[Preclinical study of the new anti-influenza drug candidate AV0038 (ethyl 2-(dimethylaminomethyl)-5-hydroxy-1-methyl-6-(pyridin-3-yl)-1H-indole-3-carboxylate)].
Eksp Klin Farmakol
; 77(5): 23-7, 2014.
Article
in Ru
| MEDLINE
| ID: mdl-25033568
ABSTRACT
In the framework of preclinical testing of AV0038, ethyl 2-(dimethylaminomethyl)-5-hydroxy-1-methyl-6-(pyridin-3-yl)-1H-indole-3-carboxylate, which showed high efficiency in the prevention and treatment of influenza A/Aichi/2/69 (H3N2) in mice, we have studied the drug solubility and stability in aqueous solutions, metabolic stability in human liver microsomes, stability in blood plasma of mice and humans, binding to plasma proteins of mice and humans, pharmacokinetics and bioavailability in mice, and the acute toxicity and the maximum tolerated dose. It is established that AV0038 has attractive pharmacological properties as anti-influenza drug candidate. The therapeutic doses of AV0038 do not cause acute toxicity in mice. It is expedient to continue preclinical investigations and study the drug metabolism, metabolites, and sub-chronic toxicity in test animals.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Antiviral Agents
/
Orthomyxoviridae Infections
/
Influenza A Virus, H3N2 Subtype
Limits:
Animals
/
Humans
/
Male
Language:
Ru
Journal:
Eksp Klin Farmakol
Journal subject:
FARMACOLOGIA
Year:
2014
Document type:
Article
Publication country:
FEDERAÇÃO RUSSA
/
RU
/
RUSIA
/
RUSSIA