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Table 1 Tacrolimus pharmacokinetic parameters when coadministered with darunavir/ritonavir (800/100 mg once daily) and with darunavir/cobicistat (800/150 mg once daily)

From: Switch from a ritonavir to a cobicistat containing antiretroviral regimen and impact on tacrolimus levels in a kidney transplant recipient

Pharmacokinetic parameter

1st pharmacokinetic profile

2nd pharmacokinetic profile

3rd pharmacokinetic profile

Tacrolimus co-administered with darunavir/ritonavir (800/100 mg once daily)

 C0h (µg/L)

7.3

6.1

6.2a

 Cmax (µg/L)

15.1

17.7

17.6

 Tmax (h)

8

4

4

 AUC264h (µg h/L)*

2647

2385

2352a

 T1/2 (h)

227

275

266

 CL/F (L/h)

0.2

0.2

0.2

Tacrolimus co-administered with darunavir/cobicistat (800/150 mg once daily)

 C0h (µg/L)

6.8b

4.1

4.0a

 Cmax (µg/L)

11.7

13.7

12.6

 Tmax (h)

2

8

4

 AUC264h (µg h/L)*

1747

1873

1235

 T1/2 (h)

226

175

183

 CL/F (L/h)

0.3

0.3

0.4

  1. *The patient received tacrolimus once every 11 days. The area under the curve (AUC) represents a dosing interval of 11 days except for the thirda and sixtha pharmacokinetic profile for which the dosing interval was 10 days for practical reasons. bTrough level at the day of the switch, i.e., last trough level on darunavir/ritonavir (800/100 mg once daily) and immediately before administration of darunavir/cobicistat (800/150 mg once daily). AUC was calculated by the linear and logarithmic trapezoidal methods. C0h represents pre-dose plasma concentration and Cmax the maximum plasma concentration. Tmax is the time to reach Cmax and T1/2 indicates the elimination half-life. CL/F represents the apparent clearance calculated by dose divided by AUC. For comparison, tacrolimus pharmacokinetic parameters in renal transplant recipients in absence of strong inhibitors are: T1/2: 15.6 h; CL/F: 6.7 L/h14