Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C26H17ClF9N3O3 |
| Molecular Weight | 625.87 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
FC(F)(F)CNC(=O)CNC(=O)C1=C2C=CC=CC2=C(C=C1)C3=NOC(C3)(C4=CC(=CC(Cl)=C4)C(F)(F)F)C(F)(F)F
InChI
InChIKey=OXDDDHGGRFRLEE-UHFFFAOYSA-N
InChI=1S/C26H17ClF9N3O3/c27-15-8-13(7-14(9-15)25(31,32)33)23(26(34,35)36)10-20(39-42-23)18-5-6-19(17-4-2-1-3-16(17)18)22(41)37-11-21(40)38-12-24(28,29)30/h1-9H,10-12H2,(H,37,41)(H,38,40)
Afoxolaner (brand name NexGard) is a member of an isoxazoline class of compounds, which is used to kill adult fleas and is indicated for the treatment and prevention of flea infestations, and the treatment and control of Black-legged tick, American Dog tick, Lone Star tick, and Brown dog tick infestations in dogs and puppies. Afoxolaner is a member of the isoxazoline family, shown to bind at a binding site to inhibit insect and acarine ligand-gated chloride channels, in particular those gated by the neurotransmitter gamma-aminobutyric acid (GABA), thereby blocking pre- and post-synaptic transfer of chloride ions across cell membranes. Afoxolaner blocks native and expressed insect GABA-gated chloride channels with nanomolar potency. Prolonged afoxolaner-induced hyperexcitation results in uncontrolled activity of the central nervous system and death of insects and acarines.
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Afoxolaner against fleas: immediate efficacy and resultant mortality after short exposure on dogs. | 2014 |
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| Discovery and mode of action of afoxolaner, a new isoxazoline parasiticide for dogs. | 2014 Apr 2 |
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| Evaluation of the efficacy of monthly oral administration of afoxolaner plus milbemycin oxime (NexGard Spectra(®), Merial) in the prevention of adult Spirocerca lupi establishment in experimentally infected dogs. | 2016 Aug 15 |
Sample Use Guides
in veterinary:
NexGard is given orally once a month, at the minimum dosage of 1.14 mg/lb (2.5 mg/kg).
Dosing Schedule:
Body Weight Afoxolaner Per Chewable (mg) Chewables Administered
4.0 to 10.0 lbs. 11.3 One
10.1 to 24.0 lbs. 28.3 One
24.1 to 60.0 lbs. 68 One
60.1 to 121.0 lbs. 136 One
Over 121.0 lbs. Administer the appropriate combination of chewables
Route of Administration:
Oral
A dosage and time titration effect was clearly identified for fleas ingesting afoxolaner with mean efficacies of >95% recorded for fleas fed blood containing the compound at concentrations of 0.16, 0.08 and 0.02 μg/ml at the 24, 48 and 72 h observation points, respectively. There was only 1%, 2.3% and 2.3% mean mortality in the vehicle-treated control at the 24, 48 and 72 h observation points, respectively. Therefore, afoxolaner was judged to be highly active against fleas following ingestion in blood.
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| Classification Tree | Code System | Code | ||
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EMA VETERINARY ASSESSMENT REPORTS |
NEXGARD SPECTRA [AUTHORIZED]
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CFR |
21 CFR 520.43
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WHO-VATC |
QP53BX04
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EMA VETERINARY ASSESSMENT REPORTS |
NEXGARD [AUTHORIZED]
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ZZ-56
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m11748
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afoxolaner
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Afoxolaner
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CHEMBL2219412
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02L07H6D0U
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1442093
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ACTIVE MOIETY
