Whole-body autoradiography (WBA) allows the determination of sites of accumulation and differential distribution of radiolabeled compounds within organs. WBA is routinely conducted in pregnant rats to evaluate placental transfer and fetal distribution of potential developmental toxins. This technique has recently been adapted to evaluate tissue distribution in the pregnant rabbit, which may be a more appropriate model for some pharmaceutical candidates. A preliminary WBA study was conducted on New Zealand white (NZW) rabbits at gestation day 18, 1 h following a single oral dose of 14C-glucose. The purpose of this study was to validate the use of WBA techniques in assessing the placental transfer of compounds in pregnant rabbits. Antiviral compound LY217896 sodium demonstrated developmental toxicity in the pregnant NZW rabbit following multiple oral doses of 10 mg/kg on gestation days 6 through 18. WBA techniques were used to determine the distribution of radiocarbon 30 minutes following a single oral 10-mg/kg dose of 14C-LY217896 sodium in pregnant NZW rabbits on gestation day 18.

01 Mar 1995·Biopharmaceutics & Drug DispositionQ4 · MEDICINE

Uptake and biodisposition of 2‐ylcyanamide‐1,3,4‐thiadiazole (LY217896) by red blood cells

Q4 · MEDICINE

Article

Author: Albert Peyton ; Peter L Bonate

AbstractIn man, 14C‐2‐ylcyanamide‐134‐thiadiazole (LY217896) accumulates into red blood cells (RBCs) where it is rapidly metabolized. Both in man and ex vivo, within a few hours of administration of 14C‐LY217896 at least two intracellular metabolites were detected within the RBCs using HPLC. These metabolites were never detected extracellularly. After 24 h no detectable radioactivity was found in the plasma and all the radioactivity was detected within the cellular fraction. All radioactivity was identified as a single peak within the RBCs, indicating the metabolite(s) to be highly polar compared to LY217896. Parent LY217896 was never detected within the RBCs at any time point, suggesting transport, either by diffusion or a carrier mediated mechanism, was the rate limiting step. Due to the nature of the preparation it was impossible to separately characterize uptake and biotransformation. Nevertheless, uptake/biotransformation was found to be temperature sensitive, sodium independent, and energy dependent. Both niacin and vitamin B6, but not nicotinamide, competitively blocked the uptake and subsequent intracellular metabolism of LY217896.

01 May 1994·Antimicrobial Agents and ChemotherapyQ2 · MEDICINE

Oral LY217896 for prevention of experimental influenza A virus infection and illness in humans

Q2 · MEDICINE

Article

Author: Tunkel, A R ; Harris, J ; Allerheiligen, S ; Hayden, F G ; Treanor, J J ; Betts, R F

The efficacy and safety of oral LY217896 for prevention of experimental influenza A/Kawasaki/86 (H1N1) virus infection were assessed in susceptible males randomly assigned to receive LY217896 (75 mg) or placebo once daily for 7 days beginning 24 h prior to viral challenge. The rates of virus shedding (100% in both groups), days of viral shedding (3.1 +/- 1.3 for the LY217896 group; 2.8 +/- 1.3 for the placebo group), and titers of virus in nasal washings did not differ between the groups. Mild upper respiratory tract illness (72% in the LY217896 group; 69% in the placebo group) developed in similar proportions of each group. LY217896 was associated with asymptomatic rises in serum uric acid levels and was ineffective in modifying the virologic or clinical course of experimental influenza A (H1N1) virus infection.

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Indication	Highest Phase	Country/Location	Organization	Date
Influenza, Human	Phase 1	US	Eli Lilly & Co.	01 Nov 1990

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