Table 3.
Tenofovir and emtricitabine pharmacokinetic parameters in plasma and peripheral blood mononuclear cells
| Biomatrix and Analyte | PK Paramater | Single Dose Phase (SDP) (Median, Range) (n = 24) |
After First Dose MDP (Median, Range) (n = 75) |
Multiple-Dose Phase (MDP) Values after 14 Daily Doses Median (Range) |
|||||
|---|---|---|---|---|---|---|---|---|---|
| F/TAF 200/25 mg (N = 12) | F/TDF 200/300 (N = 12) | F/TAF 200/10 mg (N=26) | F/TAF 200/25 mg (N = 24) | F/TDF 200/300 mg (N = 25) | F/TAF 200/10 mg (N=26) | F/TAF 200/25 mg (N = 24) | F/TDF 200/300 mg (N = 25) | ||
| Plasma TFV | AUC0-24 (h•ng/mL) | 77 (39, 224) | 2260 (1281, 2852) | 31 (22, 56) | 77 (50.9, 286.2) | 1959 (1432, 2906) | 101 (21, 167) | 294 (178, 671) | 2943 (1371, 4014) |
| Cmax (ng/mL) | 6.2 (4, 17) | 436 (272, 625) | 2.4 (1, 4) | 5.8 (4, 28) | 306 (158, 499) | 6 (2, 11) | 17 (11, 39) | 357 (176, 627) | |
| C24h (ng/mL) | 2.3 (1, 7) | 37.2 (22, 59) | 1 (1, 2) | 2.7 (1, 9) | 37.3 (25, 61) | 3.3 (1, 6) | 9.6 (5, 23) | 56 (26, 76) | |
| Tmax (hrs) | 1.5 (1, 2) | 1 (1, 2) | 2 (1, 4) | 2 (1, 4) | 1 (1, 2) | 1 (1, 4) | 1 (1, 4) | 1 (1, 2) | |
| PBMC TFV-DP | AUC0-24 (h•fmol/106 cells) | 3,504 (1565, 10,009) | 430 (180, 842) | 1389 (681, 2977) | 3781 (2058, 8288) | 341 (186, 1505) | 6,078 (961, 11604) | 15,215 (8700, 42,689) | 2,498 (562, 3993) |
| Cmax (fmol/106 cells) | 184 (80, 741) | 33 (13, 60) | 74 (43, 149) | 195 (117, 440) | 23 (9, 129) | 314 (50, 18029) | 1021 (444, 5726) | 139 (26, 1000) | |
| C24h (fmol/106 cells) | 118 (50, 397) | 26 (10, 39) | 52.3 (12, 149) | 152 (1, 350) | 16.5 (8, 41) | 201 (30, 395) | 523 (273, 931) | 87 (25, 141) | |
| Tmax (hrs) | 4 (2, 8) | 24 (2, 72) | 4 (2, 24) | 8 (2, 24) | 24 (1, 24) | 4 (1, 72) | 2 (1, 48) | 4 (0, 48) | |
| Plasma FTC | AUC0-24 (h•fmol/106 cells) | 11172 (8943, 22663) | 12464 (9410, 16136) | 10877 (7826, 20993) | 13215 (9601, 25861) | 12317 (9030, 18349) | 13824 (8232, 19836) | 15048 (11017, 22847) | 13238 (8280, 20388) |
| Cmax (fmol/106 cells) | 2165 (1750, 3950) | 2105 (1270, 3370) | 2270 (1370, 3440) | 2130 (1510, 4020) | 2060 (1300, 3740) | 2480 (1140, 4050) | 2950 (1580, 4240) | 2190 (1110, 3670) | |
| C24h (ng/mL) | 34.0 (15, 59) | 40.5 (24, 65) | 38.5 (18, 59) | 40.1 (25, 86) | 39.7 (22, 58) | 68.2 (23, 106) | 61 (39, 174) | 69.4 (37, 144) | |
| Tmax (hrs) | 1 (1, 2) | 1 (1, 2) | 1 (1, 2) | 1.5 (1, 4) | 2 (1, 4) | 1 (1, 2) | 1 (1, 2) | 2 (1, 4) | |
| PBMC FTC-TP | AUC0-24 (h•fmol/106 cells) | 67621 (47260, 87037) | 59845 (29354, 79636) | 52718 (29589, 97269) | 56535 (38445, 80424) | 54894 (28850, 98685) | 86484 (26672, 189710) | 80887 (57843, 173622) | 78228 (49154, 187278) |
| Cmax (fmol/106 cells) | 4265 (2475, 6434) | 3595 (1750, 5339) | 3120 (1705, 9464) | 3236 (2187, 5483) | 3403 (1634, 6884) | 5116 (2061, 107133) | 5149 (3196, 26924) | 4516 (2806, 23788) | |
| C24h (fmol/106 cells) | 1662 (1029, 2038) | 2055 (963, 2339) | 1475 (616, 3170) | 1518 (24, 2634) | 1448 (745, 3508) | 2219 (994, 4909) | 2060 (1313, 3940) | 2145 (1208, 4813) | |
| Tmax (hrs) | 4 (2, 8) | 4 (2, 8) | 4 (2, 8) | 8 (2, 8) | 8 (1, 8) | 4 (0, 72) | 2 (1, 8) | 4 (1, 8) | |