Efficacy of a Single Oral Dose of Oxfendazole against Fasciola hepatica in Naturally Infected Sheep

Gómez-Puerta, Luis A.; Gavidia, C César; López-Urbina, María T.; Garcı́a, Héctor H.; González, Armando E.

doi:10.4269/ajtmh.2012.11-0476

Cited by 17 publications

(7 citation statements)

References 24 publications

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“…At this stage, their activity was evaluated alongside commercial drugs, three BZs (TCBZ, OXF, and ABZSO) and CLR, at a concentration of 5 µM, to compare their activities. While OXF has demonstrated in vitro and in vivo properties, it is not currently a recommended flukicide, in contrast to ABZSO, TCBZ, and CLR [ 55 , 56 ]. When performing the EHT on a susceptible F. hepatica isolate at 5 µM, all hit compounds showed activities exceeding 71%, with BZD56 being the most potent one, displaying an activity slightly below 90%.…”

Section: Discussionmentioning

confidence: 99%

New benzimidazole derivative compounds with in vitro fasciolicidal properties

Valderas-García,

Castilla-Gómez de Agüero,

González del Palacio

et al. 2024

Parasites Vectors

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Background Control of the zoonotic food-borne parasite Fasciola hepatica remains a major challenge in humans and livestock. It is estimated that annual economic losses due to fasciolosis can reach US$3.2 billion in agriculture and livestock. Moreover, the wide distribution of drug-resistant parasite populations and the absence of a vaccine threaten sustainable control, reinforcing the need for novel flukicides. Methods The present work analyses the flukicidal activity of a total of 70 benzimidazole derivatives on different stages of F. hepatica. With the aim to select the most potent ones, and screenings were first performed on eggs at decreasing concentrations ranging from 50 to 5 µM and then on adult worms at 10 µM. Only the most effective compounds were also evaluated using a resistant isolate of the parasite. Results After the first screenings at 50 and 10 µM, four hit compounds (BZD31, BZD46, BZD56, and BZD59) were selected and progressed to the next assays. At 5 µM, all hit compounds showed ovicidal activities higher than 71% on the susceptible isolate, but only BZD31 remained considerably active (53%) when they were tested on an albendazol-resistant isolate, even with values superior to the reference drug, albendazole sulfoxide. On the other hand, BZD59 displayed a high motility inhibition when tested on adult worms from an albendazole-resistant isolate after 72 h of incubation. Conclusions BZD31 and BZD59 compounds could be promising candidates for the development of fasciolicidal compounds or as starting point for the new synthesis of structure-related compounds. Graphical Abstract

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Section: Discussionmentioning

confidence: 99%

New benzimidazole derivative compounds with in vitro fasciolicidal properties

Valderas-García,

Castilla-Gómez de Agüero,

González del Palacio

et al. 2024

Parasites Vectors

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“…Of the several strategies for the control of bovine fasciolosis described, in practice usually strategic anthelmintic control is used with flukicide treatment time and interval depending on the climatic zone (Armour, 1975;Boray, 1971Boray, , 1972Harris and Charleston, 1971;Schneider et al, 1975;Torgerson and Claxton, 1999;Whitehead, 1976). A variety of fasciolicides is available for the treatment of bovine fasiolosis: triclabendazole, albendazole, oxyclozanide, clorsulon, nitroxynil, rafoxanide or oxfendazole (Fairweather, 2011;Gomez-Puerta et al, 2012;Martínez-Valladares et al, 2010). Of all these agents, triclabendazole is the most effective against immature stages of the parasite, which makes it the drug of choice for the treatment of acute fasciolosis, which is more commonly seen in sheep than in cattle.…”

Section: Introductionmentioning

confidence: 99%

Bovine fasciolosis: Control strategies based on the location of Galba truncatula habitats on farms

Knubben‐Schweizer¹,

Torgerson

2015

Veterinary Parasitology

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“…(26) In a masked, controlled study, our group has also demonstrated that a single oral dose of 30 mg/kg of OXF was fully effective against Fasciola hepatica in naturally infected sheep (n=20) compared to no cure at all in untreated animals (n=20); no side effects were discernible in the OXF treated animals. (27)…”

Section: Introductionmentioning

confidence: 99%

Oxfendazole: a promising agent for the treatment and control of helminth infections in humans

González

Codd²,

Horton

et al. 2018

Expert Review of Anti-infective Therapy

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Introduction. Oxfendazole (methyl [5-(phenylsulphinyl)-1H benzimidazole- 2-yl] carbamate) has a particularly long metabolic half-life in ruminants, and its metabolite fenbendazole also has anthelminthic action. A very limited number of drugs are available for the treatment of some zoonotic helminth infections, such as neurocysticercosis and echinococcosis. More recent work has expanded oxfendazole’s non-clinical safety profile and demonstrated its safety and bioavailability in healthy human volunteers, thus advancing the possibility of a new and greatly needed option for antiparasitic treatment of geohelminths and tissue parasites. Areas covered. The present article reviews evidence supporting the safety and efficacy of oxfendazole against both gut and tissue dwelling helminths in animals, as well as more recent safety and pharmacokinetic data supporting its potential for use in human parasitoses. Expert commentary. The pharmacokinetics, safety and wide spectrum of efficacy of oxfendazole are consistently demonstrated in intestinal helminth infections of animals as well as in tissue dwelling larval cestode and trematode infections in diverse animal species. Now supported by first-in-human safety and pharmacokinetic data, oxfendazole becomes a promising alternative to the limited portfolio of antiparasitic drugs available to treat helminthic diseases of humans.

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Efficacy of a Single Oral Dose of Oxfendazole against Fasciola hepatica in Naturally Infected Sheep

Cited by 17 publications

References 24 publications

New benzimidazole derivative compounds with in vitro fasciolicidal properties

New benzimidazole derivative compounds with in vitro fasciolicidal properties

Bovine fasciolosis: Control strategies based on the location of Galba truncatula habitats on farms

Oxfendazole: a promising agent for the treatment and control of helminth infections in humans

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