The present study is designed to determine the effect of valproic acid (VAL), a UGT2B7 inhibiting drug, on the pharmacokinetics (PK) of estetrol (E4)
In the present study, E4/DRSP will be administered alone (Treatment A) and in combination with VAL (Treatment B) following two sequences A-B or B-A.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
PREVENTION
Masking
NONE
Enrollment
24
Quotient Sciences
Ruddington, Nottingham, United Kingdom
Maximum concentration (Cmax) of E4
PK sampling
Time frame: 0-168 hr post E4/DRSP dose in both periods 1 and 2 of the two sequences A-B and B-A
Area under the plasma concentration versus time curve from time 0 to the last determined concentration (AUC0-tdlc) of E4
PK sampling
Time frame: 0-168 hr post E4/DRSP dose in both periods 1 and 2 of the two sequences A-B and B-A
Area under the plasma concentration versus time curve from time 0 to infiny (AUC0-inf) of E4
PK sampling
Time frame: 0-168 hr post E4/DRSP dose in both periods 1 and 2 of the two sequences A-B and B-A
Number of subjects with adverse events as a measure of safety and tolerability
Time frame: The total study duration (between 50 and 86 days)
Cmax of DRSP
PK sampling
Time frame: 0-168 hr post E4/DRSP dose in both periods 1 and 2 of the two sequences A-B and B-A
Cmax of E4-glucuronide metabolites
PK sampling
Time frame: 0-168 hr post E4/DRSP dose in both periods 1 and 2 of the two sequences A-B and B-A
AUC0-tdlc of DRSP
PK sampling
Time frame: 0-168 hr post E4/DRSP dose in both periods 1 and 2 of the two sequences A-B and B-A
AUC0-tdlc of E4-glucuronide metabolites
PK sampling
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Time frame: 0-168 hr post E4/DRSP dose in both periods 1 and 2 of the two sequences A-B and B-A
AUC0-inf of DRSP
PK sampling
Time frame: 0-168 hr post E4/DRSP dose in both periods 1 and 2 of the two sequences A-B and B-A
AUC0-inf of E4-glucuronide metabolites
PK sampling
Time frame: 0-168 hr post E4/DRSP dose in both periods 1 and 2 of the two sequences A-B and B-A