TABLE 1.
In vitro Marburg egress, ADME, and PK data
| Parameter | Value for FC-10696 |
|---|---|
| % reduction in Marburg egress assay at concn (μM)a | |
| 1.0 | 99 |
| 0.5 | 94 |
| 0.3 | 91 |
| 0.1 | 86 |
| 0.03 | 0 |
| MW | 357.5 |
| t1/2 (min)b | |
| MLM stability | 76.9 |
| HLM stability | 1670 |
| Mouse PK (i.p. administration)c | |
| Cmax (ng/ml) | 953 |
| AUC (ng · ml/h) | 1,378 |
| t1/2 (s) | 1.5 |
| i.p. bioavailability (%) | 42 |
a
Percent reduction of Marburg VLPs at the listed compound concentrations in HEK293T cells, with the positive control FC-4005 (26) run at 1 μM (∼90% ± 10%).
b
MLM, mouse liver microsome; HLM, human liver microsome.
c
BALB/cJ mice were given one 10-mg/kg dose of drug with plasma collection time points of 0.25, 0.5, 1, 2, and 6 h. Intraperitoneal bioavailability is the ratio of i.p. AUC to i.v. AUC × 100. PK parameters for i.v. administration are not shown.