Lotilaner

Lotilaner, sold under the brand name Xdemvy, is an ectoparasiticide (anti-parasitic) medication used for the treatment of blepharitis (inflammation of the eyelid) caused by infestation by Demodex (tiny mites).^[1][7] It is used as an eye drop.^[1]

Lotilaner

Clinical data
Trade names	Credelio, Xdemvy, others
Other names	TP-03
AHFS/Drugs.com	Monograph
License data	US DailyMed: Lotilaner
Routes of administration	By mouth, eye drops
Drug class	Antiparasitic
ATC code	S01AX25 (WHO) QP53BE04 (WHO)
Legal status
Legal status	US: ℞-only[1][2][3] EU: Rx-only[4][5][6]
Identifiers
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
CAS Number	1369852-71-0
PubChem CID	76959255
DrugBank	DB17992
ChemSpider	32699771
UNII	HEH4938D7K
KEGG	D11212
ChEBI	CHEBI:229657
ChEMBL	ChEMBL3707310
CompTox Dashboard (EPA)	DTXSID701027551
Chemical and physical data
Formula	C20H14Cl3F6N3O3S
Molar mass	596.75 g·mol−1
3D model (JSmol)	Interactive image
SMILES Cc1cc(C2=NO[C@@](c3cc(Cl)c(Cl)c(Cl)c3)(C(F)(F)F)C2)sc1C(=O)NCC(=O)NCC(F)(F)F
InChI InChI=1S/C20H14Cl3F6N3O3S/c1-8-2-13(36-16(8)17(34)30-6-14(33)31-7-19(24,25)26)12-5-18(35-32-12,20(27,28)29)9-3-10(21)15(23)11(22)4-9/h2-4H,5-7H2,1H3,(H,30,34)(H,31,33)/t18-/m0/s1 Key:HDKWFBCPLKNOCK-SFHVURJKSA-N

It was approved for medical use in the United States in July 2023.^[1][7][8][9] The US Food and Drug Administration (FDA) considers it to be a first-in-class medication.^[10]

Medical uses

Lotilaner is indicated for the treatment of Demodex blepharitis.^[1]

History

Lotilaner paralyzes and kills parasites by interfering with the way that signals are passed between their nerve cells.^[11] It had been first used in veterinary medicine against fleas and ticks, and later for Demodex mites.^[11]

Society and culture

Legal status

In March 2024, the Committee for Veterinary Medicinal Products (CVMP) of the European Medicines Agency adopted a positive opinion, recommending the granting of a marketing authorization for the veterinary medicinal product Lotimax, Chewable tablet, intended for use in dogs.^[5] The applicant for this veterinary medicinal product is Elanco GmbH.^[5] Lotimax was approved for medical use in the European Union in April 2024.^[12]

Veterinary uses

Lotilaner, sold under the brand name Credelio among others, is a veterinary medication used to control fleas and ticks in dogs and cats.^{[2][3][4][13]} It is indicated for the treatment and prevention of flea infestations (Ctenocephalides felis) and for the treatment and control of tick infestations including lone star tick (Amblyomma americanum), American dog tick (Dermacentor variabilis), black-legged tick (Ixodes scapularis), and brown dog tick (Rhipicephalus sanguineus).^[14] It is taken by mouth.^[2][3]

Lotilaner in combination with milbemycin oxime is sold under the brand name Credelio Plus.^[15] It is used in dogs to treat concurrent infestations with parasites living outside (ticks and/or fleas) and inside (worms) the animal's body.^[15]

Lotilaner (brand Lotimax) is used for the treatment of flea, tick, and mite infestations in dogs, including treatment of demodicosis (caused by Demodex canis).^[12]

Research

Tarsus Pharmaceuticals has conducted phase II studies of lotilaner as a remedy to prevent tick bites in humans.^[16][11]