Table 2.
Demographics and baseline characteristics of subjects, route of administration, formulation, and fed/fasted state included in axitinib population pharmacokinetic analysis
| Characteristic | n = 337 |
|---|---|
| Gender, n (%) | |
| Male | 315 (93) |
| Female | 22 (7) |
| Race, n (%) | |
| White | 208 (62) |
| Black | 28 (8) |
| Asian (excluding Japanese) | 59 (18) |
| Japanese | 20 (6) |
| Hispanic | 11 (3) |
| Others | 11 (3) |
| Smoking status, n (%) | |
| Non-smoker | 297 (88) |
| Ex-smoker | 40 (12) |
| UGT1A1*28 genotype, n (%)* | |
| Homozygous wild-type (TA6/TA6) | 173 (51) |
| Heterozygous (TA6/TA7) | 107 (32) |
| Homozygous variant (TA7/TA7) | 35 (10) |
| Other† | 21 (6) |
| Unknown‡ | 1 (N/A) |
| CYP2C19 inferred phenotype, n (%)* | |
| Extensive metabolizer | 312 (93) |
| Ultra-rapid metabolizer | 8 (2) |
| Poor metabolizer | 15 (4) |
| Unknown‡ | 2 (N/A) |
| Age (years) median (mean ± SD) | 31.0 (34.1 ± 11.6) |
| Weight (kg) median (mean ± SD) | 75.0 (76.7 ± 11.6) |
| CLcr (ml min–1) median (mean ± SD) | 115.7 (117.2 ± 24.5) |
| AST (U l–1) median (mean ± SD) | 23.0 (23.9 ± 7.9) |
| ALT (U l–1) median (mean ± SD) | 22.0 (24.1 ± 9.9) |
| Bilirubin (mg dl–1) median (mean ± SD) | 0.7 (0.8 ± 0.4) |
| Route of administration, Form, Fed/Fasted, n (%)§ | |
| Oral, Form IV, Fasted | 231 (69) |
| Oral, Form IV, Fed | 138 (41) |
| Oral, Form XLI, Fed | 54 (16) |
| i.v., Form IV, Fasted | 16 (5) |
Percentage was calculated from the total number of subjects with genotype or inferred phenotype data.
Three main genotypes were derived for the UGT1A1*28 polymorphism based on the number (i.e. 6 or 7) of promoter TA repeats: (1) TA6/TA6 (homozygous wild-type), (2) TA6/TA7 (heterozygous) or (3) TA7/TA7 (homozygous variant). All other polymorphisms (i.e. number of TA repeats different from 6 or 7) were classified as ‘other.’
No genotyping samples were collected. These subjects were grouped with the reference group during the covariate testing.
Studies varied with respect to route of administration, formulation and fed/fasted; hence, subjects who crossed over to different treatments were counted more than once. ALT, alanine aminotransferase; AST, aspartate aminotransferase; CLcr, creatinine clearance; i.v., intravenous; N/A, not applicable.