Drug intelligence / Profile preview

lotilaner

Development stage
Approved
Lead developer
Tarsus Pharmaceuticals
Modality
Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Ophthalmic, Oral
01

Overview

Lotilaner is an ectoparasiticide of the isoxazoline class, used as a small molecule antiparasitic agent. It acts as a non-competitive antagonist of gamma-aminobutyric acid (GABA)-gated chloride channels, selectively targeting mites and certain insects. Inhibition of these channels causes spastic paralysis and death in target organisms such as *Demodex* mites, fleas, and ticks. Lotilaner was originally developed for veterinary use to treat flea and tick infestations in dogs and cats but has since been approved for human use as an ophthalmic solution (Xdemvy) for the treatment of *Demodex* blepharitis—the first FDA-approved therapy for this condition[2][3][7][8]. The S-enantiomer is the active form *in vivo*[2].

Brand names
XdemvyCredelioCredelio Cat
Other names
lotilaner ophthalmic solution
02

Targets

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

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