Table 2.
PK parameters of tenofovir and emtricitabine in plasma and tenofovir-DP and emtricitabine-TP in PBMCs during daily oral tenofovir disoproxil fumarate/emtricitabine
| Analyte | Parameter | Transwomen, n = 15, GM (90% CI) | Historical control,15n = 17, GM (90% CI) | Transwomen: historical control, GMR (90% CI) | P value |
|---|---|---|---|---|---|
| Plasma | |||||
| TFV | C max, mg/L | 0.23 (0.19–0.26) | 0.28 (0.26–0.31) | 0.80 (0.67–0.96) | 0.06 |
| C min, mg/L | 0.05 (0.04–0.05) | 0.05 (0.05–0.06) | 0.89 (0.75–1.05) | 0.26 | |
| T max, h | 1.45 (1.26–1.68) | 2.24 (1.81–2.78) | 0.65 (0.50–0.84) | 0.02 | |
| AUC0–24, mg·h/L | 2.10 (1.81–2.43) | 2.76 (2.57–2.96) | 0.76 (0.65–0.90) | 0.01 | |
| t ½, h | 16.83 (15.32–18.50) | 15.46 (12.87–18.58) | 1.09 (0.89–1.34) | 0.52 | |
| CL/F, mL/min | 1072.61 (998.72–1151.97) | 815.89 (705.03–944.17) | 1.32 (1.12–1.55) | 0.01 | |
| FTC | C max, mg/L | 1.55 (1.35–1.78) | 1.66 (1.55–1.79) | 0.93 (0.80–1.09) | 0.46 |
| C min, mg/L | 0.07 (0.06–0.08) | 0.07 (0.07–0.08) | 0.89 (0.75–1.07) | 0.31 | |
| T max, h | 1.74 (1.61–1.88) | 2.92 (2.40–3.55) | 0.60 (0.48–0.74) | 0.001 | |
| AUC0–24, mg·h/L | 9.15 (8.04–10.30) | 10.64 (10.18–11.11) | 0.86 (0.75–0.98) | 0.07 | |
| t ½, h | 6.00 (5.63–6.39) | 10.57 (10.13–11.02) | 0.57 (0.53–0.61) | <0.001 | |
| CL/F, mL/min | 364.42 (347.40–382.28) | 313.75 (281.52–349.67) | 1.16 (1.03–1.31) | 0.05 | |
| PBMCs | |||||
| TFV-DP | C avg, fmol/106 cells | 167.1 (146.6–190.5) | N/A | ||
| FTC-TP | C avg, pmol/106 cells | 15.4 (13.8–17.3) | N/A | ||
Duration of tenofovir/emtricitabine for each group was as follows: transwomen, 14 days; historical control (Blum et al.15), 7 days. P < 0.05 in bold.
C avg, geometric mean of intracellular concentration at steady-state; TFV, tenofovir; FTC, emtricitabine; TFV-DP, tenofovir-DP; FTC-TP, emtricitabine-TP.