Phase 1
Completed N=13
A Study to Evaluate the Effect of Itraconazole on the Pharmacokinetics of PF-04958242 in Healthy Subjects
Healthy
Source: ClinicalTrials.gov NCT02341482 ↗
Enrolled (actual)
13
Serious AEs
0.0%
Results posted
Jun 2016
Primary outcomePrimary: Area Under the Concentration-Time Profile From Time 0 to Time Tau, the Dosing Interval, Where Tau = 12 Hours (AUCtau) of PF-04958242 — 4242; 4073 picogram*hours per milliliter pg*h/mL
Summary
The purpose of the current study is to characterize the pharmacokinetic (PK) profile of PF 04958242 when co administered with a strong cytochrome P450 3A4 (CYP3A4) inhibitor.
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Area Under the Concentration-Time Profile From Time 0 to Time Tau, the Dosing Interval, Where Tau = 12 Hours (AUCtau) of PF-04958242 |
4242; 4073 | — |
| PRIMARY Maximum Observed Plasma Concentration (Cmax) of PF-04958242 |
553.4; 541.6 | — |
| SECONDARY Time for Cmax (Tmax) of PF-04958242 |
1.50; 1.50 | — |
| SECONDARY Lowest Concentration Observed During the Dosing Interval (Cmin) of PF-04958242 |
256.5; 238.2 | — |
| SECONDARY Predose Concentration (Ctrough) of PF-04958242 |
289.3; 255.0 | — |
| SECONDARY Apparent Oral Clearance (CL/F) of PF-04958242 |
98.25; 102.3 | — |
| SECONDARY Number of Participants With Abnormal Clinical Laboratory Measurements |
1 | — |
| SECONDARY Number of Participants With Vital Signs Data Meeting Criteria of Potential Clinical Concern |
0; 0; 0; 0; 2; 1 | — |
| SECONDARY Number of Participants With Electrocardiogram Data Meeting Criteria of Potential Clinical Concern |
— | — |
| SECONDARY Number of Participants With Significant Change in Neurological Examination From Previous Examination |
— | — |
| SECONDARY Number of Participants With Significant Change in Physical Examination From Previous Examination |
— | — |
| SECONDARY Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs) |
2; 7; 1; 0; 0; 0 | — |
| SECONDARY Number of Participants With Positive Response to Columbia-Suicide Severity Rating Scale (C-SSRS) |
— | — |
Eligibility Criteria
Key Inclusion Criteria
-Healthy male subjects and female subjects of non childbearing with a Body Mass Index (BMI) of 17.5 to 30.5 kg/m2; and a total body weight >55 kg (121 lbs).
Key Exclusion Criteria
- Subjects with ANY of the following abnormalities in clinical laboratory tests at screening, as assessed by the study specific laboratory and confirmed by a single repeat, if deemed necessary:
- Aspartate transaminase (AST)/serum glutamic oxaloacetic transminase (SGOT) or alanine transaminase (ALT)/serum glutamic pyruvic transminase (SGPT) >=1 x upper limit of normal (ULN);
- Total bilirubin >=1.5 x ULN; subjects with a history of Gilbert's syndrome may have a direct bilirubin measured and would be eligible for this study provided the direct bilirubin is <= ULN.
- Subjects with epilepsy, or history of epilepsy, or conditions that lower seizure threshold, seizures of any etiology (including substance or drug withdrawal), or who have increased risk of seizures as evidenced by self reported history of electroencephalogram (EEG) with epileptiform activity. Subjects with a history of childhood seizures and history of head trauma with loss of consciousness requiring hospitalization overnight will be excluded as well.
- Subjects who had a history of allergy or intolerance to azole antifungal drugs.
NOTE: Other protocol defined Inclusion/Exclusion criteria may apply
Data sourced from ClinicalTrials.gov (NCT02341482). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.