Lotilaner is an antiparasitic agent used to treat Demodex blepharitis. Lotilaner is an ectoparasiticide that is a member of the isoxazoline family of compounds.
- Mechanism
- Curator reviewed · 2 references
Lotilaner is a non-competitive antagonist of the gamma-aminobutyric acid (GABA)-gated chloride channel (GABACl) selective for mites. Inhibition of GABACl causes a paralytic action in the target organism, leading to death. Lotilaner is not an inhibitor of mammalian GABA-mediated chloride channels when tested at up to 30 µM (18 µg/mL) in vitro, which is approximately 1100 times the recommended human ophthalmic dose.
The target site in GABACl is hypothesized to be localized in a pore between the T9’ to S15’ region, an interstitial subunit region. A study suggested that lotilaner may migrate within the pore of the GABACl to its final location to stabilize the channel in a closed state; however, this hypothesis requires further investigation.
- Primary indication
- Lotilaner is indicated for the treatment of Demodex blepharitis.Curator reviewed · 1 structured indication
- Formula / weight
- C20H14Cl3F6N3O3S · 596.75 g/mol (avg)
- First approval
- United States, 2023
- Also known as
- 2-thiophenecarboxamide, 5-((5s)-4,5-dihydro-5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-3-isoxazolyl)-3-methyl-n-(2-oxo-2-((2,2,2-trifluoroethyl)amino)ethyl)- · 3-methyi-n-(2-oxo-2-((2,2,2-trifluoroethyl)amino)ethyl)-5-((55)-5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazol-3-yl)thiophene-2-carboxamide · Credelio · Lotilaner (ema epar: veterinary)
- Code names
- TP-03 · TP-05
- Brand names
Resolves to
HDKWFBCPLKNOCK-SFHVURJKSA-NSMILESCC1=C(SC(=C1)C1=NO[C@@](C1)(C1=CC(Cl)=C(Cl)C(Cl)=C1)C(F)(F)F)C(=O)NCC(=O)NCC(F)(F)FWhat you can answer from here — as of September 23, 2026
Which drugs share a target with Lotilaner, and which of those have an active Phase 3 trial?
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