Huateng Pharma Develops Systemic Antiparasitic Agent Fluralaner

By: Hunan Huateng Pharmaceutical Co. Ltd.
CHANGSHA, China - Jan. 28, 2023 - PRLog -- Fluralaner is a systemic insecticide and acaricide that can be administered orally or topically. Bravecto is the trade name. The U.S. Food and Drug Administration (FDA) approved it for flea treatment in dogs under the trade name Bravecto in May 2014 and for topical treatment in cats in November 2019.

Fluralaner is a novel isooxazoline broad-spectrum insecticide that acts on γ-aminobutyric acid (GABA) receptors and has good activity against ticks, fleas, hemiptera, diptera and lepidoptera insects.

Oral administration of fluralaner is easy to absorb, and the maximum blood concentration can be reached within 1 day, and food can promote its absorption. Fluralaner is hardly metabolized in dogs, and about 90% is excreted unchanged in feces.

Fluralaner not only has no cross-resistance with existing GABA receptor insecticides, but also is safe to non-target biotargets such as mammals, zebrafish and poultry, showing a broad application prospect. At present, fluralaner has been widely used as a new anti-parasitic veterinary drug, but its development and popularization as a pesticide is still in the embryonic stage.

Fluralaner has been widely used as a new type of anti-parasitic veterinary drug, but its development and promotion as a pesticide is still in its infancy.

In order to determine the virulence of fluralaner against Nocturea twill and its combined action with chlorpyrifos, indocarb, deltamethrin and metrel salt, and to screen out the optimal ratio, so as to provide scientific basis for the research and development of its mixture, researchers from the College of Plant Protection of Nanjing Agricultural University adopted the indoor artificial feed toxicity mixing method. The toxicity of fluralaner, chlorpyrifos, indocarb, deltamethrin, megamectin and their mixtures to the third instar larvae of Moth twill was determined, and the combined action of the compound agents was evaluated by co-toxicity coefficient method.

Single dose results showed that the LC50 values of fluralaner, deltamethrin and metrel salt were 0.48, 0.65 and 0.38 mg/kg, respectively. The LC50 values of chlorpyrifos and indocarb were 8.71 mg/kg and 3.08 mg/kg, respectively, 48 h after treatment.

The mixing results showed that fluralaner and chlorpyrifos had good synergism, and the highest co-toxicity coefficient was 164.2 when the ratio was 3:2. When mixed with indacarb, it has additive effect. However, when combined with deltamethrin or methylene salt, both showed antagonistic effect.

The results of this study provided a scientific basis for the research and development of the synergistic pesticide mixture of fluralaner.

As a leading APIs & pharmaceutical intermediates ( supplier in China, Huateng Pharma provides Fluralaner (CAS NO CAS NO.864731-61-3) ( from lab to commercial scale. Also, we can provide CDMO services to meet your requirements, combining a high level of competencies, equipment and quality.

Source:Hunan Huateng Pharmaceutical Co. Ltd.
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