Average levels of circulating eltrombopag and metabolites in humans after a single oral administration of 75 mg of [14C]eltrombopag
Data are mean ± S.D. (n = 6).
| Metabolite | %Plasma Radioactivity | |||
|---|---|---|---|---|
| 4 h | 12 h | 24 h | 48 h | |
| M1a | 0.4 ± N.A. | 0.8 ± N.A. | N.Q. | N.Q. |
| M2b | 0.6 ± N.A. | 2.3 ± N.A. | 7.3 ± 1.5 | 11.7 ± 2.1 |
| Eltrombopag | 94.2 ± 5.5 | 80.1 ± 8.4 | 62.3 ± 7.1 | 43.6 ± 5.6 |
| Total quantified | 95.3 ± 5.5 | 83.3 ± 8.4 | 69.6 ± 8.6 | 55.3 ± 7.7 |
N.A., not available because the metabolite was quantifiable in one or two of six subjects only as described above; N.Q., below level of quantitation.
a M1 was quantifiable only in subject 1 at 4 h (2.4%) and subject 6 at 12 h (5.0%) and not quantifiable in other subjects.
b M2 was a mixture of three coeluting acyl glucuronide isomers; this metabolite was quantifiable only in subject 3 (3.7%) at 4 h and in subject 1 (11%) and subject 4 (2.8%) at 12 h and was not quantifiable in other subjects at these two sampling points.