Healthy Volunteers, Pharmacokinetics of Ethinyl Estradiol and Norethindrone, Pharmacokinetics of Isavuconazole
Conditions
Keywords
isavuconazole, ethinyl estradiol, norethindrone, contraceptive, Healthy Volunteers, BAL8557, BAL4815
Brief summary
The purpose of this study is to assess the effect of multiple doses of isavuconazole on the pharmacokinetics (PK) of a single dose of contraceptive in healthy post-menopausal women.
Interventions
DRUGisavuconazole
oral
DRUGOral Contraceptive (ethinyl estradiol / norethindrone)
contraceptive pill consisting of ethinyl estradiol and norethindrone
Sponsors
Basilea Pharmaceutica International Ltd
Astellas Pharma Global Development, Inc.
Study design
Allocation
NA
Intervention model
SINGLE_GROUP
Masking
NONE
Eligibility
Sex/Gender
FEMALE
Age
50 Years to 65 Years
Healthy volunteers
Yes
Inclusion criteria
* The subject has a body weight of at least 45 kg and has a body mass index (BMI) of 18 to 32 kg/m2, inclusive * Results for aspartate aminotransferase (AST), alanine aminotransferase (ALT), and total bilirubim must not be above upper limit of normal range * The subject must be postmenopausal, defined as at least 2 years since the last regular menstrual cycle and have follicle stimulating hormone (FSH) \> 30 IU/L
Exclusion criteria
* The subject has had treatment with hormone replacement therapy within 3 months prior to Day -1 * The subject has a history of adverse events with taking oral contraceptives or hormone replacement therapy * The subject has a history of unexplained syncope, cardiac arrest, unexplained cardiac arrhythmia or torsade de pointes, structural heart disease, or family history of Long QT syndrome (suggested by sudden death of a close relative at a young age due to possible or probable cardiac causes) * The subject has a positive result for hepatitis C antibodies or hepatitis B surface antigen at Screening or is known to be positive for human immunodeficiency virus (HIV) * The subject has a known or suspected allergy to any of the components of the trial products or the azole class of compounds, or a history of multiple and/or severe allergies to drugs or foods (as judged by the investigator), or a history of severe anaphylactic reactions * The subject is a smoker (any use of tobacco or nicotine containing products) within 6 months prior to Screening * The subject has had treatment with prescription drugs or complementary and alternative medicines within 14 days prior to Day -1, or over-the-counter medications within 1 week prior to Day -1, with the exception of acetaminophen up to 2 g/day * The subject has a recent history (within the last 2 years) of drug or alcohol abuse, as defined by the investigator, or a positive drug and/or alcohol screen
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Pharmacokinetic (PK) variables for ethinyl estradiol and norethindrone (in plasma): AUCinf , AUClast, and Cmax | For Days 1 and 13: predose and 12 times post dose; for Days 2, 3, 4, 5, 14, 15, 16, and 17: one time each day | AUC from time 0 extrapolated to infinity (AUCinf), Area under the curve (AUC) from time of dosing to last quantifiable concentration (AUClast ), and maximum concentration (Cmax) |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| PK variable for ethinyl estradiol and norethindrone (in plasma): tmax , t1/2 , Vz /F, and CL/F | For Days 1 and 13: pre-dose and 12 times post dose; for Days 2, 3, 4, 5, 14, 15, 16, and 17: one time each day | Time to attain Cmax (tmax) , apparent terminal elimination half-life (t1/2 ), apparent volume of distribution (Vz /F), apparent body clearance after oral dosing (CL/F) |
| PK variable for isavuconazole (in plasma): Ctrough | For Day 11: predose; for Days 12 and 13: predose and 12 times post dose; for Day 14 and 15: predose; and for Day 16: predose and 24 hours post dose | trough concentration (Ctrough) |
| PK variable for isavuconazole (in plasma): AUCtau, Cmax, and tmax | For Days 12 and 13: predose and 12 times post dose | Area under the concentration-time curve during the time interval between consecutive dosing (AUCtau) |
| Safety assessed by recording adverse events, laboratory assessments, vital signs, electrocardiograms (ECGs) | Day 1 through Day 24 ± 2 days | — |
Countries
United States
Outcome results
None listed