This relative bioavailability (RBA) study will be conducted to investigate whether there is a potential pharmacokinetic effect when paediatric DTG and F/TAF are taken together as dispersible formulations. This study will be performed in healthy volunteers instead of HIV-infected patients.
This relative bioavailability (RBA) study will be conducted to investigate whether there is a potential pharmacokinetic effect when paediatric DT DTG (30 mg dose) and F/TAF TOS (180/22.5 mg dose) are taken together. For this purpose, Gilead's F/TAF 60/7.5 mg TOS tablets and ViiV Healthcare's DTG 5 mg tablets will be used. Given the very low plasma concentration of TAF (very probably mainly under the detection limit) with a single dose of 7.5 mg in adults, 3 tablets of F/TAF 60/7.5 mg (180/22.5 mg) will be given, which is similar to the adult dose. It was considered to keep the ratio between DTG and F/TAF similar to the to be developed paediatric fixed dose combination tablet, which would have resulted in a DTG dose of 60mg DTG DT. But because DTG shows nonlinear kinetics above a dose of 50 mg FCT (3), it was decided to use DTG 30 mg DT tablets, which is bioequivalent to adult dose of 50 mg FCT. For all compounds, a dose similar to the adult dose will be given.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
OTHER
Masking
NONE
Enrollment
16
DTG 5mg dispersible tablet
60/7.5 mg TOS emtricitabine/TAF
RTCCS Radboudumc
Nijmegen, Netherlands
The relative bioavailability of TAF and TFV
The relative bioavailability of TAF and TFV after a single-dose F/TAF 180/22.5 mg as 3X60/7.5 mg TOS (reference TAF) compared to TAF and TFV after a single-dose F/TAF 180/22.5 mg as 3X60/7.5 mg TOS in combination with a single dose of DTG 30 mg as 6X5 mg DT tablets (test).
Time frame: 17 days
The relative bioavailability of FTC
The relative bioavailability of FTC after a single-dose F/TAF 180/22.5 mg as 3X60/7.5 mg TOS (reference FTC) compared to FTC after a single-dose F/TAF 180/22.5 mg as 3X60/7.5 mg TOS in combination with a single dose of DTG 30 mg as 6X5 mg DT tablets (test).
Time frame: 17 days
The relative bioavailability of DTG
The relative bioavailability of DTG after a single-dose DTG 30 mg as 6X 5 mg DT tablets (reference DTG) compared to DTG after a single-dose F/TAF 180/22.5 mg as 3X60/7.5 mg TOS in combination with a single dose of DTG 30 mg as 6X5 mg DT tablets (test).
Time frame: 17 days
The relative bioavailability of the potential interaction and pharmacokinetics
The relative bioavailability of the potential interaction, the pharmacokinetics (AUC0-∞, Cmax, Tmax, T1⁄2) of DTG, FTC, TAF and TFV will be obtained and the geometric mean ratios of the AUC0-tlast (TAF), AUC0-∞ (DTG, FTC and TFV only), Cmax , and Cmin (DTG, FTC and TFV only) of the test versus reference treatment
Time frame: 17 days
Adverse events
Adverse events will be described and compared (including clinically relevant laboratory abnormalities) of the treatments with F/TAF and DTG once daily.
Time frame: 17 days
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