TABLE 5

Summary of key pharmacokinetic parameter values for TDF-FTC and TDF-FTC-MVC pod-IVRs

Drug(s) and sample typeMedian (SD)a
Tmax (days)Cmax (μg/ml)Cmax/D (μg/ml/mg)AUC0–t (day·μg/ml)bAUC0–∞/D (day·μg/ml/mg)Vz (ml)CL (ml/day)
Vaginal fluid
    TDF-FTC IVR
        TFV14 (7.2)1.2E+3 (3.1)1.3E+2 (5.7)1.5E+4 (0.82)1.7E+3 (1.8)0.10 (0.76)0.62 (0.78)
        FTC14 (10)3.0E+4 (12)4.4E+2 (16)3.8E+5 (8.7)5.5E+3 (12)0.083 (0.050)0.18 (0.09)
    TDF-FTC-MVC IVR
        TFV11 (9.5)1.9E+2 (0.62)16 (13)2.5E+3 (1.0)2.2E+2 (2.2)0.79 (0.64)4.7 (3.6)
        FTC7.0 (9.5)1.2E+4 (2.7)4.5E+2 (8.9)1.2E+5 (2.1)4.6E+3 (6.2)0.11 (0.092)0.25 (0.17)
        MVC18 (12)1.8E+3 (3.1)79 (120)2.0E+4 (1.8)8.7E+2 (6.8)1.1 (1.1)1.2 (1.3)
Vaginal tissue
    TDF-FTC IVR
        TFV7.0 (7.7)45 (74)6.6 (14)6.9E+2 (6.5)69 (130)8.2 (7.3)15 (13)
        FTC7.0 (7.7)6.2E+2 (8.2)8.6 (11)9.2E+3 (10)1.4E+2 (1.4)16 (18)7.7 (6.2)
    TDF-FTC-MVC IVR
        TFV22 (7.7)18 (6.6)1.6 (1.7)2.0E+2 (0.61)19 (17)30 (14)52 (22)
        FTC7.0 (6.1)1.7E+2 (2.4)6.1 (8.3)2.9E+3 (3.2)86 (110)19 (6)12 (6)
        MVC15 (8.2)27 (24)1.1 (0.92)3.2E+2 (2.8)14 (10)71 (20)72 (33)
  • a Tmax, time to Cmax; D, dose; AUC, area under the concentration-time curve; AUC0–t, AUC from the time of dosing to the time of the last observation; Vz, volume of distribution based on the terminal phase; CL, clearance.

  • b The difference between AUC0–t and AUC0–∞ was less than 1%.