||APIs for Veterinary
||Milbemycin A 5-oxime; Milbemite; Trifexis; Milbemycin oxime; Interceptor; Milbe Mite
||Prepared by the two natural products, oxidation and oximation, of an 80:20 ratio of milbemycin A3 and A,Milbemycin oxime is a semi-synthetic macrocyclic lactone. As a nematocide and insecticide in veterinary medicine,it opens glutamate sensitive chloride channels in neurons of invertebrates that leads to paralysis by hyperpolarisation of these cells and signal transfer blocking.
M1-family aminopeptidase: IC50 = 2.6 µM (Plasmodium falciparum 3D7); Bile acid transporter: IC50 = 3.6 µM (human); TGR5: EC5050 = 36.4 µM (human); HCT-116: IC50 >50 µM (human); GBM: IC50 >50 µM (human)
Certificate of Analysis-Milbemycin Oxime 129496-10-2 B15W06021
1.Efficacy of oral afoxolaner plus milbemycin oxime chewables against induced infestations with Dermacentor reticulatus in dogs
Steffen Rehbein & Josephus J. Fourie & Christa de Vos. Parasitol Res (2016) 115:1845–1851
In order to provide dog owners and veterinarians with products to be used conveniently for the treatment and/or control of multiple ectoparasites and endoparasites which may infest or
infect dogs concurrently, the parasiticidal spectrum of NexGard® chewable tablets was extended through the combination of afoxolaner with the macrocyclic lactone, milbemycin oxime, in a novel braised beef-flavored chewable formulation (NexGard Spectra®). This formulation, with respect to its composition, is similar to the afoxolaner singleentity chewable tablet formulation except for the active ingredients. Milbemycin oxime was proven to be safe in dogs (Jung et al. 2002) and, when administered to dogs orally at a dose of 0.5 mg per kg body weight, to be efficacious against adult intestinal nematode infections and to prevent heartworm disease by interrupting the life cycle of Dirofilaria immitis (Nolan and Lok 2012). At that dose and route of administration, milbemycin oxime did not demonstrate activity against fleas and ticks in dogs (Snyder and Wiseman 2012; Merial, unpublished data). The interrelationship between milbemycin oxime and afoxolaner, however, was not known.