Drug intelligence / Profile preview

sarolaner

Development stage
Unknown
Lead developer
Zoetis
Modality
Small Molecules
Administration
Oral, Topical
01

Overview

Sarolaner is a small molecule ectoparasiticide of the isoxazoline class, developed for veterinary use in dogs. It acts as an oral acaricide and insecticide, indicated primarily for the treatment and prevention of flea (Ctenocephalides felis) infestations and the treatment and control of tick infestations (including Amblyomma americanum, Amblyomma maculatum, Dermacentor variabilis, Ixodes scapularis, Rhipicephalus sanguineus, Haemaphysalis longicornis) in dogs aged 6 months or older and weighing at least 2.8 pounds. Sarolaner works by inhibiting neurotransmission through antagonism of gamma aminobutyric acid (GABA) receptors and glutamate-gated chloride channels in arthropods’ nervous systems. This leads to uncontrolled neuromuscular activity resulting in death of fleas or ticks. Sarolaner is rapidly absorbed after oral administration with high bioavailability (>85%), has a long half-life (~11–12 days), is highly protein-bound (>99.9%), minimally metabolized in dogs, and eliminated mainly via biliary excretion into feces[1][4][5][8]. It was developed by Zoetis.

Brand names
Simparica
Other names
sarolaner
02

Targets

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

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