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The study aims to understand, using radiolabelled PF-06463922, how this compound is modified by the body once it is absorbed. The study also aims to understand how much of the compound is broken down and how much leaves the body unchanged.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Treatment | Experimental | Radiolabeled PF-06463922 in healthy volunteers |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| [14C] PF-06463922 | Drug | Single oral dose of 100mg PF-06463922 + [14C] PF-06463922 |
|
| Measure | Description | Time Frame |
|---|---|---|
| Mass Balance | Mass balance: Cumulative recovery (%) of total radioactivity in urine and feces. | 14 days |
| Metabolic profiling / metabolite identification in plasma, urine, and fecal samples | 14 days | |
| AUCinf | Area Under the Curve From Time Zero to Extrapolated Infinite Time | 14 days |
| AUClast | Area under the plasma concentration time profile from time 0 to the time of the last quantifiable concentration (Clast) | 14 days |
| kel | Elimination rate constant | 14 days |
| Cmax | Maximum observed plasma concentration | 14 days |
| Tmax | Time for Cmax | 14 days |
| t1/2 | Terminal elimination half life | 14 days |
| CL/F | Apparent oral clearance | 14 days |
| Measure | Description | Time Frame |
|---|---|---|
| AUC (0-24) | Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - 24). It is obtained from AUC (0 - t) plus AUC (t - 24). | 14 days |
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Inclusion Criteria:
Exclusion Criteria:
Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurologic, or allergic disease (including drug allergies, but excluding untreated, asymptomatic, seasonal allergies at the time of dosing).
Any condition possibly affecting drug absorption (eg, gastrectomy).
A positive urine drug screen.
History of regular alcohol consumption exceeding 7 drinks/week (1 drink = 5 ounces [150 mL] of wine or 12 ounces [360 mL] of beer or 1.5 ounces [45 mL] of hard liquor) within 6 months of Screening.
Treatment with an investigational drug within 30 days (or as determined by the local requirement) or 5 half-lives preceding the first dose of study medication (whichever is longer).
Screening supine blood pressure 140 mm Hg (systolic) or 90 mm Hg (diastolic), following at least 5 minutes of supine rest. If blood pressure is 140 mm Hg (systolic) or 90 mm Hg (diastolic), the blood pressure should be repeated two more times and the average of the three blood pressure values should be used to determine the subject's eligibility.
Screening supine 12-lead ECG demonstrating QTcF (time from ECG Q wave to the end of the T wave corresponding to electrical systole [QT] corrected for the heart rate using the Fredericia's formula) >450 msec or a QRS interval (time from ECG Q wave to the end of the S wave corresponding to ventricle depolarization) >120 msec. If QTcF exceeds 450 msec, or QRS exceeds 120 msec, the ECG should be repeated two more times and the average of the three QTcF or QRS values should be used to determine the subject's eligibility.
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:
Use of prescription or nonprescription drugs and dietary supplements within 7 days or 5 half lives (whichever is longer) prior to the first dose of study medication. As an exception, acetaminophen/paracetamol may be used at doses of 1 g/day. Limited use of non-prescription medications that are not believed to affect subject safety or the overall results of the study may be permitted on a case-by-case basis following approval by the sponsor.
Herbal supplements and hormone replacement therapy must be discontinued at least 28 days prior to the first dose of study medication.
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| Name | Affiliation | Role |
|---|---|---|
| Pfizer CT.gov Call Center | Pfizer | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Covance Clinical Research Unit Inc. | Madison | Wisconsin | 53704 | United States |
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| ID | Term |
|---|---|
| C000590786 | lorlatinib |
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| Ae | Total amount of unchanged drug excreted in the urine from time 0 to discharge day | 14 days |
| Ae% | Total amount of unchanged drug excreted in the urine from time 0 to infinity expressed as percent of dose | 14 days |
| Clr | Renal Clearance | 14 days |
| Crbc | Total radioactivity in RBCs | 14 days |
| Vz/F | Apparent volume of distribution following oral administration | 14 days |