Lotilaner
{{Short description|Chemical compound}}
{{Use dmy dates|date=August 2024}}
{{cs1 config |name-list-style=vanc |display-authors=6}}
{{Infobox drug
| image = Lotilaner.svg
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| tradename = Credelio, Xdemvy, others
| Drugs.com = {{drugs.com|monograph|lotilaner-eent}}
| MedlinePlus =
| DailyMedID = Lotilaner
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| routes_of_administration = By mouth, eye drops
| class = Antiparasitic
| ATC_prefix = S01
| ATC_suffix = AX25
| ATC_supplemental = {{ATCvet|P53|BE04}}
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| legal_US = Rx-only
| legal_US_comment = {{cite web | title=Xdemvy- lotilaner ophthalmic solution solution/ drops | website=DailyMed | date=26 July 2023 | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=ccd9e37c-654e-4e84-8c85-6523457df979 | access-date=23 August 2023}}{{cite web | title=Credelio- lotilaner tablet, chewable | website=DailyMed | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=427f2ebc-ce24-452b-bbb3-43d4ef8b63b0 | access-date=4 August 2021 | archive-date=5 August 2021 | archive-url=https://web.archive.org/web/20210805060048/https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=427f2ebc-ce24-452b-bbb3-43d4ef8b63b0 | url-status=live }}{{cite web | title=Credelio- lotilaner tablet, chewable | website=DailyMed | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=365b701f-e9a8-458f-90ff-33ca1fb947ca | access-date=4 August 2021 | archive-date=5 August 2021 | archive-url=https://web.archive.org/web/20210805054924/https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=365b701f-e9a8-458f-90ff-33ca1fb947ca | url-status=live }}
| legal_EU = Rx-only
| legal_EU_comment = {{cite web | title=Credelio EPAR | website=European Medicines Agency (EMA) | date=17 September 2018 | url=https://www.ema.europa.eu/en/medicines/veterinary/EPAR/credelio | access-date=4 August 2021 | archive-date=27 January 2022 | archive-url=https://web.archive.org/web/20220127082517/https://www.ema.europa.eu/en/medicines/veterinary/EPAR/credelio | url-status=live }}{{cite web | title=Lotimax Product information | website=Union Register of veterinary medicinal products | date=29 April 2024 | url=https://ec.europa.eu/health/documents/community-register/html/v311.htm | access-date=29 August 2024}}
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| CAS_number = 1369852-71-0
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| PubChem = 76959255
| IUPHAR_ligand =
| DrugBank = DB17992
| ChemSpiderID = 32699771
| UNII = HEH4938D7K
| KEGG = D11212
| ChEBI = 229657
| ChEMBL = 3707310
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| synonyms = TP-03
| 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
| C=20 | H=14 | Cl=3 | F=6 | N=3 | O=3 | S=1
| 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
| StdInChI = 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
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| StdInChIKey = HDKWFBCPLKNOCK-SFHVURJKSA-N
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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).{{cite web | title=Novel Drug Approvals for 2023 | website=U.S. Food and Drug Administration (FDA) | date=25 July 2023 | url=https://www.fda.gov/drugs/new-drugs-fda-cders-new-molecular-entities-and-new-therapeutic-biological-products/novel-drug-approvals-2023 | access-date=5 August 2023 | archive-date=21 January 2023 | archive-url=https://web.archive.org/web/20230121035617/https://www.fda.gov/drugs/new-drugs-fda-cders-new-molecular-entities-and-new-therapeutic-biological-products/novel-drug-approvals-2023 | url-status=dead }} It is used as an eye drop.
It was approved for medical use in the United States in July 2023.{{cite web | title=Xdemvy: FDA-Approved Drugs | publisher=U.S. Food and Drug Administration (FDA) | url=https://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=overview.process&ApplNo=217603 | access-date=5 August 2023 | archive-date=27 July 2023 | archive-url=https://web.archive.org/web/20230727150956/https://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=overview.process&ApplNo=217603 | url-status=live }}{{cite press release | title=FDA Approves Xdemvy (lotilaner ophthalmic solution) 0.25% for the treatment of Demodex blepharitis | publisher=Tarsus Pharmaceuticals | via=GlobeNewswire | date=25 July 2023 | url=https://www.globenewswire.com/en/news-release/2023/07/25/2710273/0/en/FDA-Approves-XDEMVY-lotilaner-ophthalmic-solution-0-25-for-the-treatment-of-Demodex-blepharitis.html | access-date=5 August 2023}} The US Food and Drug Administration (FDA) considers it to be a first-in-class medication.{{cite report | title=New Drug Therapy Approvals 2023 | website=U.S. Food and Drug Administration (FDA) | date=January 2024 | url=https://www.fda.gov/media/175253/download | format=PDF | access-date=9 January 2024 | archive-url=https://web.archive.org/web/20240110032419/https://www.fda.gov/media/175253/download | archive-date=10 January 2024 | url-status=dead }}
Medical uses
History
Lotilaner paralyzes and kills parasites by interfering with the way that signals are passed between their nerve cells. It had been first used in veterinary medicine against fleas and ticks, and later for Demodex mites.
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. The applicant for this veterinary medicinal product is Elanco GmbH.{{cite web | title=Lotimax EPAR | website=European Medicines Agency | date=13 March 2024 | url=https://www.ema.europa.eu/en/medicines/veterinary/EPAR/lotimax | access-date=20 March 2024}} Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged. Lotimax was approved for medical use in the European Union in April 2024.{{cite web | title=Lotimax PI | website=Union Register of medicinal products | date=29 April 2024 | url=https://ec.europa.eu/health/documents/community-register/html/v311.htm | access-date=17 June 2024}}
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.{{cite journal | vauthors = Kuntz EA, Kammanadiminti S | title = Safety evaluation of lotilaner in dogs after oral administration as flavoured chewable tablets (Credelio) | journal = Parasites & Vectors | volume = 10 | issue = 1 | pages = 538 | date = November 2017 | pmid = 29089043 | pmc = 5664904 | doi = 10.1186/s13071-017-2468-y | doi-access = free }} 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).{{Cite web | url = https://animaldrugsatfda.fda.gov/adafda/app/search/public/document/downloadFoi/7663 | title = Freedom Of Information Summary, Supplemental New Animal Drug Application, NADA 141-494, Credelio, Lotilaner, Chewable Tablets, Dogs | date = 3 September 2019 | access-date = 1 December 2019 | archive-date = 18 May 2022 | archive-url = https://web.archive.org/web/20220518060831/https://animaldrugsatfda.fda.gov/adafda/app/search/public/document/downloadFoi/7663 | url-status = live }} It is taken by mouth.
Lotilaner in combination with milbemycin oxime is sold under the brand name Credelio Plus.{{cite web | title=Credelio Plus EPAR | website=European Medicines Agency | date=19 February 2021 | url=https://www.ema.europa.eu/en/medicines/veterinary/EPAR/credelio-plus | access-date=4 August 2021 | archive-date=7 December 2022 | archive-url=https://web.archive.org/web/20221207022222/https://www.ema.europa.eu/en/medicines/veterinary/EPAR/credelio-plus | url-status=live }} Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged. It is used in dogs to treat concurrent infestations with parasites living outside (ticks and/or fleas) and inside (worms) the animal's body.
Lotilaner (brand Lotimax) is used for the treatment of flea, tick, and mite infestations in dogs, including treatment of demodicosis (caused by Demodex canis).
Research
Tarsus Pharmaceuticals has conducted phase II studies of lotilaner as a remedy to prevent tick bites in humans.{{cite web | title=Tarsus Announces Positive Topline Results from Carpo, a Phase 2a Proof-of-Concept "Tick-Kill" Trial Evaluating TP-05 (lotilaner) for the Prevention of Lyme Disease (press release) | website=Tarsus Pharmaceuticals | date=22 February 2024 | url=https://ir.tarsusrx.com/news-releases/news-release-details/tarsus-announces-positive-topline-results-carpo-phase-2a-proof | access-date=17 March 2024 | archive-date=17 March 2024 | archive-url=https://web.archive.org/web/20240317143253/https://ir.tarsusrx.com/news-releases/news-release-details/tarsus-announces-positive-topline-results-carpo-phase-2a-proof | url-status=dead }}{{cite magazine | title=A Pill That Kills Ticks Is a Promising New Weapon Against Lyme Disease | magazine=Wired | date=15 March 2024 | url=https://www.wired.com/story/pill-kills-ticks-lyme-disease-babesiosis-anaplasmosis/ | access-date=17 March 2024 }}
References
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{{Ophthalmological anti-infectives}}
{{Insecticides}}
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