Sarolaner is an acaricide and insecticide belonging to the isoxazoline family. The primary target of action of sarolaner in insects and acarines is functional blockade of ligand-gated chloride channels (GABA-receptors and glutamate-receptors). Sarolaner blocks GABA- and glutamate-gated chloride channels in the central nervous system of insects and acarines. Sarolaner binding to these receptors prevents the uptake of chloride ions by GABA and glutamate gated ion channels, thus resulting in increased nerve stimulation and death of the target parasite. Sarolaner exhibits higher functional potency to block insect/acarine receptors compared to mammalian receptors. Sarolaner does not interact with known insecticidal binding sites of nicotinic or other GABAergic insecticides such as neonicotinoids, fiproles, milbemycins, avermectins, and cyclodienes. Sarolaner is active against adult fleas (Ctenocephalides felis and Ctenocephalides canis), several tick species such as Dermacentor reticulatus, Ixodes hexagonus, Ixodes ricinus and Rhipicephalus sanguineus, as well as the mites Demodex canis and Sarcoptes scabiei var. canis.

Ticks on the animal prior to administration or from new infestations after product administration are killed within 48 hours. For the species I. ricinus, this onset of efficacy is within 24 hours, during the 35-day period after product administration.

For fleas, the onset of efficacy is within 12 to 24 hours of attachment for five weeks after product administration. Fleas on the animal prior to administration are killed within 8 hours. The veterinary medicinal product kills newly emerged fleas on the dog before they can lay eggs and therefore it prevents environmental flea contamination in areas to which the dog has access.

Moxidectin is a second-generation macrocyclic lactone of the milbemycin family. Its principal mode of action is interfering with neuromuscular transmission at the level of the glutamate-gated chloride channels and, to a lesser extent, of GABA (gamma amino butyric acid)-gated channels. This interference leads to the opening of the chloride channels on the postsynaptic junction to allow the inflow of chloride ions. This results in flaccid paralysis and eventual death of parasites exposed to the drug. Moxidectin is active against adults of Toxocara canis, L4 larvae and immature stages (L5) of Ancylostoma caninum, L4 of Dirofilaria immitis, adults and immature stages (L5) of Angiostrongylus vasorum, immature stages of Thelazia callipaeda.

Pyrantel is a nicotinic acetylcholine (ACh) channel receptor (nAChR) agonist. Pyrantel mimics the agonist effects of ACh through high affinity binding to subtype specific ionophoric nAChRs in nematodes, while not binding at muscarinic mAChRs. Following receptor binding, the channel opens to allow the influx of cations resulting in a depolarization and excitatory effects on nematode muscle, ultimately leading to spastic paralysis of the worm and death. Pyrantel is active against immature stages (L5) and adults of Toxocara canis, adults of Ancylostoma caninum, Toxascaris leonina and Uncinaria stenocephala.

In this fixed combination, moxidectin and pyrantel provide complementary anthelmintic efficacy through distinct mechanisms of action. In particular, both active substances contribute to the overall efficacy against the gastrointestinal nematodes Ancylostoma caninum and Toxocara canis.

Sarolaner is readily and rapidly absorbed systemically following oral dosing, reaching maximum concentrations in plasma within 3.5 hours (tmax) after administration with a high bioavailability of 86.7%. Sarolaner is slowly eliminated from plasma (half-life of approximately 12 days) via biliary excretion and elimination through the faeces with minor contributions of metabolic clearance.

Moxidectin is readily and rapidly absorbed systemically following oral dosing, reaching maximum concentrations in plasma within 2.4 hours (tmax) after administration and with 66.9% bioavailability. Moxidectin is slowly eliminated from plasma (half-life of approximately 11 days) via biliary excretion and elimination through the faeces with minor contributions of metabolic clearance.

Pyrantel embonate is poorly absorbed and the absorbed portion has a tmax of 1.5 hours and half-life of 7.7 hours. Pyrantel is eliminated through faeces and the small absorbed portion is eliminated mainly via urine.

The prandial state of the dogs does not affect the extent of absorption of sarolaner and moxidectin.