Table 2.
Steady state Pharmacokinetics of Once-Daily Oral Administration of Tenofovir Alafenamide (TAF): aTAF (25 mg unboosted) in pregnancy, bTAF (10 mg boosted) in pregnancy, cTAF(25 mg boosted) in pregnancy, dTAF (25 mg unboosted) in non-pregnant adults, and eTAF (10 mg boosted) in non-pregnant adults.
|
a25 mg unboosted |
b10 mg with COBI |
c25 mg with RTV or COBI |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Dose | 2nd Trimester | 3rd Trimester | Postpartum | 2nd Trimester | 3rd Trimester | Postpartum | 2nd Trimester | 3rd Trimester | Postpartum |
d25 mg unboosted (Non-pregnant adults) |
e10 mg with COBI (Non-pregnant adults) |
| TFV AUCtau (ng•h/mL) | 162 (153–184) | 184 (147–350) | 390 (188–461) | 197 (145–354) | 209 (158–284) | 213 (169–304) | 133 (128–720) | 335 (192–549) | 507 (221–693) | 273 (227–319) | 271 (213–329) |
| TFV Cmax (ng/mL) | 69.7 (61.0–87.7) | 91 (50–105) | 157 (92–241) | 80.4 (57.5–121.0) | 93 (51–136) | 96 (74–110) | 44 (41–219) | 101 (78–119) | 164 (107–337) | 7.9 (6.4–9.5) | 7.4 (6–8.8) |
| TFV CL/F (L/hr) | 154 (136–163) | 136 (72–170) | 64 (55–133) | 127 (71–172) | 120 (88–158) | 118 (83–148) | 188 (35–195) | 75 (46–130) | 49 (37–123) | - | - |
| TFV T1/2 (hours) | 0.25 (0.24–0.27) | 0.28 (0.23–0.53) | 0.32 (0.30–0.43) | 0.36 (0.25–0.52) | 0.35 (0.27–0.48) | 0.30 (0.27–0.44) | 0.20 (0.20–0.33) | 0.32 (0.26–0.61) | 0.31 (0.25–0.66) | 0.40 (0.36–0.43) | 0.46 (0.38–0.53) |
Summary PK reported as median (IQR).
Source:
Momper JD, Best B, Wang J, et al. Tenofovir Alafenamide Pharmacokinetics With and Without Cobicistat in Pregnancy. 22nd International AIDS Conference; July 23–27, 2018, 2018; Amsterdam, the Netherlands.
Brooks K, Pinilla M, Shapiro D, et al. Pharmacokinetics of tenofovir alafenamide 25 mg with PK boosters during pregnancy and postpartum. Oral abstract presented at 20th International Workshop on Clinical Pharmacology of HIV, Hepatitis, and Other Antiviral Drugs; 14–16 May 2019, 2019; Noordwijk, the Netherlands
Yamaha H, Yonemura T, Nemoto T et al. Pharmacokinetics of Tenofovir Alafenamide, Tenofovir and Emtricitabine following coformulated Emtricitabine/Tenofovir Alafenamide in Healthy Japanese Subjects. Clin Pharmacol Drug Dev, 2019; 8(4):511–520
Key to Acronyms: AUCtau = area under the curve over the dosing interval (i.e., 24 hours); CL/F = apparent oral clearance; Cmax = maximum plasma concentration; T1/2 = half life; TAF = tenofovir alafenamide