Table 2.
Quantification of crizotinib in the plasma of patients, adjusted doses, and adverse events
| Patient | Daily dose of crizotinib a (mg/day) | Trough concentration (ng/mL (μM)) | Tumor response on day 28 | Crizotinib-induced adverse events b |
|---|---|---|---|---|
| 1 | 400a | 589.3 (1.31) | SD | Fatigue, staggering, dysgeusia, neutropenia***, AST elevation |
| 2 | 500 | 314.1 (0.70) | SD | Nausea, neutropenia |
| 3 | 500 | 370.8 (0.82) | SD | Fatigue, AST and ALT elevations |
| 4 | 500 | 825.2 (1.83) | SD | Fatigue, staggering, eye disorder, dysgeusia, nausea, anorexia, AST elevation, constipation |
| 5 | 500 | 847.8 (1.88) | SD | Fatigue, eye disorder, dysgeusia, nausea, vomiting, constipation, diarrhea, rise in creatinine levels, leukopenia***, neutropenia****, AST and ALT elevations |
| 6 | 500 | 470.8 (1.05) | SD | Fatigue, eye disorder, dysgeusia, constipation, diarrhea, neutropenia, AST elevation |
| 7 | 500 | 573.6 (1.27) | SD | Staggering, anorexia, dysgeusia, nausea, constipation, neutropenia, vomiting, AST elevation, QT interval prolongation*** |
| 8 | 500 | 508.5 (1.13) | SD | Nausea, vomiting, anorexia, neutropenia, AST and ALT elevations*** |
| 9 | 500 | 243.5 (0.54) | SD | Eye disorder |
AST; aspartate aminotransferase, ALT; alanine aminotransferase, SD; stable disease.
aPlasma collection was conducted after the dosage had been adjusted due to crizotinib-induced adverse events. The plasma of patients was collected at day 14 before crizotinib was taken in the morning and was analyzed as the trough sample.
bAll adverse events developed in each patient at days 7, 14, 21 and 28 were listed.
***is grade 3, ****is grade 4, and other adverse events were grade 1 or 2.