afoxolaner
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 Source | ID |
|---|---|
| PubMed CID | 25154249 |
| CHEMBL ID | 2219412 |
| SCHEMBL ID | 119580 |
| MeSH ID | M000595012 |
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)
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.
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.
Pharmacokinetics
| Excerpt | Reference | Relevance |
|---|---|---|
| " 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
| Excerpt | Reference | Relevance |
|---|---|---|
| "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.
Research
Studies (69)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 49 (71.01) | 24.3611 |
| 2020's | 20 (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.
| This Compound (42.49) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 25 (35.71%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 2 (2.86%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 43 (61.43%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||