moxidectin Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
5286 113507-06-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • moxidectin
The mechanism by which moxidectin exhibits its effect against O. volvulus is not known. Studies with other nematodes suggest that moxidectin binds to glutamate-gated chloride channels (GluCl), gamma-aminobutyric acid (GABA) receptors and/or ATP-binding cassette (ABC) transporters. This leads to increased permeability, influx of chloride ions, hyperpolarization and muscle paralysis. Additionally, there is a reduction in motility of all stages of the parasite, excretion of immunomodulatory proteins, and the fertility of both male and female adult worms.
  • Molecular weight: 639.83
  • Formula: C37H53NO8
  • CLOGP: 7.18
  • LIPINSKI: 2
  • HAC: 9
  • HDO: 2
  • TPSA: 116.04
  • ALOGS: -5.09
  • ROTB: 3

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
June 13, 2018 FDA MDGH

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC P02CX03 ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS
ANTHELMINTICS
ANTINEMATODAL AGENTS
Other antinematodals
MeSH PA D000871 Anthelmintics
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000969 Antinematodal Agents
MeSH PA D000977 Antiparasitic Agents
MeSH PA D007306 Insecticides
MeSH PA D010575 Pesticides

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Infection by Onchocerca volvulus indication 38539003 DOID:11678

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.24 acidic
pKa2 13.33 acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
2MG MOXIDECTIN MDGH N210867 June 13, 2018 RX TABLET ORAL June 13, 2023 NEW CHEMICAL ENTITY
2MG MOXIDECTIN MDGH N210867 June 13, 2018 RX TABLET ORAL June 13, 2025 INDICATED FOR THE TREATMENT OF ONCHOCERCIASIS DUE TO ONCHOCERCA VOLVULUS IN PATIENTS AGED 12 YEARS AND OLDER

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Glutamate-gated chloride channel Ion channel INHIBITOR UNKNOWN SCIENTIFIC LITERATURE

External reference:

IDSource
C0163557 UMLSCUI
CHEMBL2104415 ChEMBL_ID
D05084 KEGG_DRUG
DB11431 DRUGBANK_ID
C027837 MESH_SUPPLEMENTAL_RECORD_UI
6400 INN_ID
NGU5H31YO9 UNII
6436009 PUBCHEM_CID
1047072 RXNORM
017593 NDDF
781257003 SNOMEDCT_US
781277005 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Moxidectin HUMAN PRESCRIPTION DRUG LABEL 1 71705-050 TABLET 2 mg ORAL NDA 26 sections