Table 2.
Pharmacokinetic (PK) of exemestane and 17-hydroexemestane of serum samples processed in the absence (A) and presence (B) of beta-glucuronidase. The data are stratified by UGT2B17 genotype.
| A. Without beta-glucuronidase | ||||||
|---|---|---|---|---|---|---|
| Exemestane | 17-hydroexemestane | |||||
| PK Parameter, unit | UGT2B17 *1/*1 (n = 8) | UGT2B17 *2/*2 (n = 6) | P values | UGT2B17 *1/*1 (n = 8) | UGT2B17 *2/*2 (n = 6) | P values |
| AUC0-∞, ng × hr/ml (SD) | 22.7 (10.5) | 19.7 (3.8) | 0.7 | 1.2 (0.8) | 1.3 (0.3) | 0.4 |
| Cmax, ng/ml (SD) | 5.6 (10.5) | 5.3 (1.4) | 0.7 | 0.2 (0.1) | 0.2 (0.1) | 0.9 |
| Tmax, hr (SD) | 3.1 (1.2) | 1.7 (1.2) | 0.1 | 3.6 (1.5) | 2 (1.1) | 0.06 |
| B. With beta-glucuronidase | ||||||
|---|---|---|---|---|---|---|
| Exemestane | 17-hydroexemestane | |||||
| PK Parameter, unit | UGT2B17 *1/*1 (n = 8) | UGT2B17 *2/*2 (n = 6) | P values | UGT2B17 *1/*1 (n = 8) | UGT2B17 *2/*2 (n = 6) | P values |
| AUC0-∞, ng × hr/ml (SD) | 19.8 (5.5) | 19.0 (3.3) | 0.5 | 11.7 (7.1) | 1.6 (0.7) | 0.0007 |
| Cmax, ng/ml (SD) | 4.4 (1.6) | 5.2 (1.5) | 0.3 | 1.7 (1.5) | 0.2 (0.1) | 0.0007 |
| Tmax, hr (SD) | 3.1 (1.2) | 1.9 (1.2) | 0.1 | 3.5 (0.9) | 2 (1.1) | 0.02 |
AUC, area under the plasma concentration-time curve; SD, standard deviation;