LY253963, the sodium salt of 1,3,4-thiadiazol-2-ylcyanamide, was evaluated in tissue culture and in cotton rats for toxicity and antiviral efficacy against respiratory syncytial (RSV) and parainfluenza type 3 (PIV3) viruses. The selective index (ratio of the median toxic dose: median efficacious dose) of LY253963 in HEp2 tissue culture cells was greater than 100 against both RSV and PIV3. When given intraperitoneally to cotton rats, the minimum protective dose of LY253963 against both of these viruses was between 1 and 3 mg/kg/day. In contrast, doses of LY253963 as high as 30 mg/kg/day, administered orally after experimental inoculation of virus, did not significantly reduce pulmonary virus titers in treated animals compared to control animals given placebo. No toxic effects were noted in cotton rats, even in those given 20 mg/kg/day for eight consecutive days.

01 Jul 1990·Antiviral ResearchQ2 · MEDICINE

Anti-influenza virus activity of the compound LY253963

Q2 · MEDICINE

Article

Author: Barbara S. Rollins ; Alan J. Hay ; Frederick G. Hayden

The compound LY253963 (1,3,4-thiadiazol-2-ylcyanamide) inhibited the in vitro replication of representative influenza A and B viruses in Madin-Darby canine kidney (MDCK) cells at concentrations of 1-3.2 micrograms/ml. The yield of an influenza A (H3N2) virus in primary rhesus monkey kidney (RMK) cells was inhibited at 0.1-0.3 micrograms/ml. However, similar concentrations were inhibitory for the growth of uninfected MCDK or RMK cells. Combination drug studies generally found indifferent interactions between LY253963 and ribavirin or rimantadine. In timing of additional studies, hemagglutinin expression was inhibited to the greatest extent when LY253963 exposure was begun at least 8 h before viral infection, which suggested either slow uptake or intracellular metabolism of LY253963 to an active form. Virus-specific protein synthesis was inhibited to a greater extent by ribavirin 10 micrograms/ml or rimantadine 1 microgram/ml than by LY253963 10 micrograms/ml. No drug-resistant mutants were detected during serial passage of an influenza A (H3N2) virus in the presence of LY253963 1-16 micrograms/ml. In summary, we found that LY253963 inhibited influenza A and B virus replication in several cell types, but that it was associated with cytostatic effects at low concentrations. These studies failed to identify a selective anti-influenza action.

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Indication	Highest Phase	Country/Location	Organization	Date
Respiratory Syncytial Virus Infections	Preclinical	US	Eli Lilly & Co.	-

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