This study is designed to assess the pharmacokinetics (PK), safety, and tolerability of Ganfeborole and Microgynon, an oral contraceptive containing ethinylestradiol (EE) and levonorgestrel (LNG), when Microgynon is administered alone and in combination with Ganfeborole in healthy female participants of non-childbearing potential.
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
TREATMENT
Masking
NONE
Enrollment
28
Participants receive Ganfeborole orally.
Participants receive Microgynon orally.
Area under the plasma concentration-time curve (AUC(0-tau)) over 24 hours of EE and LNG, after repeat dose, alone and in the presence of Ganfeborole on Day 10
Time frame: On Day 10 at 30 minutes pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, and 24 hours post-dose
AUC(0-tau) over 24 hours of EE and LNG, after repeat dose, alone and in the presence of Ganfeborole on Day 24
Time frame: On Day 24 at 30 minutes pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, and 24 hours post-dose
Maximum observed concentration (Cmax) of EE and LNG, after repeat dose, alone and in the presence of Ganfeborole on Day 10
Time frame: On Day 10, at 30 minutes pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, and 24 hours post-dose
Cmax of EE and LNG, after repeat dose, alone and in the presence of Ganfeborole on Day 24
Time frame: On Day 24, at 30 minutes pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, and 24 hours post-dose
AUC(0-tau) over 24 hours of Ganfeborole in the presence of EE and LNG
Time frame: On Day 24, at 30 minutes pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, and 24 hours post-dose
Cmax of Ganfeborole in the presence of EE and LNG
Time frame: On Days 16, 22 and 23, at 30 minutes pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, and 24 hours post-dose for each day, and on Days 24 and 25, at 30 minutes pre-dose and 24 hours post-dose for each day
Time of maximum observed concentration (Tmax) of Ganfeborole in the presence of EE and LNG
Time frame: On Days 16, 22 and 23, at 30 minutes pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, and 24 hours post-dose for each day, and on Days 24 and 25, at 30 minutes pre-dose and at 24 hours post-dose for each day
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Plasma concentration over 24 hours (Ctau) of Ganfeborole in the presence of EE and LNG
Time frame: On Days 16, 22 and 23, at 30 minutes pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, and 24 hours post-dose for each day, and on Days 24 and 25, at 30 minutes pre-dose and 24 hours post-dose for each day
Tmax of EE and LNG alone and in the presence of Ganfeborole
Time frame: On Days 8, 9, 22 and 23, at 30 minutes pre-dose and 24 hours post-dose for each day, and on Days 10, 24 and 25 at 30 minutes pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, and 24 hours post-dose for each day
Ctau over 24 hours of EE and LNG alone and in the presence of Ganfeborole
Time frame: On Days 8, 9, 22 and 23, at 30 minutes pre-dose and 24 hours post-dose for each day, and on Days 10, 24 and 25 at 30 minutes pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, and 24 hours post-dose for each day
Number of participants with serious adverse events (SAEs)
An SAE is defined as any untoward medical occurrence that, at any dose, results in death, is life threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect in the offspring of a study participant, or other situations as per investigator's opinion.
Time frame: From Day 1 to Day 25
Number of participants with adverse events (AEs) of grade 3 severity or higher
An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study intervention, whether or not considered related to the study intervention. Grade 3 = severe, Grade 4 = life-threatening, Grade 5= death.
Time frame: From Day 1 to Day 25
Number of participants with any AEs related to study interventions, overall and by each type of treatment (Microgynon and Ganfeborole)
Time frame: From Day 1 to Day 25
Number of participants withdrawn from the. treatment/study due to AEs
Time frame: From Day 1 to Day 25
Number of participants with electrocardiogram (ECG) values of potential clinical importance (PCI)
Time frame: At Day 11 and Day 25
Number of participants with clinical chemistry laboratory values of PCI
Time frame: At Days 1, 7, 11, 21 and 25
Number of participants with hematology laboratory values of PCI
Time frame: At Days 1, 7, 11, 21 and 25
Number of participants with vital signs parameters of systolic blood pressure (SBP), diastolic BP (DBP) and heart rate (HR) of PCI
Time frame: At Days 1, 7, 11, 21 and 25
Change in sex hormone binding globulin (SHBG) levels following repeat-dose administration of Microgynon
Time frame: At Screening, Day 10 and Day 24