moxidectin Report issue

Small molecule Orphan Drug FDA Approved FDA Priority Review FDA

Active Ingredient History

  • Now
Moxidectin is a semi-synthetic methoxime derivative of LL F-2924α, commonly referred as F-alpha or nemadectin F-alpha is a product of fermentation of Streptomyces cyaneogriseus subsp. noncyanogenus, a bacterial organism isolated in 1983 from a sample of sand from Victoria, Australia. Moxidectin is a potent, broad-spectrum endectocide with activity against a wide range of nematodes, insects and acari. The compound acts by binding to ligand-gated chloride channels, more specifically the subtypes that are gamma-aminobutyric (GABA) mediated and glutamate-gated. The consequence of Moxidectin binding and activation is an increased permeability, leading to an influx of chloride ions and flaccid paralysis of the parasite leading to death. The macrocyclic lactones probably act by binding to and opening glutamate-gated chloride channels found only in neurons and myocytes of invertebrates. Because moxidectin is very lipophilic, it becomes highly concentrated in the serum. When the concentration of moxidectin in the serum is high, moxidectin is able to cross the blood-brain barrier. Once it is in the central nervous system, a macrocyclic lactone stimulates the synaptic secretion of the inhibitory neurotransmitter, GABA. By binding at the receptor site, GABA causes influx of chloride ions into neurons, causing the neurons to become hyperpolarised, which in turn, causes diminution in neuronal activity, resulting in sedation and relaxation of the skeletal muscles. Signs displayed by foals with moxidectin toxicity included dyspnoea, depression, ataxia, weakness, coma and seizures. In a Phase 3 study compared the efficacy, safety and tolerability of moxidectin and ivermectin in subjects infected with Onchocerca volvulus, which is the parasite that causes river blindness.   NCATS

  • SMILES: CO\N=C1/C[C@]2(C[C@@H]3C[C@@H](C\C=C(C)\C[C@@H](C)\C=C\C=C4/CO[C@@H]5[C@H](O)C(C)=C[C@@H](C(=O)O3)[C@]45O)O2)O[C@@H]([C@H]1C)C(\C)=C\C(C)C
  • Mol. Mass: 639.8186
  • ALogP: 5.73
  • ChEMBL Molecule:
More Chemistry
5-hydroxymilbemycin beta7 | cl 301423 | cl 301,423 | cl-301423 | cydectin | milbemectin | milbemycin | milbemycin a3 | milbemycin a4 | milbemycin alpha1 | milbemycin alpha10 | milbemycin alpha11 | milbemycin alpha13 | milbemycin alpha14 | milbemycin alpha15 | milbemycin alpha2 | milbemycin alpha3 | milbemycin alpha4 | milbemycin alpha5 | milbemycin alpha6 | milbemycin alpha7 | milbemycin alpha8 | milbemycin alpha9 | milbemycin b | milbemycin beta1 | milbemycin beta12 | milbemycin beta2 | milbemycin beta3 | milbemycin d | milbemycins | moxidectin


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