Drug intelligence / Profile preview

esafoxolaner

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

Overview

Esafoxolaner is a small molecule antiparasitic drug belonging to the aryl isoxazoline class, specifically the (S)-enantiomer of afoxolaner. Developed by Boehringer Ingelheim Animal Health, it is primarily used in feline veterinary medicine. The drug acts as an ectoparasiticide by potently inhibiting insect and acarine ligand-gated chloride channels, particularly those gated by gamma-aminobutyric acid (GABA) and glutamate. This inhibition blocks the transfer of chloride ions across cell membranes, leading to uncontrolled hyperexcitation of the parasite's central nervous system and subsequent death. It is FDA-approved as the key ectoparasiticidal component of the topical solution NexGard COMBO for the treatment and prevention of flea and tick infestations, ear mites, and various internal parasites in cats, including heartworm disease prevention.

Other names
(S)-afoxolaner
02

Targets

RDL (Insect GABA-gated chloride channel)GluCl (Glutamate-gated chloride channel)

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