Page last updated: 2024-11-13

afoxolaner

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Description

afoxolaner: an oral, chewable insecticide-acaricide to control fleas and ticks in dogs [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID25154249
CHEMBL ID2219412
SCHEMBL ID119580
MeSH IDM000595012

Synonyms (42)

Synonym
CHEMBL2219412
4-(5-(3-chloro-5-(trifluoromethyl)phenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl)-n-(2-oxo-2-((2,2,2-trifluoroethyl)amino)ethyl)naphthalene-1-carboxamide
1093861-60-9
unii-02l07h6d0u
afoxolaner [usan:inn]
02l07h6d0u ,
afoxolaner
1-naphthalenecarboxamide, 4-(5-(3-chloro-5-(trifluoromethyl)phenyl)-4,5-dihydro-5-(trifluoromethyl)-3-isoxazolyl)-n-(2-oxo-2-((2,2,2-trifluoroethyl)amino)ethyl)-
D10361
afoxolaner (usan)
SCHEMBL119580
afoxolaner conponent of nexgard spectra
afoxolaner [inn]
nexgard
4-(5-(3-chloro-5-(trifluoromethyl)phenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl(-n- (2-oxo-2-((2,2,2-trifluoroethyl)amino)ethyl(naphthalene-1-carboxamide
afoxolaner [mi]
nexgard spectra conponent afoxolaner
afoxolaner [green book]
afoxolaner [usan]
1-naphthalenecarboxamide, 4-(5-(3-chloro-5-(trifluoromethyl)phenyl)-4,5-dihydro-5- (trifluoromethyl)-3-isoxazolyl)-n-(2-oxo-2-((2,2,2-trifluoroethyl)amino)ethyl)-
afoxolaner [ema epar veterinary]
DTXSID50148921 ,
4-[5-[3-chloro-5-(trifluoromethyl)phenyl]-4,5-dihydro-5-(trifluoromethyl)-3-isoxazolyl]-n-[2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl]-1-naphthalenecarboxamide; 4-[5-(3-chloro-5-trifluoromethylphenyl)-5-trifluoromethyl-4,5-dihydro-isoxazol-3-yl]-naphthale
BCP21108
HY-16974
Q21051346
c26h17clf9n3o3
4-[(5r)-5-[3-chloro-5-(trifluoromethyl)phenyl]-5-(trifluoromethyl)-4h-1,2-oxazol-3-yl]-n-[2-oxo-2-(2,2,2-trifluoroethylamino)ethyl]naphthalene-1-carboxamide
CS-0013215
MS-30823
4-(5-(3-chloro-5-(trifluoromethyl)phenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl)-n-(2-oxo-2-((2,2,2-trifluoroethyl)amino)ethyl)-1-naphthamide
4-[5-[3-chloro-5-(trifluoromethyl)phenyl]-5-(trifluoromethyl)-4h-1,2-oxazol-3-yl]-n-[2-oxo-2-(2,2,2-trifluoroethylamino)ethyl]naphthalene-1-carboxamide
EX-A3267
4-[5-[3-chloro-5-(trifluoromethyl)phenyl]-4,5-dihydro-5-(trifluoromethyl)-3-isoxazolyl]-n-[2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl]-1-naphthalenecarboxamide
oxdddhggrfrlee-uhfffaoysa-n
afoxolaner 100 microg/ml in acetonitrile
AKOS040740686
dtxcid5071412
afoxolanerum
4-(5-(3-chloro-5-(trifluoromethyl)-phenyl)-4,5-dihydro-5-(trifluoromethyl)-3-isoxazolyl)-n-(2-oxo-2-((2,2,2-trifluoroethyl)amino)ethyl-1-naphthalenecarboxamide
afoxolaner (ema epar veterinary)
4-(5-(3-chloro-5-(trifluoromethyl)phenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl(-n-(2-oxo-2-((2,2,2-trifluoroethyl)amino)ethyl(naphthalene-1-carboxamide

Research Excerpts

Overview

Afoxolaner is a novel insecticidal and acaricidal of the isoxazoline family. Used in veterinary practice to control infestation of dogs by fleas, ticks, and mites (NexGard, Boehringer Ingelheim)

ExcerptReferenceRelevance
"Afoxolaner is a novel insecticidal and acaricidal of the isoxazoline family, which is used in veterinary practice to control infestation of dogs by fleas, ticks, and mites (NexGard, Boehringer Ingelheim). "( Comparative efficacy of afoxolaner and ivermectin in dogs naturally infested with Rhipicephalus sanguineus sensu lato: A clinical field study conducted in Thailand.
Beugnet, F; Meesaimongkon, P; Srifawattana, N; Tangtrongsup, S; Thitaram, N; Tinkruejeen, G; Tiwananthagorn, S, 2019
)
2.26
"Afoxolaner is an isoxazoline that has been shown to be effective against these ectoparasites without known adverse effects."( Use of afoxolaner for the treatment of lice (Goniodes pavonis) in different genera (Chrysolophus spp, Lophura spp, Phasianus spp, and Syrmaticus spp) and species of pheasants and West Mexican Chachalacas (Ortalis poliocephala).
Álvarez Zavala, MLÁ; Cruz López, E; Galicia Franco, E; Heredia Cárdenas, R; Miranda Contreras, L; Rangel Díaz, J; Romero Núñez, C; Yarto Jaramillo, E, 2020
)
1.73
"Afoxolaner is a molecule from the isoxazoline family with proven ectoparasiticide action against fleas, ticks and mites in dogs."( Efficacy of afoxolaner (NexGard®) on the treatment of myiasis caused by the New World screwworm fly Cochliomyia hominivorax (Diptera: Calliphoridae) in naturally infested dogs.
Beugnet, F; Cutolo, AA; Menz, I; Perier, N; Silva, FO; Thyssen, P, 2021
)
1.72
"Afoxolaner is a drug belonging to the isoxazolines' family, and it is recommended for ectoparasite control in dogs. "( Efficacy of afoxolaner in the treatment of otodectic mange in naturally infested cats.
Barbieri Bastos, IP; Botelho, CB; Campos, DR; Correia, TR; Fernandes, JI; Lopes, NL; Machado, MA; Scott, FB, 2018
)
2.3
"Afoxolaner is an isoxazoline compound characterized by a good safety profile and extended effectiveness against fleas and ticks on dogs following a single oral administration. "( Discovery and mode of action of afoxolaner, a new isoxazoline parasiticide for dogs.
Benner, EA; Confalone, PN; Cordova, D; Dietrich, RF; Gould, BR; Hartline, EJ; Jones, GS; Kinney, JB; Lahm, GP; Long, JK; McDowell, RG; Rhoades, DF; Schroeder, ME; Shoop, WL; Waddell, ME; Wagerle, T; Xu, M, 2014
)
2.13
"Afoxolaner is a member of one of the newest classes of antiparasitic agents, known as antiparasitic isoxazolines."( The intravenous and oral pharmacokinetics of afoxolaner used as a monthly chewable antiparasitic for dogs.
Drag, M; Harriman, J; Huang, R; Kvaternick, V; Letendre, L; Soll, M, 2014
)
1.38
"Afoxolaner is a new antiparasitic molecule from the isoxazoline family that acts on insect acarine g-aminobutyric acid and glutamate receptors. "( Development and Validation of a Reversed-Phase Chiral HPLC Method to Determine the Chiral Purity of Bulk Batches of (
Kumar, S; Padivitage, N; Rustum, A, 2017
)
1.9

Treatment

Treatment with afoxolaner or fluralaner does not impact on cutaneous Demodex populations of normal dogs over a 90 day period. Dogs treated with afOxolaner plus milbemycin oxime chewables had significantly (p≤0.0002) fewer nematodes than the untreated controls in all studies.

ExcerptReferenceRelevance
"The afoxolaner treated group had significantly fewer fleas than the untreated control group at 8, 12, and 24h (p<0.001)."( Assessment of the onset of action of afoxolaner against existing adult flea (Ctenocephalides felis) infestations on dogs.
Chester, TS; Drag, MD; Kunkle, BN; Larsen, DL, 2014
)
1.16
"Treatment with afoxolaner or fluralaner does not impact on cutaneous Demodex populations of normal dogs over a 90 day period."( Afoxolaner and fluralaner treatment do not impact on cutaneous Demodex populations of healthy dogs.
Altet, L; Ferrer, L; Lam, ATH; Zewe, CM, 2017
)
2.25
"Treatment with afoxolaner significantly decreased the number of peacocks positive for lice (P = 0.02) compared to the control group, in which the number of positive birds did not decrease. "( Effect of oral afoxolaner on naturally occurring infestations of peacocks by the louse Goniodes pavonis.
Heredia Cardenas, R; Miranda Contreras, L; Osorio Marquez, R; Rangel Díaz, J; Romero Núñez, C; Yarto Jaramillo, E, 2019
)
1.22
"Treatment with afoxolaner resulted in efficacies of 98.8-100% within 48 h on existing tick infestations, while the efficacy against new tick infestations was >95.7% over five weeks."( Assessment of the efficacy of orally administered afoxolaner against Rhipicephalus sanguineus sensu lato.
Daly, S; Drag, M; Dumont, P; Kunkle, B; Larsen, D, 2014
)
1
"Dogs treated with afoxolaner plus milbemycin oxime chewables had significantly (p≤0.0002) fewer nematodes than the untreated controls in all studies."( Efficacy of oral afoxolaner plus milbemycin oxime chewables against induced gastrointestinal nematode infections in dogs.
Bowman, DD; Crafford, D; Dorr, P; Fankhauser, R; Hamel, D; Larsen, DL; Reinemeyer, CR; Ulrich, M; Yoon, S, 2016
)
1.1

Toxicity

Afoxolaner was shown to be safe when administered repeatedly in a soft chewable formulation at up to 5× the maximum exposure dose in dogs as young as 8 weeks of age.

ExcerptReferenceRelevance
" Based upon the results of this study, afoxolaner was shown to be safe when administered repeatedly in a soft chewable formulation at up to 5× the maximum exposure dose in dogs as young as 8 weeks of age."( Safety evaluation of orally administered afoxolaner in 8-week-old dogs.
Drag, M; Harriman, J; Larsen, D; Saik, J, 2014
)
0.94
" No treatment-related adverse experiences were observed throughout the study."( Efficacy against nematode infections and safety of afoxolaner plus milbemycin oxime chewable tablets in domestic dogs under field conditions in Europe.
Breiltgens, T; Brianti, E; Capári, B; Dantas-Torres, F; Dollhofer, D; Gau, M; Jeannin, P; Joachim, A; Kaulfuß, KH; Kirkova, Z; Kley, K; Knaus, M; Lebon, W; Lechner, J; Mallouk, Y; Mihalca, AD; Mirabito, R; Petkevičius, S; Rapti, D; Rehbein, S; Sedeilhan, M; Shukullari, E; Visser, M, 2017
)
0.71
" Based upon the results of this study, afoxolaner/milbemycin oxime soft chewables were shown to be safe when administered repeatedly at up to 5× the maximum exposure dose in dogs as young as 8 weeks of age."( Safety evaluation of orally administered afoxolaner and milbemycin oxime in eight-week-old dogs.
Drag, M; Harriman, J; Larsen, D; Letendre, L; Saik, J; Yoon, S, 2017
)
0.99
" The absence of treatment-related adverse events confirms the safety of lotilaner in dogs."( A randomized, controlled field study to assess the efficacy and safety of lotilaner flavored chewable tablets (Credelio™) in eliminating fleas in client-owned dogs in the USA.
Cavalleri, D; Chappell, K; Coble, S; Drake, J; Karadzovska, D; Murphy, M; Nanchen, S; Wiseman, S, 2017
)
0.46
"No adverse events related to the two products, nor skin reactions, general signs, or changes in the haematological profile, were observed during the study."( Six-month field efficacy and safety of the combined treatment of dogs with Frontline Tri-Act® and NexGard Spectra®.
Abbate, JM; Arfuso, F; Beugnet, F; Brianti, E; Gaglio, G; Giannetto, S; Halos, L; Napoli, E, 2018
)
0.48
"Simparica Trio™ administered orally once monthly for two consecutive treatments was safe and effective against natural flea infestations and substantially improved clinical signs associated with FAD in client-owned dogs in a field study conducted in the USA."( Safety and efficacy of a novel oral chewable combination tablet containing sarolaner, moxidectin and pyrantel (Simparica Trio™) against natural flea infestations in client-owned dogs in the USA.
Inskeep, T; Kryda, K; Mahabir, SP; Rugg, J, 2020
)
0.56
" Forty-two percent (1,157) reported no flea treatment or adverse events (AE), while 58% (1594) had been treated with some parasiticide for flea control, and of those that received a parasiticide, the majority, or 83% (1,325), received an isooxazoline."( Survey of canine use and safety of isoxazoline parasiticides.
Bullock, R; Carney, E; Dodds, WJ; Fritsche, HA; Jeffrey, J; Kimball, JP; Morgan, J; Palmieri, V, 2020
)
0.56
" Dogs were closely monitored for adverse reactions on the day of treatment and for the following two days."( Safety of oral afoxolaner formulated with or without milbemycin oxime in homozygous MDR1-deficient collie dogs.
Drag, M; Mitchell, E; Tielemans, E, 2022
)
1.07

Pharmacokinetics

ExcerptReferenceRelevance
" The terminal plasma half-life was 15."( The intravenous and oral pharmacokinetics of afoxolaner used as a monthly chewable antiparasitic for dogs.
Drag, M; Harriman, J; Huang, R; Kvaternick, V; Letendre, L; Soll, M, 2014
)
0.66

Bioavailability

ExcerptReferenceRelevance
"8 days, and oral bioavailability was 73."( The intravenous and oral pharmacokinetics of afoxolaner used as a monthly chewable antiparasitic for dogs.
Drag, M; Harriman, J; Huang, R; Kvaternick, V; Letendre, L; Soll, M, 2014
)
0.66

Dosage Studied

Hominivorax larvae, were treated with afoxolaner (NexGard®) as per label recommendations. At least the minimum dosage of 2.5mg/kg oral dosage demonstrated uniform and predictable af Oxolaner plasma concentrations above threshold levels required for efficacy.

ExcerptRelevanceReference
"5mg/kg oral dosage demonstrated uniform and predictable afoxolaner plasma concentrations above threshold levels required for efficacy for more than one month."( Discovery and mode of action of afoxolaner, a new isoxazoline parasiticide for dogs.
Benner, EA; Confalone, PN; Cordova, D; Dietrich, RF; Gould, BR; Hartline, EJ; Jones, GS; Kinney, JB; Lahm, GP; Long, JK; McDowell, RG; Rhoades, DF; Schroeder, ME; Shoop, WL; Waddell, ME; Wagerle, T; Xu, M, 2014
)
0.93
" Following the second dosing on study day 28-30, total on-dog flea burden was reduced by 100% on days 40-45 and 54-60."( Evaluation of afoxolaner chewables to control flea populations in naturally infested dogs in private residences in Tampa FL, USA.
Carithers, D; Chwala, M; Crevoiserat, L; Dryden, MW; Foley, KM; Hawkins, A; Jones, E; McGrady, JC; Patton, PR; Smith, V, 2015
)
0.78
" Group 4 was dosed once on Day 0 with Bravecto™."( Comparative efficacy of oral administrated afoxolaner (NexGard™) and fluralaner (Bravecto™) with topically applied permethrin/imidacloprid (Advantix(®)) against transmission of Ehrlichia canis by infected Rhipicephalus sanguineus ticks to dogs.
Crafford, D; Erasmus, H; Fourie, JJ; Jongejan, F; Schunack, B, 2016
)
0.7
" Prior studies in human and animal medicine have suggested that patients more closely adhere to prescriber dosing recommendations when they receive a longer-duration medication."( Dog owner flea/tick medication purchases in the USA.
Armstrong, R; Lavan, R; Normile, D; Tunceli, K, 2018
)
0.48
" Ectoparasiticide purchase patterns were compared for two products (afoxalaner and spinosad) with monthly dosing and one product (fluralaner) with an extended (12 week) dosing interval."( Dog owner flea/tick medication purchases in the USA.
Armstrong, R; Lavan, R; Normile, D; Tunceli, K, 2018
)
0.48
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (69)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's49 (71.01)24.3611
2020's20 (28.99)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 42.49

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

MetricThis Compound (vs All)
Research Demand Index42.49 (24.57)
Research Supply Index4.56 (2.92)
Research Growth Index4.60 (4.65)
Search Engine Demand Index126.99 (26.88)
Search Engine Supply Index3.98 (0.95)

This Compound (42.49)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials25 (35.71%)5.53%
Reviews0 (0.00%)6.00%
Case Studies2 (2.86%)4.05%
Observational0 (0.00%)0.25%
Other43 (61.43%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]