Table 6. Intensity percentage (%HPLC) and percentage of dose administered (%Dose) of [14C] almonertinib and its metabolites over the total radioactivity in feces samples at different time intervals in 4 participants.
| Metabolic peak No. | Liquid phase time, Rt (min) | 0–48 h (45.32%Dose) | 48–96 h (20.06%Dose) | 96–240 h (16.61%Dose) | |||||
|---|---|---|---|---|---|---|---|---|---|
| % HPLCa | % Doseb | %HPLCa | % Doseb | %HPLCa | % Doseb | ||||
| 1 | 2.9–3.1 | ND | ND | 0.42 | 0.08 | ND | ND | ||
| 3 | 9.9–10.4 | 0.29 | 0.13 | 0.69 | 0.14 | ND | ND | ||
| 4 | 10.6–11.1 | 0.57 | 0.26 | 1.25 | 0.25 | ND | ND | ||
| 5 | 11.6–12.1 | 0.90 | 0.41 | 0.63 | 0.13 | 0.45 | 0.07 | ||
| 6 | 12.6–13.4 | 0.98 | 0.44 | 1.11 | 0.22 | 0.45 | 0.07 | ||
| 7 | 13.6–13.9 | 0.41 | 0.19 | 0.56 | 0.11 | ND | ND | ||
| 8 | 15.1–15.4 | 2.86 | 1.30 | 1.74 | 0.35 | ND | ND | ||
| 9 | 16.60 | 1.60 | 0.72 | 1.67 | 0.34 | 1.35 | 0.22 | ||
| 10 (M717) | 17.4–17.9 | 0.74 | 0.34 | 1.11 | 0.22 | 0.45 | 0.07 | ||
| 11 | 18.6–19.4 | 2.54 | 1.15 | 2.36 | 0.47 | 2.69 | 0.45 | ||
| 12 (M607) | 19.9–20.6 | 3.11 | 1.41 | 2.64 | 0.53 | 2.24 | 0.37 | ||
| 13 (M621) | 21.1–21.9 | 1.68 | 0.76 | 1.94 | 0.39 | 0.45 | 0.07 | ||
| 14 (M621a) | 23.1–23.4 | 1.76 | 0.80 | 1.67 | 0.34 | 2.69 | 0.45 | ||
| 15 | 23.9–24.3 | 0.82 | 0.37 | 1.11 | 0.22 | 0.90 | 0.15 | ||
| 16 | 24.90 | 1.06 | 0.48 | 1.25 | 0.25 | 0.45 | 0.07 | ||
| 17 | 26.1–27.6 | 2.50 | 1.13 | 2.50 | 0.50 | 0.90 | 0.15 | ||
| 18 (M527a) | 29.9–30.3 | 0.74 | 0.34 | 0.42 | 0.08 | ND | ND | ||
| 19 | 31.1–31.6 | 0.98 | 0.44 | 0.83 | 0.17 | 0.45 | 0.07 | ||
| 20 | 32.9–34.4 | 2.37 | 1.07 | 1.94 | 0.39 | 0.45 | 0.07 | ||
| 21 (M527b) | 36.9–37.4 | 4.74 | 2.15 | 3.12 | 0.63 | 0.90 | 0.15 | ||
| 22 (M687) | 37.9–38.9 | 1.47 | 0.67 | 2.92 | 0.59 | 2.69 | 0.45 | ||
| 23 (M617 and M575) | 41.1–41.5 | 8.55 | 3.87 | 7.56 | 1.52 | 8.97 | 1.49 | ||
| 24 (M541a and M470a) | 42.6–42.9 | 13.25 | 6.02 | 12.98 | 2.61 | 21.53 | 3.57 | ||
| 25 (M632b) | 44.1–44.4 | 1.51 | 0.68 | 1.60 | 0.32 | 0.90 | 0.15 | ||
| 26 (M646) | 45.3–45.6 | 1.64 | 0.74 | 1.94 | 0.39 | 4.48 | 0.74 | ||
| 27 (M688) | 46.1–46.4 | 2.45 | 1.11 | 3.05 | 0.61 | 2.69 | 0.45 | ||
| 28 (M470b and M541c) | 47.90 | 2.78 | 1.26 | 3.12 | 0.63 | 2.24 | 0.37 | ||
| 29 (almonertinib-M30 and M470c) | 48.9–49.8 | 1.19 | 0.54 | 0.97 | 0.19 | ND | ND | ||
| 30 (M470d) | 50.6–51.6 | 1.47 | 0.67 | 1.60 | 0.32 | 0.90 | 0.15 | ||
| 31 (M497a) | 52.8–53.4 | 0.16 | 0.07 | 0.28 | 0.06 | ND | ND | ||
| 32 (M511a) | 54.1–54.5 | 2.95 | 1.34 | 3.05 | 0.61 | 1.35 | 0.22 | ||
| 33 (M470e) | 54.90 | 1.55 | 0.70 | 2.08 | 0.42 | 1.79 | 0.30 | ||
| 34 (M440) | 55.6–55.9 | 2.45 | 1.11 | 1.80 | 0.36 | 4.48 | 0.74 | ||
| 35 (M497b) | 56.10 | 1.06 | 0.48 | 1.25 | 0.25 | 0.90 | 0.15 | ||
| 36 (HAS-719) | 56.9–57.1 | 12.31 | 5.57 | 17.07 | 3.44 | 22.87 | 3.80 | ||
| 37 (almonertinib-M2) | 57.8–58.1 | 0.74 | 0.34 | 0.83 | 0.17 | 1.35 | 0.22 | ||
| 38 ([14C]almonertinib) | 58.9–59.1 | 11.94 | 5.39 | 7.56 | 1.52 | 7.18 | 1.19 | ||
| 39c | 60.1–69.9 | 1.88 | 0.85 | 1.39 | 0.28 | 0.90 | 0.15 | ||
| Othersc | <0.01 | ND | <0.01 | ND | <0.01 | ND | |||
a, the intensity percentages of [14C]almonertinib and its metabolites over the TRA in urine samples. For specific data, see ARC1340N: 2a, 2b, 3a, and 3b; b, the dose percentages of [14C]almonertinib and its metabolites (%Dose) = the total radioactivity in urine sample over the dose administered (RTC01289) × the intensity percentages of [14C]almonertinib and its metabolites over the TRA in urine sample; c, contains multiple <0.1% metabolites. ND, not detected.