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. Author manuscript; available in PMC: 2019 Jun 1.
Published in final edited form as: J Acquir Immune Defic Syndr. 2018 Jun 1;78(2):175–182. doi: 10.1097/QAI.0000000000001655

Table 1.

Pharmacokinetics of Sampled Compartments by Dosing Route

Dosing Route Compartment Analyte (units) LLOQ #Quantifiable
Samples		 Concentration,
median (IQR1)1
Vaginal Application Plasma TVF† (ng/mL) 0.31 10/14 0.58(BLQ§, 1.3)
PBMCs TFV-DP‡ (fmol/106 cells) 50 fmol/sample 0/14 BLQ (BLQ, BLQ)
Vaginal fluid TVF(ng/swab) 0.625 14/14 7138 (1370, 24375)
CVL TVF (ng/mL) 5 13/14 4485 (2410, 48900)
Vaginal tissue2,3 TVF (ng/mg) 0.0046 12/13 8.5 (1.0, 44.8)
TFV-DP (fmol/mg) 4.61 12/13 166 (37, 2377)
Endocervical cells TFV-DP (fmol/106 cells) 50 fmol/sample 8/14 126.3 (BLQ, 421.7)
Rectal fluid TFV (ng/sponge) 1.25 ng/sponge 10/14 4.4 (BLQ, 7.1)
Rectal tissue2,4 TVF (ng/mg) 0.0270 1/13 0.2
TFV-DP (fmol/mg) 27.03 2/13 59.8; 76.5
Rectal Application Plasma TVF (ng/mL) 0.31 10/14 0.82 (BLQ, 1.2)
PBMCs TFV-DP (fmol/106 cells) 50 fmol/sample 1/14 48.32
Vaginal fluid TVF (ng/swab) 0.625 9/14 1.1 (BLQ, 2.8)
CVL TVF (ng/mL) 5 3/14 9.2; 8.5; 43
Vaginal tissue2,3 TVF (ng/mg) 0.0046 6/14 BLQ (BLQ, 0.16)
TFV-DP (fmol/mg) 4.61 3/14 17.3; 87.6; 77.1
Endocervical cells TFV-DP (fmol/106 cells) 50 fmol/sample 0/14 BLQ (BLQ, BLQ)
Rectal fluid TVF (ng/sponge) 1.25 ng/sponge 12/14 202 (55, 2205)
Rectal tissue2,4 TVF (ng/mg) 0.0270 12/14 3.0 (0.7, 10.9)
TFV-DP (fmol/mg) 27.03 10/14 196 (BLQ, 550)

Notes:

*

Inter-Quartile Range;

†

Tenofovir;

§

Below the Limit of Quantitation;

‡

Tenofovir Diphosphate

1

Values represent median of all collected samples followed, in parentheses, by the interquartile range (IQR). When three or fewer samples were quantifiable, all values are shown without parentheses.

2

The overall LLOQ of TFV was 0.05 ng/mg tissue and the overall LLOQ of TFV-DP was 50 fmol/mg of tissue. The tissue-specific LLOQ of TFV and of TFV-DP were calculated by dividing the overall LLOQ by the median weight of the biopsy samples from each anatomic location. As the median tissue weights obtained after each dosing route were similar, the LLOQs for vaginal and rectal tissue are based on the average of the tissue weights obtained after each dosing route.

3

Mean duration of time between the final dose at the end of each product-use period and vaginal tissue collection was 21.6 h (SD 2.6 h).

4

Mean duration of time between the final dose at the end of each product-use period and rectal tissue collection was 20.4 h (SD 2.7 h)