Moxidectin

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Structural formula
Structure of moxidectin
General
Non-proprietary name Moxidectin
other names
  • Milbemycin
  • Cydectin
Molecular formula C 37 H 53 NO 8
External identifiers / databases
CAS number 113507-06-5
EC number 635-129-7
ECHA InfoCard 100.163.046
PubChem 9571036
ChemSpider 16736424
DrugBank DB11431
Wikidata Q903824
Drug information
ATC code

Q P54AB02

Drug class

Antiparasitic

properties
Molar mass 639.82 g · mol -1
solubility

practically insoluble in water

safety instructions
Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed
GHS labeling of hazardous substances
06 - Toxic or very toxic 09 - Dangerous for the environment

danger

H and P phrases H: 301-400
P: 301 + 330 + 331 + 310
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Moxidectin is an anti-parasitic drug . Chemically it is a macrocyclic lactone from the milbemycine group . The active ingredient is a chemical modification of the fermentation product nemadectin of the ray fungus Streptomyces cyaneogriseus . It is a lipophilic substance that is well soluble in organic solvents but poorly soluble in water.

Clinical information

The drug is used in veterinary medicine as a remedy against roundworms and mites . The anti-parasitic effect is mediated by an increase in the membrane permeability of the nerve cells of the nematodes or the nerve and muscle cells of the arthropods for chloride ions.

In human medicine, moxidectin has been approved in the United States since June 2018 for the treatment of onchocerciasis , a disease caused by the tropical nematode Onchocerca volvulus . The treatment is carried out with a single oral administration of the active ingredient.

It is assumed that P2X4 purino receptors modulate reward stimuli by regulating synaptic plasticity in the mesocortical system . Moxidectin has a potentiating effect on the P2X4 receptor and shows a reduction in ethanol uptake in the experiment on mice. This receptor is seen as a promising target in drug development for the treatment of alcoholism .

Hazard assessment

The Committee for Medicinal Products for Veterinary Use (CVMP) of the European Medicines Agency (EMA) concluded that moxidectin is persistent , bioaccumulative and toxic ( PBT ).

Trade names (veterinary medicinal products)

Cydectin, Equest, Equimoxectin, Zermex

Combination preparations

Individual evidence

  1. ↑ a b c data sheet moxidectin from Sigma-Aldrich , accessed on May 14, 2017 ( PDF ).
  2. ↑ New Drug Application (NDA): 210867 , accessed February 10, 2019.
  3. ↑ Huynh N, Arabian N, Naito A, Louie S, Jakowec MW, Asatryan L, Davies DL: Preclinical development of moxidectin as a novel therapeutic for alcohol use disorder . In: Neuropharmacology . 113, No. Pt A, 2016, pp. 60-70. doi : 10.1016 / j.neuropharm.2016.09.016 . PMID 27641072 .
  4. ↑ Franklin KM, Asatryan L, Jakowec MW, Trudell JR, Bell RL, Davies DL: P2X4 receptors (P2X4Rs) represent a novel target for the development of drugs to prevent and / or treat alcohol use disorders . In: Front Neurosci . 8, 2014, p. 176. doi : 10.3389 / fnins.2014.00176 . PMID 25009459 . PMC 4068020 (free full text).
  5. ↑ EMA: Questions and Answers on the Effects of Moxidectin-Containing Veterinary Medicinal Products for Use in Cattle, Sheep and Horses on the Environment , 2017.
  6. ↑ CVMP: Moxidectin - Art. 35 - Annexes I-II-III-IV , 2017.

Web links