title: [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)].
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.
authors.forename: A V
authors.initials: AV
authors.lastname: Ivashchenko
authors.forename: P M
authors.initials: PM
authors.lastname: Iamanushkin
authors.forename: O D
authors.initials: OD
authors.lastname: Mit'kin
authors.forename: O M
authors.initials: OM
authors.lastname: Korzinov
authors.forename: N A
authors.initials: NA
authors.lastname: Shevkun
authors.forename: R N
authors.initials: RN
authors.lastname: Karapetian
authors.forename: A A
authors.initials: AA
authors.lastname: Ivashchenko
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000493:pharmacokinetics* / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D006801:Humans; D053122:Influenza A Virus, H3N2 Subtype; D008297:Male; D020714:Maximum Tolerated Dose; D051379:Mice; D008807:Mice, Inbred BALB C; D009976:Orthomyxoviridae Infections / Q000097:blood / Q000188:drug therapy*
chemical_list: D000998:Antiviral Agents