Chemistry:Lotilaner

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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).[1][2] It is used as an eye drop.[1]

It was approved for medical use in the United States in July 2023.[1][2][3][4] The US Food and Drug Administration (FDA) considers it to be a first-in-class medication.[5]

Lotilaner is a member of the isoxazoline family of compounds.

Medical uses

Lotilaner is indicated for the treatment of Demodex blepharitis.[1] It had been first used in veterinary medicine against fleas and ticks, and later for Demodex mites.[6]

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.[7][8][9][10] 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).[11] It is taken by mouth.[7][8]

Lotilaner in combination with milbemycin oxime is sold under the brand name Credelio Plus.[12] It is used in dogs to treat concurrent infestations with parasites living outside (ticks and/or fleas) and inside (worms) the animal's body.[12]

Lotilaner (brand Lotimax) is used for the treatment of flea, tick, and mite infestations in dogs, including treatment of demodicosis (caused by Demodex canis).[13]

Mechanism of action

Lotilaner paralyzes and kills parasites by interfering with the way that signals are passed between their nerve cells.[6]

Lotilaner is a gamma-aminobutyric acid (GABA)-gated chloride channel inhibitor selective for arthropods. Inhibition of these GABA chloride channels causes a paralytic action in the target organism leading to its death. Lotilaner is not an inhibitor of mammalian GABA mediated chloride channels when tested at up to 30 µM (18 µg/mL) in vitro (approximately 1100 times the RHOD).[14]

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.[15] The applicant for this veterinary medicinal product is Elanco GmbH.[15] Lotimax was approved for medical use in the European Union in April 2024.[13]

Research

Tarsus Pharmaceuticals has conducted phase II studies of lotilaner as a remedy to prevent tick bites in humans.[16][6]

References

  1. ↑ 1.0 1.1 1.2 1.3 Cite error: Invalid <ref> tag; no text was provided for refs named Xdemvy FDA label
  2. ↑ 2.0 2.1 "Novel Drug Approvals for 2023". 25 July 2023. https://www.fda.gov/drugs/new-drugs-fda-cders-new-molecular-entities-and-new-therapeutic-biological-products/novel-drug-approvals-2023. 
  3. ↑ "Xdemvy: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA). https://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=overview.process&ApplNo=217603. 
  4. ↑ "FDA Approves Xdemvy (lotilaner ophthalmic solution) 0.25% for the treatment of Demodex blepharitis" (Press release). Tarsus Pharmaceuticals. 25 July 2023. Retrieved 5 August 2023 – via GlobeNewswire.
  5. ↑ (PDF) New Drug Therapy Approvals 2023 (Report). January 2024. https://www.fda.gov/media/175253/download. Retrieved 9 January 2024. 
  6. ↑ 6.0 6.1 6.2 "A Pill That Kills Ticks Is a Promising New Weapon Against Lyme Disease". Wired. 15 March 2024. https://www.wired.com/story/pill-kills-ticks-lyme-disease-babesiosis-anaplasmosis/. Retrieved 17 March 2024. 
  7. ↑ 7.0 7.1 Cite error: Invalid <ref> tag; no text was provided for refs named Credelio dog label
  8. ↑ 8.0 8.1 Cite error: Invalid <ref> tag; no text was provided for refs named Credelio cat label
  9. ↑ Cite error: Invalid <ref> tag; no text was provided for refs named Credelio EPAR
  10. ↑ "Safety evaluation of lotilaner in dogs after oral administration as flavoured chewable tablets (Credelio)". Parasites & Vectors 10 (1): 538. November 2017. doi:10.1186/s13071-017-2468-y. PMID 29089043. 
  11. ↑ "Freedom Of Information Summary, Supplemental New Animal Drug Application, NADA 141-494, Credelio, Lotilaner, Chewable Tablets, Dogs". 3 September 2019. https://animaldrugsatfda.fda.gov/adafda/app/search/public/document/downloadFoi/7663. 
  12. ↑ 12.0 12.1 "Credelio Plus EPAR". 19 February 2021. https://www.ema.europa.eu/en/medicines/veterinary/EPAR/credelio-plus.  Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  13. ↑ 13.0 13.1 "Lotimax PI". 29 April 2024. https://ec.europa.eu/health/documents/community-register/html/v311.htm. 
  14. ↑ Prescribing Information for XDEMVY, Irvine, CA: Tarsus Pharmaceuticals, Inc., 2024 
  15. ↑ 15.0 15.1 "Lotimax EPAR". 13 March 2024. https://www.ema.europa.eu/en/medicines/veterinary/EPAR/lotimax.  Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  16. ↑ "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)". 22 February 2024. https://ir.tarsusrx.com/news-releases/news-release-details/tarsus-announces-positive-topline-results-carpo-phase-2a-proof. 

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