Table 3.
Rates of formation (V, pmol mg−1 protein min−1) of Z-4-OH-tam from 10 µm tamoxifen (1% dimethyl sulfoxide) and CYP expression (pmol mg−1 protein) in human liver microsomes from patients with varying CYP2B6 (a), CYP2D6 (b) and CYP2C9 (c) genotypes. Data are mean±s.d. (CI).
| a | ||
|---|---|---|
| CYP2B6 variant alleles | V (pmol mg−1 protein min−1) | CYP2B6 expression |
| zero (n = 18) | 9.44±5.47 (6.72–12.2) | 26.3±18.6 (17.1–35.6)a,b |
| one (n = 20) | 8.83±6.08 (6.06–11.6) | 15.4±19.2 (6.67–24.1) |
| two (n = 10) | 6.82±3.76 (4.13–9.51) | 8.77±5.88 (4.56–13.0) |
| b | ||
|---|---|---|
| CYP2D6 functional alleles | V (pmol mg−1 protein min−1) | CYP2D6 expression |
| two (n = 26) | 9.93±5.43 (7.74–12.1)c | 10.4±7.08 (7.51–13.4)d |
| one (n = 18) | 8.10±5.48 (5.38–10.8) | 6.45±4.82 (4.05–8.84)e |
| zero (n = 4) | 5.04±3.17 (−0.002–10.1) | 0.155±0.161 (−0.1–0.4) |
| c | CYP2C9 variant alleles | V (pmol mg−1 protein min−1) | CYP2C9 expression | ||
|---|---|---|---|---|---|
| zero: CYP2C9*1/*1 (n = 26) | 9.98±6.67 (7.29–12.7) | 123±52.0 (102–144) | |||
| one: CYP2C9*1/*2 or *1/*3 (n = 19) | 7.81±2.69 (6.51–9.10) | 111±39.6 (91.8–130) | |||
| two: CYP2C9*2/*2 or *2/*3 (n = 4) | 5.12±3.93 (−1.13–11.4) | 94.9±66.1 (−10.3–200) | |||
P<0.05 vs one variant allele
P<0.05 vs two variant alleles
P<0.05 vs zero functional alleles
P<0.001 vs zero functional alleles
P<0.05 vs zero functional alleles.