Lotilaner

Summary

Lotilaner (CHEMBL3707310) is an approved small-molecule GABA-gated chloride channel antagonist (ATC S01AX25); indicated across 3 conditions including parasitic eye infection and blepharitis.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: S01AX25
• Indications: 3 conditions
• Clinical trials: 3
• Chemistry: 596.8 Da · C20H14Cl3F6N3O3S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL3707310
Name	Lotilaner
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	76959255
ChEBI	CHEBI:229657
ATC	S01AX25
Molecular formula	C20H14Cl3F6N3O3S
Molecular weight	596.8
InChIKey	HDKWFBCPLKNOCK-SFHVURJKSA-N

SMILES: CC1=C(SC(=C1)C2=NO[C@@](C2)(C3=CC(=C(C(=C3)Cl)Cl)Cl)C(F)(F)F)C(=O)NCC(=O)NCC(F)(F)F

IUPAC name: 3-methyl-N-[2-oxo-2-(2,2,2-trifluoroethylamino)ethyl]-5-[(5S)-5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4H-1,2-oxazol-3-yl]thiophene-2-carboxamide

ChEBI definition: A member of the class of isoxazoles that is 4,5-dihydro-1,2-oxazole substituted by 4-methyl-5-({2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl}carbamoyl)thiophen-2-yl, trifluoromethyl, and 3,4,5-trichlorophenyl groups at positions 3, 5 and 5, respectively (the 5S-stereoisomer). It is a γ-aminobutyric acid (GABA)-gated chloride channel inhibitor selective for mites, approved for the treatment of Demodex blepharitis.

Pharmacological roles (ChEBI): GABA-gated chloride channel antagonist, ophthalmology drug, ectoparasiticide.

Also known as: Adtab (previously lotilaner elanco), Credelio, Lotilaner, Lotilaner (ema epar: veterinary), Lotimax, Xdemvy, LOTILANER

Patent coverage: 679 distinct patent families (1,619 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

No target linkage available.

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

3 indications (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
parasitic eye infection	4	MONDO:0020947	EFO:1001888
blepharitis	3	MONDO:0004785	EFO:0009536
rosacea	2	MONDO:0006604	EFO:1000760

Clinical trials

Total trials: 3.

Phase distribution

Phase	Trials
PHASE4	1
PHASE3	1
PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT07561450	PHASE4	NOT_YET_RECRUITING	Demodex Blepharitis in Scleral Lens Wearers
NCT05629390	PHASE3	COMPLETED	Trial to Evaluate the Efficacy and Safety of TP-03, LIBRA Study
NCT07443202	PHASE2	ENROLLING_BY_INVITATION	Study of Lotilaner Ophthalmic Gel in Patients With Ocular Rosacea (KORE)

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).