Projected human CNS penetration of 5-FU after oral administration of capecitabine
| Compound (Analyte) | Clinical Dose | Cplasma,max | Cu,plasma,max | Cu,brain,max | CCSF,max |
|---|---|---|---|---|---|
| ng/ml | ng/ml | ng/g | ng/ml | ||
| 5-FU | Capecitabine 2000 mg/m2/day | 472 (343–650) | 449 (326–618) | 76.3 (55.4–105) | 130 (94.5–179) |
| Capecitabine 2000 mg/m2/day + lapatinib 1250 mg/day | 375 (274–512) | 357 (261–487) | 60.7 (44.4–82.8) | 104 (75.7–141) |
Data are presented as mean (90% CI); Kp,uu,brain at 0.17 from preclinical brain tumor in BCBM mouse was used to estimate the free brain concentration of 5-FU; Kp,uu,CSF at 0.29 from BALB/c mouse was used to estimate CSF concentration of 5-FU.