Summary of therapeutic index of GSK356278 over emesis in various preclinical models
The table shows the ED50 values derived in the rat lung neutrophilia and rat pica-feeding assays for GSK356278. The therapeutic index in rodents is summarized as the ratio of the ED50 in the rat lung neutrophilia assay to the ED50 in the rat pica-feeding assay for GSK356278.
| Assay | Rolipram | Roflumilast | GSK356278 |
|---|---|---|---|
| LPS neutrophilia ED50 mg/kg | 3.3a | 0.24a | 0.09 |
| Pica-feeding ED50 mg/kg | 0.5a | 1.6a | 15 |
| Rat (ED50 pica/ED50 LPS neutrophilia) | 0.15a | 6.4a | 166 |
↵a The ED50 values for rolipram and roflumilast are also shown for comparison and were derived using the same assays as for GSK356278 and have been previously described (Davis et al., 2009).