Chemistry:Fluralaner

From HandWiki

Fluralaner (INN),[1] sold under the brand name Bravecto among others, is a systemic insecticide and acaricide that is administered orally[2] or topically.[3]

Mode of action

Fluralaner inhibits γ-aminobutyric acid (GABA)-gated chloride channels (GABAA receptors) and L-glutamate-gated chloride channels (GluCls).[4] Potency of fluralaner is comparable to fipronil (a related GABA-antagonist insecticide and acaricide).[5]

Society and culture

The US Food and Drug Administration (FDA) approved it for flea treatment in dogs in May 2014,[6] and approved the combination fluralaner/moxidectin (Bravecto Plus) as a topical treatment for cats in November 2019.[7][8][9][10] The EU approved fluralaner in March 2014.[11][12][13] Australia approved it for the treatment and prevention of ticks and fleas on dogs in January 2015.[14] For treating mites in chickens, a solution for use in drinking water is available under the brand name Exzolt[15] and was approved for use in the EU in 2017.[16]

Bravecto 1-Month was approved by the FDA in November 2024 for the addition of the indication for the treatment and control of Haemaphysalis longicornis (Asian longhorned tick) infestations for one month in dogs and puppies eight weeks of age and older, and weighing 4.4 pounds (2.0 kg) or greater.[17][18]

In June 2025, the Committee for Veterinary Medicinal Products of the European Medicines Agency adopted a positive opinion, recommending the granting of a marketing authorization for the veterinary medicinal product Bravecto Combiuno chewable tablets intended for dogs.[19] The applicant for this veterinary medicinal product is Intervet International B.V.[19] Bravecto Combiuno is an antiparasitic medicinal product containing fluralaner and milbemycin oxime as active substances. Both substances exert parasiticidal activity by interacting with ligand-gated ion channels in the nervous system of various parasites such as insects, acari and helminths.[19]

Research

Fluralaner is being investigated to determine its ability to reduce the incidence of mosquito-borne diseases,[20] as well as bed bugs.[21][22]

A recent systematic review has been published on fluralaner efficacy and safety [23]

References

  1. ↑ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 69". WHO Drug Information 27 (1): 59. 2013. http://apps.who.int/medicinedocs/documents/s20154en/s20154en.pdf. Retrieved 14 November 2016. 
  2. ↑ "Safety of fluralaner chewable tablets (Bravecto), a novel systemic antiparasitic drug, in dogs after oral administration". Parasites & Vectors 7 (1): 87. March 2014. doi:10.1186/1756-3305-7-87. PMID 24606886. 
  3. ↑ "A single topical fluralaner application to cats and to dogs controls fleas for 12 weeks in a simulated home environment". Parasites & Vectors 11 (1). July 2018. doi:10.1186/s13071-018-2927-0. PMID 29970135. 
  4. ↑ "The novel isoxazoline ectoparasiticide fluralaner: selective inhibition of arthropod γ-aminobutyric acid- and L-glutamate-gated chloride channels and insecticidal/acaricidal activity". Insect Biochemistry and Molecular Biology 45: 111–124. February 2014. doi:10.1016/j.ibmb.2013.11.009. PMID 24365472. Bibcode: 2014IBMB...45..111G. 
  5. ↑ "Differential mechanisms of action of the novel γ-aminobutyric acid receptor antagonist ectoparasiticides fluralaner (A1443) and fipronil". Pest Management Science 71 (1): 91–95. January 2015. doi:10.1002/ps.3768. PMID 24591229. Bibcode: 2015PMSci..71...91A. 
  6. ↑ "New Flea/Tick Medication by Merck Just Approved: Bravecto". 21 May 2014. http://drjustinelee.com/new-fleatick-medication-bravecto-just-approved/. 
  7. ↑ "Bravecto Plus (fluralaner and moxidectin topical solution) for Cats Receives Approval from US Food and Drug Administration". 15 November 2019. https://www.merck-animal-health.com/blog/2019/11/15/bravecto-plus-fluralaner-and-moxidectin-topical-solution-for-cats-receives-approval-from-us-food-and-drug-administration/. 
  8. ↑ Center for Veterinary Medicine (31 July 2020). "Fact Sheet for Pet Owners and Veterinarians about Potential Adverse Events Associated with Isoxazoline Flea and Tick Products". https://www.fda.gov/animal-veterinary/animal-health-literacy/fact-sheet-pet-owners-and-veterinarians-about-potential-adverse-events-associated-isoxazoline-flea. 
  9. ↑ "Bravecto Plus EPAR". 7 June 2018. https://www.ema.europa.eu/en/medicines/veterinary/EPAR/bravecto-plus. 
  10. ↑ "Bravecto Plus PI". 16 May 2018. https://ec.europa.eu/health/documents/community-register/html/v224.htm. 
  11. ↑ Cite error: Invalid <ref> tag; no text was provided for refs named Bravecto EPAR
  12. ↑ Cite error: Invalid <ref> tag; no text was provided for refs named Bravecto PI
  13. ↑ "MSD Animal Health receives EU approval for Bravecto". 19 February 2014. https://www.zenopa.com/news/801695271/msd-animal-health-receives-eu-approval-for-bravecto. 
  14. ↑ "Agricultural and Veterinary Chemicals". Australian Pesticides and Veterinary Medicines Authority. 10 February 2015. https://apvma.gov.au/sites/default/files/gazette_10022015.pdf. 
  15. ↑ "Backyard poultry red mite treatment launches". 24 June 2020. https://www.vettimes.co.uk/news/backyard-poultry-red-mite-treatment-launches/. 
  16. ↑ "The acaricidal speed of kill of orally administered fluralaner against poultry red mites (Dermanyssus gallinae) on laying hens and its impact on mite reproduction". Parasites & Vectors 10 (1). December 2017. doi:10.1186/s13071-017-2534-5. PMID 29197422. 
  17. ↑ "Recent Animal Drug Approvals". 2 December 2024. https://www.fda.gov/animal-veterinary/approved-animal-drug-products-green-book/recent-animal-drug-approvals.  Public Domain This article incorporates text from this source, which is in the public domain.
  18. ↑ fda.gov
  19. ↑ 19.0 19.1 19.2 "Bravecto CombiUNO EPAR". 13 June 2025. https://www.ema.europa.eu/en/medicines/veterinary/EPAR/bravecto-combiuno.  Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  20. ↑ "Repurposing isoxazoline veterinary drugs for control of vector-borne human diseases". Proceedings of the National Academy of Sciences of the United States of America 115 (29): E6920–E6926. July 2018. doi:10.1073/pnas.1801338115. PMID 29967151. Bibcode: 2018PNAS..115E6920M. 
  21. ↑ "Two veterinary drugs may help eliminate bedbugs". United Press International, Inc.. 1 December 2022. https://www.upi.com/Health_News/2022/12/01/veterinary-medicine-bedbugs/6091669903318/. 
  22. ↑ "A Preliminary Report Showing Spinosad and Fluralaner Are Able to Incapacitate Cimex lectularius L., the Common Bed Bug". Cureus 12 (4). 2020. doi:10.7759/cureus.7529. PMID 32377477. 
  23. ↑ "A systematic review of fluralaner as a treatment for ectoparasitic infections in mammalian species". PeerJ 13. 2025. doi:10.7717/peerj.18882. PMID 40093406. 



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