Moxidectin is a semi-synthetic antiparasitic agent belonging to the the macrocyclic lactone (LC) family, and milbemycin sub-family. It is derived from nemadectin by selective oxidation followed by methyloximation. Nemadectin is a fermentation product of the bacterium Streptomyces cyanogriseus subsp. noncyanogenus. It targets glutamate-gated chloride channels (GluCls) of the parasite. It was patended in 1991 as an anthelmintic for internal parasite control. It is also used in veterinary research and crop pest control. it exhibits low toxicity to the host and low ecotoxicity. The presence of methyloxime affords Moxidectin a greater hydrophobicity and longer biological half-life compared to nemadectin.
Moxidectin is soluble in ethanol, methanol, DMF and DMSO. It is insoluble in water.
| Mechanism of Action | Moxidectin binding increases target GluCl permeability, resulting in an influx of chloride ions and dysfunction of the excretory pore, flaccid paralysis of neuromuscular systems, and death of the nematode and arthropods via host response. |
| Spectrum | Moxidectin is broad-spectrum endectocide effective against a wide range of nematodes, insects, and acari. It is effective for parasites, including macrocyclic lactone (ML)-resistant parasites. It has a higher potency against some parasites, especially filarial nematodes, than the avermectins. |
| Microbiology Applications | A number of in vivo studies demonstrate that Moxidectin has potent activity on microfilariae. |
| References |
Cobb R and Boeckh A (2009) Moxidectin: A review of chemistry, pharmacokinetics and use in horses. Parasites and Vectors 2 (Suppl 2) S5 Maulding D. R & Kumar A (1991) US Patent 4,988,824. Process for the preparation of 23-(C1-C6 alkyloxime)-LL-F28249 compounds. Prichard RK and Geary TC (2019) Perspectives on the utility of moxidectin for the control of parasitic nematodes in the face of developing anthelmintic resistance. Int. J. Parasitol: Drugs and Drug Resis. 10:69-83 Roger K. Prichard RK and Geary TG (2019) Perspectives on the utility of moxidectin for the control of parasitic nematodes in the face of developing anthelmintic resistance. Int. J. Parasitol. Drugs and Drug Resistance 10:69-83 Tagboto SK and Townson S (1996) Onchocerca volvulus and O. lienalis: the microfilaricidal activity of moxidectin compared with that of ivermectin in vitro and in vivo. Ann. Trop. Med. Parasitol. 90:497-505 |