Canis ISSN: 2398-2942

Moxidectin

Synonym(s): Advocate®, Advantage® Multi, Proheart 6, Proheart 12, Simparica Trio

Contributor(s): Linda Horspool, Vetstream Ltd

Introduction

Name

  • Moxidectin.

Class of drug

  • 23-(O-methyloxime)-F28249 alpha is a second-generation macrocyclic lactone of the milbemycin family. 

Description

Chemical name

  • (2aE,4E,8E)-(52S,6R,62S,11R,13R,15S,17aR,20R,20aR,20bS)-62-[(1E)-1,3-dimethylbut-1-enyl]-52,62,10,11,14,15,17a,20,20a,20b-decahydro-20,20b-dihydroxy-52,6,8,19-tetramethylspiro[11,15-methano-2H,13H,17H-furo[4,3,2-pq][2,6]benzodioxacyclooctadecin-13,22-[2H]pyran]-42,17(32H,6H)-dione 42-(E)-(O-methyloxime).

Molecular formula

  • C37H53NO8

Molecular weight

  • 639.84

Physical properties

  • Water Solubility (at 25 °C, pH 7): 51 ppb.
  • Octanol-water Partition Coefficient: 58.3.
  • Photolysis half-life: 6.8 hours.
  • Finished product:
    • Clear to yellow spot-on solution (Advantage Multi, Advocate). 
    • Extended-release injectable suspension (Proheart 6, Proheart 12). 
    • Chewable tablet (Simparica Trio). 

Storage requirements

  • Product as packaged for sale: Do not store above 30°C.

Uses

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Indications

  • Endectocide - activity against endo- and ectoparasites. Spectrum below reflects activity due to moxidectin. 

    Parasite indication 

    Advantage Multi
    (US) 

    Advocate  
    (UK, EU) 

    Proheart 6  
    (US) 

    Proheart 12  
    (US) 

    Simparica Trio  
    (UK, EU) 

    Simparica Trio (US) 

    Treatment of Ear mites  
    (Otodectes cynotis

     

    Treatment of Sarcoptic mange,
    Scabies (Sarcoptes scabei var. canis

    Treatment of Demodectic mange (Demodex canis

    Prevention of Heartworm disease (D immitis

    L3, L4 

    L3, L4 

    L3, L4 

    L3, L4 

    L3, L4 

    L3 

    Prevention and treatment Skin worm  
    (Dirofilaria repens

    PV L3  
    TX A 

    Treatment of Hookworm  
    (A caninumU stenocephala

    A, L5,  
    L4  

    A, L5,  
    L4  

    A, L5, L4  

    A, L5, L4  

    A, L5*, L4* 

    Treatment of Roundworm  
    (Toxocara canis

    A, L4 

    A, L4 

    A, L5* 

    A, L5* 

    Treatment of Roundworm  
    (Toxascaris leonina

    TX 

    TX 

    TX  

    TX  

    Tretment of Whipworm  
    (Trichuris vulpis

    TX 

    TX 

    Prevention and Treatment of Lungworm
    (Angiostrongylus vasorum

    PV L5, L4 

    TX 

    PV L5* 

    Treatment of Lungworm
    (C vulpisEucoleus (syn. Capillaria) boehmi

    Prevention of Spirocercosis  
    (Spirocerca lupi

    Treatment of Eye worm  
    (Thelazia callipaeda

KEY:  

  • Dirofilaria immitis (D. immitis), Ancylostoma caninum (A. caninum)Uncinaria stenocephala (U. stenocephala), Crenosoma vulpis (C. vulpis), TX – treatment, PV – prevention, A – adult, L5 – immature adult, L3, L4 – L3 and L4 larvae.  
  • *Pyrantel Pyrantel embonate in Simparica Trio is effective against immature adult (L5) Toxocara canis roundworms and Ancylostoma caninum hookworm L4 larvae and immature adults (L5).  
  • Ectoparasite spectrum (fleas, biting lice) of Advantage Multi and Advocate is due to imidacloprid Imidacloprid
  • Ectoparasite activity (fleas and ticks) of Simparica Trio is due to sarolaner Sarolaner

Administration

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Pharmacokinetics

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Precautions

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Interactions

with other drugs

  • No other antiparasitic macrocyclic lactone should be administered concurrently. 
  • No interactions with routinely used veterinary medicinal products or medical or surgical procedures have been observed. 

Adverse Reactions

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Further Reading

Publications

Refereed papers

  • Recent references from VetMedResource and PubMed.
  • Becskei C, Thys M, Doherty P, Mahabir SP (2020) Efficacy of orally administered combination of moxidectin, sarolaner and pyrantel (Simparica Trio™) for the prevention of experimental Angiostrongylus vasorum infection in dogs. Parasit Vectors 13, 64 PubMed.   
  • Kryda K, Six R H, Walsh K F, Holzmer S J, Chapin S, Mahabir S P, Myers M, Inskeep T, Rugg J, Cundiff B, Pullins A, Ulrich M, McCall J W, McTier T L, Maeder S J (2019) Laboratory and field studies to investigate the efficacy of a novel, orally administered combination product containing moxidectin, sarolaner and pyrantel for the prevention of heartworm disease (Dirofilaria immitis) in dogs. Parasit Vectors 12, 445 PubMed
  • McTier T L, Six R H, Pullins A, Chapin S, Kryda K, Mahabir S P, Woods D J, Maeder S J (2019) Preventive efficacy of oral moxidectin at various doses and dosage regimens against macrocyclic lactone-resistant heartworm (Dirofilaria immitis) strains in dogs. Parasit Vectors 12, 444 PubMed
  • Krautmann M J, Mahabir S, Fielder A, Collard W, Wolthuis T L, Esch K, Morton T, Alleman K, Luo L, McCandless E, Nederveld S, Kryda K, Carroll R, Boucher J F (2019) Safety of an extended-release injectable moxidectin suspension formulation (ProHeart® 12) in dogs. Parasit Vectors 12, 433 PubMed
  • McTier T L, Kryda K, Wachowski M, Mahabir S, Ramsey D, Rugg D, Mazaleski M, Therrien C, Adams E, Wolff T, Bowman D D (2019) ProHeart® 12, a moxidectin extended-release injectable formulation for prevention of heartworm (Dirofilaria immitis) disease in dogs in the USA for 12 months. Parasit Vectors 12, 369 PubMed
  • Fourie J J, Meyer L, Thomas E (2019) Efficacy of topically administered fluralaner or imidacloprid/moxidectin on dogs with generalised demodicosis. Parasit Vectors 12, 59 PubMed
  • Segev G, Rojas A, Lavy E, Yaffe M, Aroch I, Baneth G (2018) Evaluation of a spot-on imidacloprid-moxidectin formulation (Advocate®) for the treatment of naturally occurring esophageal spirocercosis in dogs: a double-blinded, placebo-controlled study. Parasit Vectors 11, 127 PubMed.
  • Bowman D D, Ohmes C M, Hostetler J A, Keil D J, Settje T L, Charles S D (2017) Efficacy of 10% imidacloprid + 2.5% moxidectin topical solution (Advantage Multi® for Dogs) for the prevention of heartworm disease and infection all month long. Parasit Vectors 10(Suppl 2), 478 PubMed
  • Bowman D D, McTier T L, Adams E L, Mahabir S P, Login J A, Bidgood T, Woods D J  (2017) Evaluation of the efficacy of ProHeart® 6 (moxidectin) against a resistant isolate of Dirofilaria immitis (JYD-34) in dogs. Parasit Vectors 10(Suppl 2), 502 PubMed
  • McTier T L, Pullins A, Inskeep G A, Gagnon G, Fan H, Schoell A, Bidgood T, Login J, Meeus P. (2017) Microfilarial reduction following ProHeart® 6 and ProHeart® SR-12 treatment in dogs experimentally inoculated with a resistant isolate of Dirofilaria immitis. Parasit Vectors 10(Suppl 2), 485 PubMed
  • McTier T L, Six R H, Pullins A, Chapin S, McCall J W, Rugg D, Maeder S J, Woods D J (2017) Efficacy of oral moxidectin against susceptible and resistant isolates of Dirofilaria immitis in dogs. Parasit Vectors 10(Suppl 2), 482 PubMed
  • Böhm C, Petry G, Schmidt H, Raue K, Barthel F, Schaper R (2017) Evaluation of the persistent preventive efficacy of 2.5 % moxidectin/10 % imidacloprid spot-on (Advocate®, Advantage® Multi) in dogs experimentally infected with Angiostrongylus vasorum. Parasitol Res 116(Suppl 1), 1-10 PubMed.  
  • Otranto D, Colella V, Crescenzo G, Solari Basano F, Nazzari R, Capelli G, Petry G, Schaper R, Pollmeier M, Mallia E, Dantas-Torres F, Lia R P (2016) Efficacy of moxidectin 2.5% and imidacloprid 10% in the treatment of ocular thelaziosis by Thelazia callipaeda in naturally infected dogs. Vet Parasitol 227, 118-21 PubMed.
  • Frangipane di Regalbono A, Di Cesare A, Traversa D, Simonato G, Poser H, Danesi P, Furnari C, Russi I, Raele D A, Crisi P, Pampurini F, Pietrobelli M (2016) Microfilaricidal efficacy of a single administration of Advocate(®) (Bayer Animal Health) in dogs naturally infected with Dirofilaria immitis or Dirofilaria repens. Vet Parasitol 226, 30-34 PubMed.
  • Blagburn B L, Arther R G, Dillon A R, Butler J M, Bowles J V, von Simson C, Zolynas R. (2016) Efficacy of four commercially available heartworm preventive products against the JYD-34 laboratory strain of Dirofilaria immitis. Parasit Vectors 9, 191 PubMed
  • Petry G, Genchi M, Schmidt H, Schaper R, Lawrenz B, Genchi C (2015) Evaluation of the adulticidal efficacy of imidacloprid 10 %/moxidectin 2.5 % (w/v) spot-on (Advocate®, Advantage® Multi) against Dirofilaria repens in experimentally infected dogs. Parasitol Res 114 Suppl 1, S131-44 PubMed.
  • Bourguinat C, Lee A C, Lizundia R, Blagburn B L, Liotta J L, Kraus M S, Keller K, Epe C, Letourneau L, Kleinman CL, Paterson T, Gomez E C, Montoya-Alonso J A, Smith H, Bhan A, Peregrine A S, Carmichael J, Drake J, Schenker R, Kaminsky R, Bowman D D, Geary T G, Prichard R K (2015) Macrocyclic lactone resistance in Dirofilaria immitis: Failure of heartworm preventives and investigation of genetic markers for resistance. Vet Parasitol 210, 167-178 PubMed.
  • Fourie J J, Liebenberg J E, Horak I G, Taenzler J, Heckeroth A R, Frénais R (2015) Efficacy of orally administered fluralaner (Bravecto™) or topically applied imidacloprid/moxidectin (Advocate®) against generalized demodicosis in dogs. Parasit Vectors 8, 187 PubMed
  • Arther R G, Davis W L, Jacobsen J A, Lewis V A, Settje T L (2015) Clinical evaluation of the safety and efficacy of 10% imidacloprid + 2.5% moxidectin topical solution for the treatment of ear mite (Otodectes cynotis) infestations in dogs. Vet Parasitol 210(1-2), 64-68 PubMed
  • Traversa D, Mazzi A, Di Cesare A, Famigli Bergamini P, Fracassi F, Fanini G, Aste G, Pampurini F, Boari A (2013) Potential efficacy of monthly administrations of spot-on moxidectin 2.5 %/imidacloprid 10 % in the simultaneous prevention of major canine filarioses. Parasitol Res 112, 3753-3756 PubMed.
  • Austin C M, Kok D J, Crafford D, Schaper R (2013) The efficacy of a topically applied imidacloprid 10 % / moxidectin 2.5 % formulation (Advocate®, Advantage® Multi, Bayer) against Immature and Adult Spirocerca lupi worms in experimentally infected dogs. Parasitol Res 112 Suppl 1, 91-108 PubMed.
  • Janko C, Geyer J (2013) Moxidectin has a lower neurotoxic potential but comparable brain penetration in P-glycoprotein-deficient CF-1 mice compared to ivermectin. J Vet Pharmacol Ther 36, 275-284 PubMed.
  • Taweethavonsawat P, Chungpivat S, Watanapongchati S, Traub R J, Schaper R (2012) Efficacy of a spot on combination containing imidacloprid 10% and moxidectin 1% (Advocate(®)/Advantage(®) Multi, Bayer Animal Health) against Ancylostoma ceylanicum in cats. Vet Parasitol 190, 289-293 PubMed.
  • Fourie J J, Delport P C, Fourie L J, Heine J, Horak I G, Krieger K J (2009) Comparative efficacy and safety of two treatment regimens with a topically applied combination of imidacloprid and moxidectin (Advocate) against generalised demodicosis in dogs. Parasitol Res 105 Suppl 1, S115-124 PubMed.
  • Paterson T E, Halliwell R E, Fields P J, Louw M L, Louw J P, Ball G S, Pinckney R D, McKibben J S (2009) Treatment of canine-generalized demodicosis: a blind, randomized clinical trial comparing the efficacy of Advocate(Bayer Animal Health) with ivermectin. Vet Dermatol 20, 447-455 PubMed.
  • Heine J, Krieger K, Dumont P, Hellmann K (2005) Evaluation of the efficacy and safety of imidacloprid 10% plus moxidectin 2.5% spot-on in the treatment of generalized demodicosis in dogs: results of a European field study. Parasitol Res 97 Suppl 1, S89-96 PubMed.
  • Arther R G, Bowman D D, Slone R L, Travis L E (2005) Imidacloprid plus moxidectin topical solution for the prevention of heartworm disease (Dirofiloria immitis) in dogs. Parasitol Res 97Suppl 1,S76-80 PubMed.
  • Bianciardi P, Otranto D (2005) Treatment of dog thelaziosis caused by Thelazia callipaeda (Spirurida, Thelaziidae) using a topical formulation of imidacloprid 10% and moxidectin 2.5%. Vet Parasitol 129, 89-93 PubMed.
  • Krieger K, Heine J, Dumont P, Hellmann K (2005) Efficacy and safety of imidacloprid 10% plus moxidectin 2.5% spot-on in the treatment of sarcoptic mange and otoacariosis in dogs: results af a European field study. Parasitol Res 97Suppl 1, S81-88 PubMed.
  • Paul A J, Hutchens D E, Firkins L D, Borgstrom M (2004) Dermal safety study with imidacloprid/moxidectin topical solution in the ivermectin-sensitive collie. Vet Parasitol 121, 285-291 PubMed.
  • Hellmann K, Knoppe T, Radeloff I, Heine J (2003) The anthelmintic efficacy and the safety of a combination of imidacloprid and moxidectin spot-on in cats and dogs under field conditions in Europe. Parasitol Res 90 Suppl 3, S142-143 PubMed.
  • von Samson-Himmelstjerna G, Epe C, Schimmel A, Heine J (2003) Larvicidal and persistent efficacy of an imidacloprid and moxidectin topical formulation against endoparasites in cats and dogs. Parasitol Res 90 Suppl 3, S114-115 PubMed.

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