Drug intelligence / Profile preview

afoxolaner

Development stage
Unknown
Lead developer
Boehringer Ingelheim
Modality
Small Molecules
Administration
Oral
01

Overview

Afoxolaner is an insecticide and acaricide belonging to the isoxazoline class of compounds. It is primarily used in veterinary medicine for the treatment and prevention of flea and tick infestations in dogs. Afoxolaner acts as an antagonist at insect and acarine gamma-aminobutyric acid (GABA)-gated chloride channels. By binding to a unique site on these channels, it blocks pre-and post-synaptic transfer of chloride ions across cell membranes in insects and acarines. This results in prolonged hyperexcitation of their central nervous system leading to death. The drug demonstrates selective toxicity due to differences between insect/acarine GABA receptors and those found in mammals[1][3][7][8]. Afoxolaner is administered orally (as chewable tablets) with high systemic absorption and provides extended effectiveness against fleas (Ctenocephalides felis) and several tick species including Dermacentor reticulatus/variabilis, Ixodes ricinus/scapularis, Rhipicephalus sanguineus, Amblyomma americanum, and Haemaphysalis longicornis[4][8]. It prevents household contamination by killing fleas before egg production. Developers: Boehringer Ingelheim

Brand names
NexGardFrontpro
Other names
4-[(5 RS)-5-(5-Chloro-α,α,α-trifluoro-m-tolyl)-4,5-dihydro-5-(trifluoromethyl)-1,2-oxazol-3-yl]-N-[2-oxo-2-(2,2,2-trifluoroethylamino)ethyl]naphthalene-1-carboxamide
02

Targets

RDL (Insect GABA-gated chloride channel)

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