Antifungal activity against Rhizopus microsporus ATCC 662762007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
AID266929Antifungal activity against Aspergillus fumigatus2006Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
Discovery of a new boron-containing antifungal agent, 5-fluoro-1,3-dihydro-1-hydroxy-2,1- benzoxaborole (AN2690), for the potential treatment of onychomycosis.
AID1863502Inhibition of C-terminal His tagged SARS CoV-2 main protease transfected in Escherichia coli BL21 (DE3) using 2-Abz-Ser-AlaVal-Leu-Gln-Ser-Gly-Tyr(3-NO2)-Arg-OH as substrate preincubated for 15 mins followed by substrate addition and measured after 15 min
AID1863506Cytotoxicity against human HeLa cells expressing luciferase-based DENV-2 protease reporter system assessed as reduction in cell viability by celltiter-blue assay
AID1726060Inhibition of Vibrio cholerae beta carbonic anhydrase incubated for 30 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay
AID1380105Inhibition of Saccharomyces cerevisiae LeuRs2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Emerging New Targets for the Treatment of Resistant Fungal Infections.
AID289217Antimicrobial activity against AN2690-resistant Saccharomyces cerevisiae ANA324 with CDC60 C326R mutation2007Science (New York, N.Y.), Jun-22, Volume: 316, Issue:5832
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (72)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's6 (8.33)29.6817
2010's56 (77.78)24.3611
2020's10 (13.89)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 53.67

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 very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index53.67 (24.57)
Research Supply Index4.44 (2.92)
Research Growth Index5.56 (4.65)
Search Engine Demand Index102.91 (26.88)
Search Engine Supply Index2.46 (0.95)

This Compound (53.67)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials9 (12.00%)5.53%
Reviews21 (28.00%)6.00%
Case Studies1 (1.33%)4.05%
Observational0 (0.00%)0.25%
Other44 (58.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (11)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
An Open-label Study To Evaluate The Safety, Tolerability, And Pharmacokinetics Of Kerydin (Registered) (Tavaborole) Topical Solution, 5% In The Treatment Of Onychomycosis Of The Toenail In Pediatric Subjects Ages 6 To 16 Years And 11 Months [NCT03405818]Phase 455 participants (Actual)Interventional2015-10-22Completed
A Randomized, Double-Blind, Vehicle-Controlled, Multi-Center Study to Evaluate the Safety and Efficacy of Topically Applied AN2690 2.5%, 5.0%, and 7.5% Solutions vs. Vehicle for the Treatment of Adult Subjects With Onychomycosis of the Great Toenail [NCT00679965]Phase 2159 participants (Actual)Interventional2006-02-28Completed
A Randomized, Double-blind, Vehicle-controlled, Multi-center Study To Evaluate The Safety And Efficacy Of Topically Applied An2690 2.5%, 5.0%, And 7.5% Solutions Vs. Vehicle For The Treatment Of Adult Subjects With Onychomycosis Of The Great Toenail. [NCT00679770]Phase 228 participants (Actual)Interventional2006-06-30Completed
An Open-label, Multiple-dose Study Of The Absorption And Systemic Pharmacokinetics Of An2690 Applied As A 7.5% Solution To All Toenails Of Adult Patients With Moderate To Severe Onychomycosis [NCT00680160]Phase 215 participants (Actual)Interventional2006-04-30Completed
An Open-Label, Rising Multiple-Dose, Multi-Center Study to Evaluate the Safety and Efficacy of Topically Applied AN2690 5.0% and 7.5% Solution for the Treatment of Adult Subjects With Onychomycosis of the Great Toenail [NCT00679523]Phase 260 participants (Actual)Interventional2005-11-30Completed
An Open-label, Multiple-dose Study Of The Absorption And Systemic Pharmacokinetics Of An2690 Applied As A 7.5% Solution To All Toenails Of Adult Patients With Moderate To Severe Onychomycosis [NCT00679601]Phase 220 participants (Actual)Interventional2007-03-31Completed
21-day Cumulative Irritation Test [NCT00680095]Phase 137 participants (Actual)Interventional2007-01-22Completed
An Open Label, Multi-center Study To Evaluate The Safety And Efficacy Of Topically Applied An2690 1% And 5% Solutions For The Treatment Of Adult Subjects With Onychomycosis Of The Great Toenail [NCT00680134]Phase 260 participants (Actual)Interventional2006-06-30Completed
A Randomized, Double-Blind, Vehicle-Controlled, Multi-Center Study to Evaluate the Efficacy and Safety of AN2690 Topical Solution, 5%, vs. Solution Vehicle in the Treatment of Onychomycosis of the Toenail in Adults [NCT01302119]Phase 3604 participants (Actual)Interventional2011-02-28Completed
An Open-Label, Rising Multiple-Dose, Multi-Center Study to Evaluate the Safety and Efficacy of Topically Applied AN2690 5.0% and 7.5% Solution for the Treatment of Adult Subjects With Onychomycosis of the Great Toenail [NCT01278394]Phase 229 participants (Actual)Interventional2007-03-31Completed
A Randomized, Double-Blind, Vehicle-Controlled, Multi-Center Study to Evaluate the Efficacy and Safety of AN2690 Topical Solution, 5%, vs. Solution Vehicle in the Treatment of Onychomycosis of the Toenail in Adults [NCT01270971]Phase 3594 participants (Actual)Interventional2010-12-01Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT01270971 (4) [back to overview]Treatment Success (Completely Clear or Almost Clear Nail and Negative Mycology) of Target Great Toenail at Week 52
NCT01270971 (4) [back to overview]Complete Cure (Completely Clear Nail and Negative Mycology) of Target Great Toenail at Week 52
NCT01270971 (4) [back to overview]Completely Clear or Almost Clear Target Great Toenail at Week 52
NCT01270971 (4) [back to overview]Negative Mycology of Target Great Toenail at Week 52
NCT01278394 (7) [back to overview]Mycological Evaluations (Negative KOH and Negative Fungal Culture) Compared to Baseline
NCT01278394 (7) [back to overview]Clear Nail Growth of the Targeted Toenail
NCT01278394 (7) [back to overview]Length of Time to Clinical Evaluation of Clear or at Least 5 mm of CNG
NCT01278394 (7) [back to overview]Clinical Evidence of Complete Clearance of the Treatment-targeted Great Toenail Plus a Negative Fungal Culture at Day 360
NCT01278394 (7) [back to overview]Mycological Evaluations (Negative KOH and Negative Fungal Culture) Compared to Baseline
NCT01278394 (7) [back to overview]Mycological Evaluations (Negative KOH and Negative Fungal Culture) Compared to Baseline
NCT01278394 (7) [back to overview]Mycological Evaluations (Negative Potassium Hydroxide (KOH) and Negative Fungal Culture) Compared to Baseline
NCT01302119 (4) [back to overview]Complete Cure (Completely Clear Nail and Negative Mycology) of Target Great Toenail at Week 52
NCT01302119 (4) [back to overview]Completely Clear or Almost Clear Target Great Toenail at Week 52
NCT01302119 (4) [back to overview]Treatment Success (Completely Clear or Almost Clear Nail and Negative Mycology) of Target Great Toenail at Week 52
NCT01302119 (4) [back to overview]Negative Mycology of Target Great Toenail at Week 52
NCT03405818 (38) [back to overview]Change From Baseline in Chemistry Parameters (Albumin and Protein) at Week 52
NCT03405818 (38) [back to overview]Change From Baseline in Chemistry Parameters (Bilirubin, Creatinine, Glucose [Non-fasting] and Urea Nitrogen) at Week 24
NCT03405818 (38) [back to overview]Change From Baseline in Chemistry Parameters (Bilirubin, Creatinine, Glucose [Non-fasting] and Urea Nitrogen) at Week 52
NCT03405818 (38) [back to overview]Change From Baseline in Chemistry Parameters (Potassium and Sodium) at Week 24
NCT03405818 (38) [back to overview]Change From Baseline in Chemistry Parameters (Potassium and Sodium) at Week 52
NCT03405818 (38) [back to overview]Change From Baseline in Hematology Parameter (Erythrocytes) at Week 24
NCT03405818 (38) [back to overview]Change From Baseline in Hematology Parameter (Hematocrit) at Week 24
NCT03405818 (38) [back to overview]Change From Baseline in Hematology Parameters (Hemoglobin) at Week 24
NCT03405818 (38) [back to overview]Change From Baseline in Hematology Parameters (Leukocytes and Platelets) at Week 24
NCT03405818 (38) [back to overview]Change From Baseline in Hematology Parameters (Leukocytes and Platelets) at Week 52
NCT03405818 (38) [back to overview]Change From Baseline in Hematology Parameters (Leukocytes: Basophils, Eosinophils, Lymphocytes, Monocytes and Neutrophils) at Week 24
NCT03405818 (38) [back to overview]Change From Baseline in Vital Sign (Respiratory Rate) at Week 52
NCT03405818 (38) [back to overview]Change From Baseline in Vital Sign (Blood Pressure) at Week 24
NCT03405818 (38) [back to overview]Change From Baseline in Vital Sign (Blood Pressure) at Week 52
NCT03405818 (38) [back to overview]Change From Baseline in Vital Sign (Pulse Rate) at Week 24
NCT03405818 (38) [back to overview]Change From Baseline in Vital Sign (Respiratory Rate) at Week 24
NCT03405818 (38) [back to overview]Number of Participants With Adverse Events (AEs) By Severity
NCT03405818 (38) [back to overview]Number of Participants With Local Tolerability Reactions by Severity
NCT03405818 (38) [back to overview]Number of Participants With Treatment-Emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)
NCT03405818 (38) [back to overview]Percentage of Participants With Almost Complete Cure of Target Great Toenail (TGT) at Week 24 and 52
NCT03405818 (38) [back to overview]Percentage of Participants With Clinical Efficacy of Target Great Toenail (TGT) at Week 24 and 52
NCT03405818 (38) [back to overview]Percentage of Participants With Mycological Cure of Target Great Toenail (TGT) at Week 24 and 52
NCT03405818 (38) [back to overview]Percentage of Participants With Negative Fungal Culture of the Target Great Toenail (TGT) at Weeks 24 and 52
NCT03405818 (38) [back to overview]Area Under the Plasma Concentration-Time Curve Extrapolated to Infinity (AUCinf) of Tavaborole
NCT03405818 (38) [back to overview]Area Under the Plasma Concentration-Time Curve From Hour Zero to Hour 24 (AUC24) of Tavaborole
NCT03405818 (38) [back to overview]Change From Baseline in Hematology Parameter (Erythrocytes) at Week 52
NCT03405818 (38) [back to overview]Change From Baseline in Hematology Parameter (Hematocrit) at Week 52
NCT03405818 (38) [back to overview]Change From Baseline in Hematology Parameters (Hemoglobin) at Week 52
NCT03405818 (38) [back to overview]Change From Baseline in Vital Sign (Pulse Rate) at Week 52
NCT03405818 (38) [back to overview]Elimination Half-Life of Tavaborole
NCT03405818 (38) [back to overview]Elimination Rate Constant of Tavaborole
NCT03405818 (38) [back to overview]Change From Baseline in Hematology Parameters (Leukocytes: Basophils, Eosinophils, Lymphocytes, Monocytes and Neutrophils) at Week 52
NCT03405818 (38) [back to overview]Maximum Observed Plasma Concentration (Cmax) of Tavaborole
NCT03405818 (38) [back to overview]Percentage of Participants With Complete Cure of Target Great Toenail (TGT) at Week 52
NCT03405818 (38) [back to overview]Time to Maximum Observed Plasma Concentration (Tmax) of Tavaborole
NCT03405818 (38) [back to overview]Change From Baseline in Chemistry Parameters (Alanine Aminotransferase, Alkaline Phosphatase and Aspartate Aminotransferase) at Week 24
NCT03405818 (38) [back to overview]Change From Baseline in Chemistry Parameters (Alanine Aminotransferase, Alkaline Phosphatase and Aspartate Aminotransferase) at Week 52
NCT03405818 (38) [back to overview]Change From Baseline in Chemistry Parameters (Albumin and Protein) at Week 24

Treatment Success (Completely Clear or Almost Clear Nail and Negative Mycology) of Target Great Toenail at Week 52

No clinical evidence of onychomycosis as evidenced by normal toenail plate, no onycholysis, and no subungual hyperkeratosis, or no more than minimal evidence of onychomycosis as evidenced by toenail plate dystrophic or discolored over ≤ 10% of the distal aspect, with minimally evident onycholysis and subungual hyperkeratosis, and negative KOH wet mount and negative fungal culture. (NCT01270971)
Timeframe: Week 52

,
Interventionparticipants (Number)
SuccessFailure
AN2690 Topical Solution, 5%61338
Solution Vehicle3191

[back to top]

Complete Cure (Completely Clear Nail and Negative Mycology) of Target Great Toenail at Week 52

No clinical evidence of onychomycosis as evidenced by normal toenail plate, no onycholysis, and no subungual hyperkeratosis, and negative KOH wet mount and negative fungal culture. (NCT01270971)
Timeframe: Week 52

,
Interventionparticipants (Number)
SuccessFailure
AN2690 Topical Solution, 5%26373
Solution Vehicle1193

[back to top]

Completely Clear or Almost Clear Target Great Toenail at Week 52

No clinical evidence of onychomycosis as evidenced by normal toenail plate, no onycholysis, and no subungual hyperkeratosis, or no more than minimal evidence of onychomycosis as evidenced by toenail plate dystrophic or discolored over ≤ 10% of the distal aspect, with minimally evident onycholysis and subungual hyperkeratosis. (NCT01270971)
Timeframe: Week 52

,
Interventionparticipants (Number)
SuccessFailure
AN2690 Topical Solution, 5%104295
Solution Vehicle18176

[back to top]

Negative Mycology of Target Great Toenail at Week 52

Negative KOH and negative fungal culture. (NCT01270971)
Timeframe: Week 52

,
Interventionparticipants (Number)
SuccessFailure
AN2690 Topical Solution, 5%124275
Solution Vehicle14180

[back to top]

Mycological Evaluations (Negative KOH and Negative Fungal Culture) Compared to Baseline

Number of subjects with negative KOH, and number of subjects with negative fungal cultures. (NCT01278394)
Timeframe: Day 270

Interventionparticipants (Number)
Fungal Culture Result PositiveFungal Culture Result NegativeKOH Result PositiveKOH Result Negative
AN2690 Solution, 5.0%1281712

[back to top]

Clear Nail Growth of the Targeted Toenail

Clear nail was measured on digital images as the distance in millimeters from the proximal nail fold to the proximal limit of the disease as marked by the Investigator. New Clear Nail Growth (CNG) was calculated from the clear nail measurements. (NCT01278394)
Timeframe: Day 360

Interventionmillimeters (Mean)
AN2690 Solution, 5.0%0.5

[back to top]

Length of Time to Clinical Evaluation of Clear or at Least 5 mm of CNG

Length of time to clinical evaluation of clear or at least 5 mm of CNG. (NCT01278394)
Timeframe: Baseline to 360

Interventiondays (Mean)
AN2690 Solution, 5.0%138.0

[back to top]

Clinical Evidence of Complete Clearance of the Treatment-targeted Great Toenail Plus a Negative Fungal Culture at Day 360

Proportion of subjects with a clinical assessment of a clear (completely normal) nail unit plus a negative fungal culture from the treatment-targeted toenail at Day 360. (NCT01278394)
Timeframe: Day 360

Interventionparticipants (Number)
SuccessFailure
AN2690 Solution, 5.0%227

[back to top]

Mycological Evaluations (Negative KOH and Negative Fungal Culture) Compared to Baseline

Number of subjects with negative KOH, and number of subjects with negative fungal cultures. (NCT01278394)
Timeframe: Day 180

Interventionparticipants (Number)
Fungal Culture Result PositiveFungal Culture Result NegativeKOH Result PositiveKOH Result Negative
AN2690 Solution, 5.0%029209

[back to top]

Mycological Evaluations (Negative KOH and Negative Fungal Culture) Compared to Baseline

Number of subjects with negative KOH, and number of subjects with negative fungal cultures. (NCT01278394)
Timeframe: Day 360

Interventionparticipants (Number)
Fungal Culture Result PositiveFungal Culture Result NegativeKOH Result PositiveKOH Result Negative
AN2690 Solution, 5.0%128236

[back to top]

Mycological Evaluations (Negative Potassium Hydroxide (KOH) and Negative Fungal Culture) Compared to Baseline

Number of subjects with negative KOH, and number of subjects with negative fungal cultures. (NCT01278394)
Timeframe: Day 90

Interventionparticipants (Number)
Fungal Culture Result PositiveFungal Culture Result NegativeKOH Result PositiveKOH Result Negative
AN2690 Solution, 5.0%128245

[back to top]

Complete Cure (Completely Clear Nail and Negative Mycology) of Target Great Toenail at Week 52

No clinical evidence of onychomycosis as evidenced by normal toenail plate, no onycholysis, and no subungual hyperkeratosis, and negative KOH wet mount and negative fungal culture. (NCT01302119)
Timeframe: Week 52

,
Interventionparticipants (Number)
SuccessFailure
AN2690 Topical Solution, 5%36360
Solution Vehicle3202

[back to top]

Completely Clear or Almost Clear Target Great Toenail at Week 52

No clinical evidence of onychomycosis as evidenced by normal toenail plate, no onycholysis, and no subungual hyperkeratosis, or no more than minimal evidence of onychomycosis as evidenced by toenail plate dystrophic or discolored over ≤ 10% of the distal aspect, with minimally evident onycholysis and subungual hyperkeratosis. (NCT01302119)
Timeframe: Week 52

,
Interventionparticipants (Number)
SuccessFailure
AN2690 Topical Solution, 5%109287
Solution Vehicle30175

[back to top]

Treatment Success (Completely Clear or Almost Clear Nail and Negative Mycology) of Target Great Toenail at Week 52

No clinical evidence of onychomycosis as evidenced by normal toenail plate, no onycholysis, and no subungual hyperkeratosis, or no more than minimal evidence of onychomycosis as evidenced by toenail plate dystrophic or discolored over ≤ 10% of the distal aspect, with minimally evident onycholysis and subungual hyperkeratosis, and negative KOH wet mount and negative fungal culture. (NCT01302119)
Timeframe: Week 52

,
Interventionparticipants (Number)
SuccessFailure
AN2690 Topical Solution, 5%71325
Solution Vehicle8197

[back to top]

Negative Mycology of Target Great Toenail at Week 52

Negative KOH and negative fungal culture. (NCT01302119)
Timeframe: Week 52

,
Interventionparticipants (Number)
SuccessFailure
AN2690 Topical Solution, 5%142254
Solution Vehicle25180

[back to top]

Change From Baseline in Chemistry Parameters (Albumin and Protein) at Week 52

(NCT03405818)
Timeframe: Baseline, Week 52

Interventiongram per deciliter (g/dL) (Mean)
Change at Week 52: AlbuminChange at Week 52: Protein
Kerydin-0.08-0.07

[back to top]

Change From Baseline in Chemistry Parameters (Bilirubin, Creatinine, Glucose [Non-fasting] and Urea Nitrogen) at Week 24

(NCT03405818)
Timeframe: Baseline, Week 24

Interventionmilligram per deciliter (mg/dL) (Mean)
Baseline: BilirubinBaseline: CreatinineBaseline: Glucose [non-fasting]Baseline: Urea NitrogenChange at Week 24: BilirubinChange at Week 24: CreatinineChange at Week 24: Glucose [non-fasting]Change at Week 24: Urea Nitrogen
Kerydin0.460.6887.513.50.030.010.0-0.1

[back to top]

Change From Baseline in Chemistry Parameters (Bilirubin, Creatinine, Glucose [Non-fasting] and Urea Nitrogen) at Week 52

(NCT03405818)
Timeframe: Baseline, Week 52

Interventionmilligram per deciliter (mg/dL) (Mean)
Change at Week 52: BilirubinChange at Week 52: CreatinineChange at Week 52: Glucose [non-fasting]Change at Week 52: Urea Nitrogen
Kerydin-0.010.045.9-0.7

[back to top]

Change From Baseline in Chemistry Parameters (Potassium and Sodium) at Week 24

(NCT03405818)
Timeframe: Baseline, Week 24

Interventionmillimole per liter (mmol/L) (Mean)
Baseline: PotassiumBaseline: SodiumChange at Week 24: PotassiumChange at Week 24: Sodium
Kerydin4.25138.0-0.051.6

[back to top]

Change From Baseline in Chemistry Parameters (Potassium and Sodium) at Week 52

(NCT03405818)
Timeframe: Baseline, Week 52

Interventionmillimole per liter (mmol/L) (Mean)
Change at Week 52: PotassiumChange at Week 52: Sodium
Kerydin0.002.1

[back to top]

Change From Baseline in Hematology Parameter (Erythrocytes) at Week 24

(NCT03405818)
Timeframe: Baseline, Week 24

Intervention10^12 cells per liter (Mean)
BaselineChange at Week 24
Kerydin4.7860.045

[back to top]

Change From Baseline in Hematology Parameter (Hematocrit) at Week 24

(NCT03405818)
Timeframe: Baseline, Week 24

Interventionvolume percentage of red blood cells (Mean)
BaselineChange at Week 24
Kerydin42.040.57

[back to top]

Change From Baseline in Hematology Parameters (Hemoglobin) at Week 24

(NCT03405818)
Timeframe: Baseline, Week 24

Interventiongram per deciliter (g/dL) (Mean)
BaselineChange at Week 24
Kerydin13.790.11

[back to top]

Change From Baseline in Hematology Parameters (Leukocytes and Platelets) at Week 24

(NCT03405818)
Timeframe: Baseline, Week 24

Intervention10^9 cells per liter (Mean)
Baseline: LeukocytesBaseline: PlateletsChange at Week 24: LeukocytesChange at Week 24: Platelets
Kerydin7.11255.6-0.51-4.1

[back to top]

Change From Baseline in Hematology Parameters (Leukocytes and Platelets) at Week 52

(NCT03405818)
Timeframe: Baseline, Week 52

Intervention10^9 cells per liter (Mean)
Change at Week 52: LeukocytesChange at Week 52: Platelets
Kerydin-0.62-9.4

[back to top]

Change From Baseline in Hematology Parameters (Leukocytes: Basophils, Eosinophils, Lymphocytes, Monocytes and Neutrophils) at Week 24

(NCT03405818)
Timeframe: Baseline, Week 24

Interventionpercentage of leukocytes (Mean)
Baseline: Basophils/LeukocytesBaseline: Eosinophil/LeukocytesBaseline: Lymphocytes/LeukocytesBaseline: Monocytes/LeukocytesBaseline: Neutrophils/LeukocytesChange at Week 24: Basophils/LeukocytesChange at Week 24: Eosinophil/LeukocytesChange at Week 24: Lymphocytes/LeukocytesChange at Week 24: Monocytes/LeukocytesChange at Week 24: Neutrophils/Leukocytes
Kerydin0.63.334.46.855.10.1-0.51.1-0.2-0.7

[back to top]

Change From Baseline in Vital Sign (Respiratory Rate) at Week 52

Respiratory rate was defined as the number of inspirations per minute. (NCT03405818)
Timeframe: Baseline, Week 52

InterventionBreaths per minute (Mean)
Kerydin-0.5

[back to top]

Change From Baseline in Vital Sign (Blood Pressure) at Week 24

(NCT03405818)
Timeframe: Baseline, Week 24

Interventionmillimeter of mercury (mmHg) (Mean)
Baseline: Systolic Blood PressureBaseline: Diastolic Blood PressureChange at Week 24: Systolic Blood PressureChange at Week 24: Diastolic Blood Pressure
Kerydin110.968.30.41.0

[back to top]

Change From Baseline in Vital Sign (Blood Pressure) at Week 52

(NCT03405818)
Timeframe: Baseline, Week 52

Interventionmillimeter of mercury (mmHg) (Mean)
Change at Week 52: Systolic Blood PressureChange at Week 52: Diastolic Blood Pressure
Kerydin0.11.0

[back to top]

Change From Baseline in Vital Sign (Pulse Rate) at Week 24

Pulse rate was defined as the number of pulsations noted in a peripheral artery per minute after participant rested supine for 5 minutes. (NCT03405818)
Timeframe: Baseline, Week 24

InterventionBeats per minute (bpm) (Mean)
BaselineChange at Week 24
Kerydin76.2-3.0

[back to top]

Change From Baseline in Vital Sign (Respiratory Rate) at Week 24

Respiratory rate was defined as the number of inspirations per minute. (NCT03405818)
Timeframe: Baseline, Week 24

InterventionBreaths per minute (Mean)
BaselineChange at Week 24
Kerydin16.10.2

[back to top]

Number of Participants With Adverse Events (AEs) By Severity

An AE was any untoward medical occurrence in a participant who received study drug without regard to possibility of causal relationship. AEs were classified as mild, moderate and severe based on severity assessment by investigator and defined as: Mild = symptoms barely noticeable to the participant or does not make the participant uncomfortable; moderate = symptoms of a sufficient severity to make the participant uncomfortable; severe = symptoms of a sufficient severity to cause the participant severe discomfort. (NCT03405818)
Timeframe: Baseline up to 28 days after last dose of study drug (up to Week 52)

InterventionParticipants (Count of Participants)
MildModerateSevere
Kerydin12162

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Number of Participants With Local Tolerability Reactions by Severity

Local tolerability reactions consisted of burning/stinging, induration/edema, oozing and crusting, pruritus, erythema, and scaling. Here 0 indicates None, 1 (Mild), 2 (Moderate) and 3 (severe). Grading details are as follows: Burning/Stinging (0: no stinging/burning, 1: slight warm, 2: definite warm, 3: hot); Induration/Edema (0: no elevation, 1: barely perceptible elevation, 2: clearly perceptible elevation but not extensive, 3: marked and extensive elevation); Oozing and Crusting (0: absent, 1: faint signs of oozing, 2: definite oozing, 3: marked and extensive oozing); Pruritus (0: no pruritus, 1: occasional, slight itching, 2: constant itching which is not disturbing sleep, 3: severe bothersome itching/scratching which is disturbing sleep); Erythema (0: no redness present, 1: faintly detectable erythema; very light pink, 2: dull red, 3: deep/dark red); Scaling (0: no scaling, 1: barely perceptible shedding, 2: obvious but not profuse scaling, 3: heavy scale production). (NCT03405818)
Timeframe: Baseline up to Week 52

InterventionParticipants (Count of Participants)
None Burning/StingingMild Burning/StingingModerate Burning/StingingSevere Burning/StingingNone Induration/EdemaMild Induration/EdemaModerate Induration/EdemaSevere Induration/EdemaNone Oozing and CrustingMild Oozing and CrustingModerate Oozing and CrustingSevere Oozing and CrustingNone PruritusMild PruritusModerate PruritusSevere PruritusNone ErythemaMild ErythemaModerate ErythemaSevere ErythemaNone ScalingMild ScalingModerate ScalingSevere Scaling
Kerydin540105342154210532105062051431

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Number of Participants With Treatment-Emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)

An AE was any untoward medical occurrence in a participant who received study drug without regard to possibility of causal relationship. An SAE was an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly. Treatment-emergent are events between first dose of study drug and up to 28 days after last dose that were absent before treatment or that worsened relative to pre-treatment state. AEs included both serious and non-serious AEs. (NCT03405818)
Timeframe: Baseline up to 28 days after last dose of study drug (up to Week 52)

InterventionParticipants (Count of Participants)
Participants with AEsParticipants with SAEs
Kerydin301

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Percentage of Participants With Almost Complete Cure of Target Great Toenail (TGT) at Week 24 and 52

Almost complete cure was defined as almost clear nail and negative mycology (negative mycology was defined as negative fungal culture and negative KOH wet mount). (NCT03405818)
Timeframe: Week 24, 52

Interventionpercentage of participants (Number)
Week 24Week 52
Kerydin1014.9

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Percentage of Participants With Clinical Efficacy of Target Great Toenail (TGT) at Week 24 and 52

Clinical efficacy target great toenail (TGT) was defined as completely clear nail or almost clear nail. (NCT03405818)
Timeframe: Week 24, 52

Interventionpercentage of participants (Number)
Week 24Week 52
Kerydin1025.5

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Percentage of Participants With Mycological Cure of Target Great Toenail (TGT) at Week 24 and 52

Mycological cure was defined as negative mycology of the TGT. Negative mycology was defined as negative fungal culture and negative potassium hydroxide (KOH) wet mount. Participants with only one result for either fungal culture or KOH were excluded from this analysis. (NCT03405818)
Timeframe: Week 24, 52

Interventionpercentage of participants (Number)
Week 24Week 52
Kerydin38.036.2

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Percentage of Participants With Negative Fungal Culture of the Target Great Toenail (TGT) at Weeks 24 and 52

(NCT03405818)
Timeframe: Week 24, 52

Interventionpercentage of participants (Number)
Week 24Week 52
Kerydin9687.2

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Area Under the Plasma Concentration-Time Curve Extrapolated to Infinity (AUCinf) of Tavaborole

(NCT03405818)
Timeframe: Pre-dose, 4, 6, 8, 24 hours post-dose on Day 29

Interventionhour*nanogram per milliliter (hr*ng/mL) (Mean)
Kerydin124.820

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Area Under the Plasma Concentration-Time Curve From Hour Zero to Hour 24 (AUC24) of Tavaborole

AUC24 was defined as the area under the plasma concentration-time curve from hour 0 to hour 24. AUC24 was calculated using the linear trapezoidal rule. (NCT03405818)
Timeframe: Pre-dose, 4, 6, 8, 24 hours post-dose on Day 29

Interventionhour*nanogram per milliliter (hr*ng/mL) (Mean)
Kerydin102.273

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Change From Baseline in Hematology Parameter (Erythrocytes) at Week 52

(NCT03405818)
Timeframe: Baseline, Week 52

Intervention10^12 cells per liter (Mean)
Kerydin-0.009

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Change From Baseline in Hematology Parameter (Hematocrit) at Week 52

(NCT03405818)
Timeframe: Baseline, Week 52

Interventionvolume percentage of red blood cells (Mean)
Kerydin-0.12

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Change From Baseline in Hematology Parameters (Hemoglobin) at Week 52

(NCT03405818)
Timeframe: Baseline, Week 52

Interventiongram per deciliter (g/dL) (Mean)
Kerydin0.06

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Change From Baseline in Vital Sign (Pulse Rate) at Week 52

Pulse rate was defined as the number of pulsations noted in a peripheral artery per minute after participant rested supine for 5 minutes. (NCT03405818)
Timeframe: Baseline, Week 52

InterventionBeats per minute (bpm) (Mean)
Kerydin-3.9

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Elimination Half-Life of Tavaborole

Elimination half-life (t1/2) was defined as the time required for the body to eliminate half of the drug than its original concentration. (NCT03405818)
Timeframe: Pre-dose, 4, 6, 8, 24 hours post-dose on Day 29

Interventionhour (Mean)
Kerydin9.783

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Elimination Rate Constant of Tavaborole

Elimination rate constant was defined as the rate at which a drug was removed from the body. (NCT03405818)
Timeframe: Pre-dose, 4, 6, 8, 24 hours post-dose on Day 29

Interventionper hour (Mean)
Kerydin0.08528

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Change From Baseline in Hematology Parameters (Leukocytes: Basophils, Eosinophils, Lymphocytes, Monocytes and Neutrophils) at Week 52

(NCT03405818)
Timeframe: Baseline, Week 52

Interventionpercentage of leukocytes (Mean)
Change at Week 52: Basophils/LeukocytesChange at Week 52: Eosinophils/LeukocytesChange at Week 52: Lymphocytes/LeukocytesChange at Week 52: Monocytes/LeukocytesChange at Week 52: Neutrophils/Leukocytes
Kerydin0.10.30.7-0.5-0.7

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Maximum Observed Plasma Concentration (Cmax) of Tavaborole

(NCT03405818)
Timeframe: Pre-dose, 4, 6, 8, 24 hours post-dose on Day 29

InterventionNanogram per milliliter (ng/mL) (Mean)
Kerydin5.4049

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Percentage of Participants With Complete Cure of Target Great Toenail (TGT) at Week 52

Complete cure was defined as completely clear nail, negative fungal culture and negative potassium hydroxide (KOH) wet mount. (NCT03405818)
Timeframe: Week 52

Interventionpercentage of participants (Number)
Kerydin8.5

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Time to Maximum Observed Plasma Concentration (Tmax) of Tavaborole

(NCT03405818)
Timeframe: Pre-dose, 4, 6, 8, 24 hours post-dose on Day 29

Interventionhour (Median)
Kerydin6.000

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Change From Baseline in Chemistry Parameters (Alanine Aminotransferase, Alkaline Phosphatase and Aspartate Aminotransferase) at Week 24

(NCT03405818)
Timeframe: Baseline, Week 24

InterventionInternational Unit per liter (IU/L) (Mean)
Baseline: Alanine AminotransferaseBaseline: Alkaline PhosphataseBaseline: Aspartate AminotransferaseChange at Week 24:Alanine AminotransferaseChange at Week 24:Alkaline PhosphataseChange at Week 24:Aspartate Aminotransferase
Kerydin14.6178.721.7-1.7-1.5-3.3

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Change From Baseline in Chemistry Parameters (Alanine Aminotransferase, Alkaline Phosphatase and Aspartate Aminotransferase) at Week 52

(NCT03405818)
Timeframe: Baseline, Week 52

InterventionInternational Unit per liter (IU/L) (Mean)
Change at Week 52:Alanine AminotransferaseChange at Week 52:Alkaline PhosphataseChange at Week 52:Aspartate Aminotransferase
Kerydin-1.6-18.4-2.7

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Change From Baseline in Chemistry Parameters (Albumin and Protein) at Week 24

(NCT03405818)
Timeframe: Baseline, Week 24

Interventiongram per deciliter (g/dL) (Mean)
Baseline: AlbuminBaseline: ProteinChange at Week 24: AlbuminChange at Week 24: Protein
Kerydin4.496.94-0.05-0.04

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