The purpose of this study is to assess the effect of PC14586 pharmacokinetics when co administered with itraconazole in healthy participants.
PC14586 is a first-in-class, oral, small molecule p53 reactivator that is selective for the TP53 Y220C mutation. This is a Phase 1, open-label, fixed-sequence study to investigate the effect of coadministration of itraconazole on the pharmacokinetics (PK) of PC14586 (rezatapopt) in healthy male and female participants. Potential participants will be screened to assess their eligibility to enter the study within 56 days prior to the first dose administration. Participants will be admitted into the study site on Day -1 and be confined to the study site until discharge on Day 33. Participants will return to the study site for PK sample collection on Day 37 and a follow-up visit and PK sample collection on Day 42. Approximately 16 participants will be enrolled in this study.
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
OTHER
Masking
NONE
Enrollment
12
First-in-class, oral, small molecule p53 reactivator that is selective for the TP53 Y220C mutation.
Antifungal treatment that is a potent inhibitor of CYP3A4.
Fortrea
Madison, Wisconsin, United States
Characterize the Maximum Plasma Concentration (Cmax) of PC14586 when co-administered with itraconazole in healthy participants.
Determine the Cmax of PC14586 when co-administered with itraconazole in plasma.
Time frame: 6 weeks
Characterize the total drug exposure (AUC0-inf) of PC14586 when co-administered with itraconazole in healthy participants.
Determine the AUC0-inf of PC14586 when co-administered with itraconazole in plasma.
Time frame: 6 weeks
Characterize the time to peak drug concentration (Tmax) of PC14586 when co-administered with itraconazole in healthy participants.
Determine the Tmax of PC14586 when co-administered with itraconazole in plasma.
Time frame: 6 weeks
Characterize the total drug exposure from time zero to 24 hours (AUC0-24) of PC14586 when co-administered with itraconazole in healthy participants.
Determine the AUC0-24 of PC14586 when co-administered with itraconazole in plasma.
Time frame: 6 weeks
Characterize the total drug exposure from time zero to the last timepoint (AUC0-t) of PC14586 when co-administered with itraconazole in healthy participants.
Determine the AUC0-t of PC14586 when co-administered with itraconazole in plasma.
Time frame: 6 weeks
Characterize the half-life (t1/2) of PC14586 when co-administered with itraconazole in healthy participants.
Determine the t1/2 of PC14586 when co-administered with itraconazole in plasma.
Time frame: 6 weeks
Characterize the Maximum Plasma Concentration (Cmax) of PC14586 metabolites M13 and M14 when co-administered with itraconazole in healthy participants.
This platform is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional.
Determine the Cmax of PC14586 metabolites M13 and M14 when co-administered with itraconazole in plasma.
Time frame: 6 weeks
Characterize the total drug exposure (AUC0-inf) of PC14586 metabolites M13 and M14 when co-administered with itraconazole in healthy participants.
Determine the AUC0-inf of PC14586 metabolites M13 and M14 when co-administered with itraconazole in plasma.
Time frame: 6 weeks
Characterize the time to peak drug concentration (Tmax) of PC14586 metabolites M13 and M14 when co-administered with itraconazole in healthy participants.
Determine the Tmax of PC14586 metabolites M13 and M14 when co-administered with itraconazole in plasma.
Time frame: 6 weeks
Characterize the total drug exposure from time zero to 24 hours (AUC0-24) of PC14586 metabolites M13 and M14 when co-administered with itraconazole in healthy participants.
Determine the AUC0-24 of PC14586 metabolites M13 and M14 when co-administered with itraconazole in plasma.
Time frame: 6 weeks
Characterize the total drug exposure from time zero to the last timepoint (AUC0-t) of PC14586 metabolites M13 and M14 when co-administered with itraconazole in healthy participants.
Determine the AUC0-t of PC14586 metabolites M13 and M14 when co-administered with itraconazole in plasma.
Time frame: 6 weeks
Characterize the half-life (t1/2) of PC14586 metabolites M13 and M14 when co-administered with itraconazole in healthy participants.
Determine the t1/2 of PC14586 metabolites M13 and M14 when co-administered with itraconazole in plasma.
Time frame: 6 weeks
Identification of the incidence of treatment emergent adverse events (TEAE) of PC14586 when administered alone and co-administered with itraconazole in healthy participants.
Identify the incidence of TEAEs of PC14586 alone or when co-administered with itraconazole.
Time frame: 6 weeks
Identification of vital sign abnormalities after administration of PC14586 alone and when co-administered with itraconazole in healthy participants.
Identify the number of participants with abnormal vital signs.
Time frame: 6 weeks
Identification of 12-lead electrocardiogram (ECG) abnormalities after administration of PC14586 alone and when co-administered with itraconazole in healthy participants.
Identify the number of participants with abnormal ECG results.
Time frame: 6 weeks
Identification of laboratory abnormalities based on hematology and clinical chemistry after administration of PC14586 alone and when co-administered with itraconazole in healthy participants.
Identify the number of participants with an incidence of laboratory abnormalities in test results.
Time frame: 6 weeks