Drug intelligence / Profile preview

afoxolaner + milbemycin oxime

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

Overview

Afoxolaner + milbemycin oxime is a fixed-dose combination veterinary pharmaceutical used primarily in dogs for the treatment and prevention of ectoparasite (fleas, ticks, mites) and endoparasite (intestinal nematodes, heartworm) infections. Afoxolaner is an ectoparasiticide from the isoxazoline class that acts as an antagonist at GABA-gated chloride channels in arthropods, leading to hyperexcitation and death of fleas and ticks. Milbemycin oxime is a macrocyclic lactone endectocide that disrupts glutamate neurotransmission in invertebrates by increasing chloride ion influx through glutamate-gated chloride channels, resulting in paralysis and death of susceptible parasites. The combination provides broad-spectrum efficacy against adult fleas (Ctenocephalides felis), several tick species (including Dermacentor variabilis, Ixodes scapularis), demodicosis caused by Demodex canis, heartworm disease prevention (Dirofilaria immitis), and treatment/control of intestinal nematode infections such as hookworms (Ancylostoma caninum/braziliense/ceylanicum), roundworms (Toxocara canis/Toxascaris leonina), whipworms (Trichuris vulpis), among others. It is administered orally as a palatable chewable tablet once monthly[1][2][3][4][5][6][7].

02

Targets

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

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