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. 2017 Feb 20;83(6):1353–1356. doi: 10.1111/bcp.13249

Table 1.

Multivariable determinants of tacrolimus apparent oral clearance

MDZ model 4β‐OHC model
Determinants B value P R 2 Determinants B value P R 2
All patients (n = 147) 0.569 0.525
CYP3A5 expresser 0.671 <0.001 0.292 CYP3A5 expresser 0.604 <0.001 0.292
MDZ Cl/F 0.337 <0.001 0.103 4β‐OHC/C 0.304 0.002 0.032
Haematocrit –3.358 <0.001 0.060 Haematocrit –2.661 <0.001 0.074
Weight (kg) 0.008 <0.001 0.046 Weight (kg) 0.012 <0.001 0.050
Age (years) –0.008 0.001 0.040 Age (years) –0.008 0.001 0.061
TAC QD 0.182 0.003 0.029 TAC QD 0.139 0.026 0.017
CYP3A5 non‐expressers (n = 118) 0.437 0.319
MDZ Cl/F 0.423 <0.001 0.220 4β‐OHC/C 0.357 0.002 0.063
Haematocrit –3.398 <0.001 0.097 Haematocrit –2.556 <0.001 0.074
Weight (kg) 0.005 0.029 0.024 Weight (kg) 0.012 <0.001 0.083
Age (years) –0.008 0.002 0.049 Age (years) –0.008 0.005 0.100
TAC QD 0.190 0.005 0.047
CYP3A5 expressers (n = 29) 0.342
Weight (kg) 0.014 0.001 0.247
Age (years) –0.008 0.045 0.095

Neither MDZ Cl/F nor 4β‐OHC/C explained TAC Cl/F variability in CYP3A5 expressers

4β‐OHC/C, 4β‐hydroxycholesterol/cholesterol; CYP, cytochrome P450; MDZ Cl/F, midazolam apparent oral clearance; QD, once‐daily formulation; TAC, tacrolimus