Estimated amount of naveglitazar and metabolites in pooled plasma from mice, rats, and monkeys after oral administration of [14C]naveglitazar
Compound | Percentage of Plasma Radioactivitya | ||||
|---|---|---|---|---|---|
| Mouseb | Ratc | Monkeyd | |||
| Naveglitazar (includes compound 591026) | 76.2 | 81.0 | 68.2 | ||
| M1 (sulfate conjugate of para-hydroxy naveglitazar, LY2291229) | 0.4 | 3.7 | 5.6 | ||
| M2 (para-hydroxy naveglitazar, LY621631) | 0.4 | N.D. | 7.5 | ||
| M3 (glucuronide conjugate of para-hydroxy naveglitazar) | 3.0 | N.D. | N.D. | ||
| M6 (phenyl acetic acid metabolite) | 3.8 | N.Q. | N.Q. | ||
| M7 (dehydrogenated naveglitazar, LY2419535) | 0.4 | 0.6 | N.D. | ||
| M9 (dehydrogenated naveglitazar + O + sulfate) | N.Q. | N.D. | N.D. | ||
| M17 (sulfate conjugate of 4-hydroxy diphenyl ether) | 0.6 | N.D. | 0.7 | ||
| Total | 84.8 | 85.3 | 82.0 | ||
N.D., not detected; N.Q., detected but not quantifiable.
↵ a The percentage of plasma radioactivity values was adjusted by multiplying extraction recoveries, which were 88%, 85%, and 82% for mouse, rat, and monkey plasma, respectively. Time points containing the highest level of radioactivity were used to pool samples to estimate analytes: b 2 h for mice, c 1 h for rats, and d 4 h for monkeys.