Table 2. Intensity percentage (%HPLC) and levels (almonertinibng Eq./g) of [14C]almonertinib and its metabolites over the total radioactivity in plasma samples.
| Metabolic peak, no. | Liquid phase time, Rt (min) | % HPLCa | Level (almonertinib ng Eq./g)a | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 2 h | 4 h | 6 h | 10 h | 24 h | 48 h | 2 h | 4 h | 6 h | 10 h | 24h | 48 h | |||
| 1 | 2.6–3.9 | 5.41 | ND | ND | 3.45 | ND | ND | 17.8 | ND | ND | 12.5 | ND | ND | |
| 3 | 10.1–10.6 | 1.35 | ND | ND | ND | ND | ND | 4.44 | ND | ND | ND | ND | ND | |
| 5 | 12.1–13.1 | ND | ND | ND | 3.45 | ND | ND | ND | ND | ND | 12.5 | ND | ND | |
| 7 | 14.1–15.4 | 1.35 | ND | ND | ND | ND | ND | 4.44 | ND | ND | ND | ND | ND | |
| 9 | 16.9–17.9 | ND | ND | ND | 3.45 | ND | ND | ND | ND | ND | 12.5 | ND | ND | |
| 10 (M717) | 18.3–18.9 | 1.35 | ND | 4.08 | ND | ND | ND | 4.44 | ND | 15.2 | ND | ND | ND | |
| 17 | 27.1–29.6 | ND | 1.67 | ND | ND | ND | ND | ND | 7.75 | ND | ND | ND | ND | |
| 23 (M617 and M575) | 41.1–42.6 | 1.35 | ND | ND | ND | ND | ND | 4.44 | ND | ND | ND | ND | ND | |
| 24 (M541a and M470a) | 43.4–44.4 | 1.35 | ND | ND | ND | ND | ND | 4.44 | ND | ND | ND | ND | ND | |
| 29 (almonertinib-M30) | 49.6–50.6 | 1.35 | 10 | 4.08 | 10.35 | ND | ND | 4.44 | 46.4 | 15.2 | 37.2 | ND | ND | |
| 32 (M511a) | 54.1–54.9 | ND | ND | 2.04 | ND | ND | ND | ND | ND | 7.61 | ND | ND | ND | |
| 33 (M470e) | 55.4–56.1 | 2.7 | 1.67 | ND | ND | ND | ND | 8.88 | 7.75 | ND | ND | ND | ND | |
| 34 (M440) | 56.4–56.9 | 10.81 | 21.67 | 16.33 | 3.45 | 9.68 | ND | 35.5 | 101 | 60.8 | 12.5 | 31.5 | ND | |
| 35 (M497b) | 56.9–57.4 | 1.35 | 1.67 | ND | ND | ND | ND | 4.44 | 7.75 | ND | ND | ND | ND | |
| 36 (HAS-719) | 57.9–58.4 | 2.7 | ND | 8.16 | 3.45 | 16.13 | ND | 8.88 | ND | 30.4 | 12.5 | 52.3 | ND | |
| 37 (almonertinib-M2) | 58.6–59.4 | 8.11 | 1.67 | 2.04 | 3.45 | 3.23 | 25 | 26.7 | 7.75 | 7.61 | 12.5 | 10.5 | 70.5 | |
| 38 ([14C]almonertinib) | 59.6–60.1 | 60.81 | 61.67 | 63.27 | 68.97 | 70.97 | 75 | 200 | 286 | 236 | 249 | 231 | 212 | |
a, the percentages of [14C]almonertinib and its metabolites over plasma extract samples can be seen in ARC1340N: 9a, 9b, 10a, 10b, 11a, 11b, 12a, 12b, 13a, 13b, 14a, and 14b. Due to the low radioactivity in the 96-h plasma sample, no radioactive metabolites were detected.