Abstract
Background
This study evaluated the ethinyl estradiol (EE) and levonorgestrel (LNG) pharmacokinetic
profiles of AG200-15, a transdermal contraceptive delivery system, compared with a
combination oral contraceptive (COC) containing EE 35 mcg and norgestimate 250 mcg.
Study design
A Phase 1, open-label, single-center study in 36 healthy women was conducted over
three cycles with a randomized crossover design. After a run-in cycle of 21 days on
and 7 days off with AG200-15, participants were randomized to receive one of two treatments:
a 21/7-day cycle of AG200-15 either followed or preceded by one cycle of the COC.
This trial is registered on ClinicalTrials.gov under the identifier NCT01243580.
Results
During the third week of AG200-15 use, mean (��standard deviation) maximum serum concentration
(Cmax), area under the curve0���168 h and steady-state concentration (Css48���168 h) for EE were 51.3��17.3 pg/mL, 6.26��2.46 ng h/mL and 35.7��14.5 pg/mL, respectively;
for LNG, the corresponding values were 2400��1140 pg/mL, 317��159 ng h/mL and 1847��930
pg/mL, respectively. The AG200-15 EE Cmax was approximately 60% lower and the EE Css was 15%���20% lower than those obtained with the COC. The calculated daily dose of
AG200-15 was equivalent to a 30-mcg EE COC. The most common adverse events (AEs; >10%)
in the AG200-15 group were headache, nausea and application-site irritation. All drug-related
AEs were mild, and no serious AEs were reported.
Conclusions
EE and LNG daily exposure during AG200-15 treatment was within the range reported
for a low-dose COC. The daily EE dose with AG 200-15 was equivalent to a 30-mcg COC
and was safe and well tolerated.
Keywords
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Article info
Publication history
Published online: December 02, 2011
Accepted:
October 14,
2011
Received in revised form:
October 4,
2011
Received:
June 21,
2011
Footnotes
���This study was funded by Agile Therapeutics, Inc.
Identification
Copyright
© 2012 Elsevier Inc. Published by Elsevier Inc. All rights reserved.
