Lotilaner Chemical Properties

Density 

1.66±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO : ≥ 100 mg/mL (167.57 mM)

form 

Solid

pka

12.52±0.46(Predicted)

color 

White to off-white

InChIKey

HDKWFBCPLKNOCK-SFHVURJKSA-N

SMILES

C1(C(NCC(=O)NCC(F)(F)F)=O)SC(C2C[C@](C3=CC(Cl)=C(Cl)C(Cl)=C3)(C(F)(F)F)ON=2)=CC=1C

Lotilaner Usage And Synthesis

Description

Lotilaner is a representative of the isoxazolines, a new class of insecticides discovered in the 2000s.
Isoxazolines (Afoxolaner, Fluralaner, Lotilaner, and Sarolaner) Isoxazolines are insecticidal and arachnicidal substances that can be given orally, or topically as spot-ons, and act systemically in the blood circulation.
lotilaner (Credeliot), a novel oral isoxazoline against naturally occurring mange mite infestations in dogs caused by Demodex spp.
Lotilaner, like the other isooxazolines is active against fleas, mites, and ticks. After oral administration or topical application, it can kill fleas rapidly.

Uses

Lotilaner is a new member of the isoxazoline class for the treatment of flea and tick infestations in cats.

Indications

Lotilaner is a monthly chewable tablet for the treatment and prevention of fleas and ticks. It is used in dogs and puppies 8 weeks of age or older weighing 4.4 pounds or greater (Elanco, 2019).

Side effects

These include weight loss, elevated blood urea nitrogen, increased urination, and diarrhea (Elanco, 2019).

Mode of action

Lotilaner is available for oral administration to dogs (CREDELIO), i.e. it has a systemic mode of action. Ingested lotilaner is rapidly absorbed into blood and distributed throughout the whole body of the treated dog. Blood-sucking parasites (mainly fleas and ticks) are killed during their blood meal.
But the systemic mode of action means also that for fleas and/or ticks to be killed, they have to bite the dog first and suck enough blood before the ingested active ingredient kills them.
As other isoxazolines with insecticidal and tickicidal efficacy, lotilaner is a non-competitive GABA (gamma-aminobutyric acid) receptor antagonist, much more selective for GABA receptors in insects or ticks, than for those in mammals, including humans. It binds to chloride channels in nerve and muscle cells, which blocks the transmission of neuronal signals. Affected parasites are paralyzed and die.