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| ID | Type | Description | Link |
|---|---|---|---|
| 2016-002386-57 | EudraCT Number | ||
| ITRACONAZOLE DDI STUDY | Other Identifier | Alias Study Number |
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The purpose of this study is to estimate the effect of itraconazole on the single dose pharmacokinetics of PF-06463922 in healthy volunteers in the fasted state.
This will be a Phase 1, open-label, 2-period, fixed-sequence, crossover study to investigate the effect of the strong CYP3A inhibitor itraconazole on PF-06463922 PK in approximately 16 healthy volunteers. The study will consist of potentially up to 6 treatments: single dose of PF-06463922 50, 75 or 100 mg and PF-06463922 50, 75 or 100 mg in combination with multiple dose itraconazole.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Cohort 1 | Experimental | All subjects in this cohort will receive the same dose of PF-06463922 in both periods. Subjects will receive PF-06463922 Alone in Period 1 followed by PF-06463922 with Itraconazole in Period 2. |
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| Cohort 2 | Experimental | All subjects in this cohort will receive the same dose of PF-06463922 in both periods. Subjects will receive PF-06463922 Alone in Period 1 followed by PF-06463922 with Itraconazole in Period 2. |
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| Cohort 3 | Experimental | All subjects in this cohort will receive the same dose of PF-06463922 in both periods. Subjects will receive PF-06463922 Alone in Period 1 followed by PF-06463922 with Itraconazole in Period 2. |
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| Cohort 4 | Experimental | All subjects in this cohort will receive the same dose of PF-06463922 in both periods. Subjects will receive the highest safe dose (mg) of PF-06463922 as a single-dose Alone in Period 1 followed by PF-06463922 with Itraconazole in Period 2. |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| PF-06463922 | Drug | Single oral dose of PF-06463922 50 mg on Day 1 of Period 1 and Day 5 of Period 2 |
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| Measure | Description | Time Frame |
|---|---|---|
| AUCinf for PF-06463922 | Area under the plasma concentration-time profile from time zero extrapolated to infinite time | PF-06463922 pre-dose, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and up to 168 hours post-dose. |
| Cmax for PF-06463922 | Maximum plasma concentration | PF-06463922 pre-dose, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and up to 168 hours post-dose. |
| Measure | Description | Time Frame |
|---|---|---|
| AUClast for PF-06463922 | Area under the plasma concentration-time profile from time zero to the time of the last quantifiable concentration (Clast) | PF-06463922 pre-dose, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and up to 168 hours post-dose. |
| Tmax for PF-06463922 |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Pfizer CT.gov Call Center | Pfizer | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Pfizer Clinical Research Unit | Brussels | B-1070 | Belgium |
| PubMed Identifier | Type | Citation | Retractions |
|---|---|---|---|
| 31728714 | Derived | Patel M, Chen J, McGrory S, O'Gorman M, Nepal S, Ginman K, Pithavala YK. The effect of itraconazole on the pharmacokinetics of lorlatinib: results of a phase I, open-label, crossover study in healthy participants. Invest New Drugs. 2020 Feb;38(1):131-139. doi: 10.1007/s10637-019-00872-7. Epub 2019 Nov 14. |
| Label | URL |
|---|---|
| To obtain contact information for a study center near you, click here. | View source |
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| ID | Term |
|---|---|
| C000590786 | lorlatinib |
| D017964 | Itraconazole |
| ID | Term |
|---|---|
| D014230 | Triazoles |
| D001393 | Azoles |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D006571 | Heterocyclic Compounds |
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| PF-06463922 | Drug | Single oral dose of PF-06463922 75 mg on Day 1 of Period 1 and Day 5 of Period 2 |
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| PF-06463922 | Drug | Single oral dose of PF-06463922 100 mg on Day 1 of Period 1 and Day 5 of Period 2 |
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| PF-06463922 | Drug | Highest safe single oral dose (mg) of PF-06463922 identified in the previous cohorts will be administered on Day 1 of Period 1 and Day 5 of Period 2 |
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| Itraconazole | Drug | 200 mg oral dose of itraconazole on Days 1 to 11 during Period 2 |
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Time to Cmax |
| PF-06463922 pre-dose, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and upto 168 hours post-dose. |
| t1/2 for PF-06463922 | Terminal plasma elimination half-life | PF-06463922 pre-dose, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and up to 168 hours post-dose. |
| CL/F for PF-06463922 | Apparent clearance | PF-06463922 pre-dose, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and up to 168 hours post-dose. |
| Vz/F for PF-06463922 | Apparent volume of distribution | PF-06463922 pre-dose, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and up to 168 hours post-dose. |
| AUCinf for any potential PF-06463922 metabolite if necessary | Area under the plasma concentration-time profile from time zero extrapolated to infinite time | PF-06463922 pre-dose, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and up to 168 hours post-dose. |
| AUClast for any potential PF-06463922 metabolite if necessary | Area under the plasma concentration-time profile from time zero to the time of the last quantifiable concentration (Clast) | PF-06463922 pre-dose, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and up to 168 hours post-dose. |
| Cmax for any potential PF-06463922 metabolite if appropriate | Maximum plasma concentration | PF-06463922 pre-dose, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and up to 168 hours post-dose. |
| Tmax for any potential PF-06463922 metabolite if appropriate | Time to Cmax | PF-06463922 pre-dose, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and up to 168 hours post-dose. |
| t1/2 for any potential metabolite of PF-06463922 if appropriate | Terminal plasma elimination half-life | PF-06463922 pre-dose, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and up to 168 hours post-dose. |
| MRCmax for any potential PF-06463922 metabolite if appropriate | metabolite to parent ratio for Cmax | PF-06463922 pre-dose, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and up to 168 hours post-dose. |
| MRAUClast for any potential PF-06463922 metabolite if appropriate | metabolite to parent ratio for AUClast | PF-06463922 pre-dose, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and up to 168 hours post-dose. |
| MRAUCinf for any potential PF-06463922 metabolite if appropriate | metabolite to parent ratio for AUCinf | PF-06463922 pre-dose, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and up to 168 hours post-dose. |
| PR interval after PF-06463922 alone and after increased exposure of PF 06463922 (due to concomitant itraconzole administration). | Change in PR interval from baseline after administration of PF-06463922 single dose as assessed by ECG. | Within 24 hours after single dose administration of PF-06463922 alone and in combination with itraconazole. |
| D010879 |
| Piperazines |