Brain penetration of capecitabine and 5-FU in brain tumor and adjacent normal brain tissue
| Compound | Time Point (hour) | Capecitabine Monotherapy | Capecitabine + Lapatinib | ||||||
|---|---|---|---|---|---|---|---|---|---|
| Normal Brain Tissue | Brain Tumor | Normal Brain Tissue | Brain Tumor | ||||||
| Kp,brain | Kp,uu,brain | Kp,brain | Kp,uu,brain | Kp,brain | Kp,uu,brain | Kp,brain | Kp,uu,brain | ||
| Capecitabine | 1 | 0.06 ± 0.03 | 0.05 ± 0.02 | 0.07 ± 0.03 | 0.05 ± 0.02 | 0.05 ± 0.01 | 0.04 ± 0.01 | 0.05 ± 0.01 | 0.04 ± 0.01 |
| 5-FU | 1 | 0.08 ± 0.02 | 0.06 ± 0.02 | 0.17 ± 0.03a | 0.13 ± 0.02a | 0.15 ± 0.07 | 0.12 ± 0.05 | 0.22 ± 0.10 | 0.17 ± 0.08 |
| Lapatinib | 1 | NC | NC | NC | NC | 0.10 ± 0.01 | NA | 0.12 ± 0.01 | NA |
NA, not applicable (due to protein binding of lapatinib > 99.9% in brain tissue and blood); NC, not conducted; refer to the Supplemental Material to check the raw data and calculations.
↵a p < 0.05.