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The purpose of this study is to investigate the pharmacokinetics of single doses of PF-02341066 (150, 250, and 400 mg) in the fasted condition in Japanese healthy male volunteers.
The purpose of this study is to investigate the pharmacokinetics of single doses of PF-02341066 (150, 250, and 400 mg) in the fasted condition in Japanese healthy male volunteers.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| 1.0 | Experimental | This study will consist of three cohorts: PF-02341066 150 mg treatment group (n = 6), PF-02341066 250 mg treatment group (n = 6) and PF-02341066 400 mg treatment group (n = 6). |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| PF-02341066 | Drug | Cohort 1: a 150 mg single dose of PF-02341066 administered as 1 x 50 mg IRT and 1 x 100 mg IRT. |
|
| Measure | Description | Time Frame |
|---|---|---|
| Area Under the Plasma Concentration-time Profile From Time Zero Extrapolated to Infinite Time [AUC(0-inf)] of Crizotinib | AUC(0-inf) of crizotinib is estimated from the crizotinib concentration. It is obtained from AUClast plus (Clast/kel). AUClast = area under the plasma concentration-time curve from zero time until the last measurable concentration. Clast = the last quantifiable concentration. Kel = terminal phase elimination rate constant. | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
| Area Under the Plasma Concentration-time Profile From Time Zero to the Time of the Last Quantifiable Concentration (AUClast) of Crizotinib | AUClast of crizotinib is estimated from the crizotinib concentration. It is obtained from Linear/Log trapezoidal method. | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
| Maximum Plasma Concentration (Cmax) of Crizotinib | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose | |
| Time to Cmax (Tmax) of Crizotinib | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose | |
| Terminal Elimination Half-life (t1/2) of Crizotinib | t1/2 of crizotinib is the time measured for the plasma concentration to decrease by one half. It is obtained from a Loge(2)/kel. Kel = terminal phase elimination rate constant | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
| Apparent Oral Clearance (CL/F) of Crizotinib | CL/F of crizotinib is obtained from a Dose per AUCinf. | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
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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 Investigational Site | Hachioji-shi | Tokyo | Japan |
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| Label | URL |
|---|---|
| To obtain contact information for a study center near you, click here. | View source |
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Twelve healthy subjects were assigned to open-label crizotinib treatment in either the 150 mg cohort (6 subjects) or 250 mg cohort (6 subjects).
After the completion of assessment of safety at both 150 mg and 250 mg cohorts, the 400 mg cohort, the highest dose level in this study, was started.
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| ID | Title | Description |
|---|---|---|
| FG000 | Crizotinib 150 mg | A 150 mg single dose of crizotinib administered as one 50 mg Immediate Release Tablet (IRT) and one 100 mg IRT |
| FG001 | Crizotinib 250 mg | A 250 mg single dose of crizotinib administered as one 50 mg IRT and two 100 mg IRTs |
| FG002 | Crizotinib 400 mg | A 400 mg single dose of crizotinib administered as four 100 mg IRTs. |
| Title | Milestones | Reasons Not Completed | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Overall Study |
|
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| ID | Title | Description |
|---|---|---|
| BG000 | Crizotinib 150 mg | A 150 mg single dose of crizotinib administered as one 50 mg Immediate Release Tablet (IRT) and one 100 mg IRT |
| BG001 | Crizotinib 250 mg | A 250 mg single dose of crizotinib administered as one 50 mg IRT and two 100 mg IRTs |
| Units | Counts |
|---|---|
| Participants |
|
| Title | Description | Population Description | Parameter Type | Dispersion Type | Unit of Measure | Calculate Percentage | Denominator Units Selected | Denominators | Classes |
|---|---|---|---|---|---|---|---|---|---|
| Age, Categorical | Count of Participants |
| Type | Title | Description | Population Description | Reporting Status | Anticipated Posting Date | Parameter Type | Dispersion Type | Unit of Measure | Calculate Percentage | Time Frame | Units Analyzed | Denominator Units Selected | Arm/Group Information | Denominators | Classes | Analyses | ||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Primary | Area Under the Plasma Concentration-time Profile From Time Zero Extrapolated to Infinite Time [AUC(0-inf)] of Crizotinib | AUC(0-inf) of crizotinib is estimated from the crizotinib concentration. It is obtained from AUClast plus (Clast/kel). AUClast = area under the plasma concentration-time curve from zero time until the last measurable concentration. Clast = the last quantifiable concentration. Kel = terminal phase elimination rate constant. | Posted | Geometric Mean | Standard Deviation | ng*hr/mL | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
|
For serious adverse event, up to 28 days after the last administration of the study drugs
The same event may appear as both an AE and a SAE. However, what is presented are distinct events. An event may be categorized as serious in one subject and as nonserious in another subject, or one subject may have experienced both a serious and nonserious event during the study.
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| ID | Title | Description | Deaths (Affected) | Deaths (At Risk) | Serious Events (Affected) | Serious Events (At Risk) | Other Events (Affected) | Other Events (At Risk) |
|---|---|---|---|---|---|---|---|---|
| EG000 | Crizotinib 150 mg | A 150 mg single dose of crizotinib administered as one 50 mg Immediate Release Tablet (IRT) and one 100 mg IRT |
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| Term | Organ System | Source Vocabulary | Assessment Type | Notes | Statistical Information |
|---|---|---|---|---|---|
| Nausea | Gastrointestinal disorders | MedDRA 13.1 | Systematic Assessment |
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| Title | Organization | Phone | Extension | |
|---|---|---|---|---|
| Pfizer ClinicalTrials.gov Call Center | Pfizer, Inc. | 1-800-718-1021 | ClinicalTrials.gov_Inquiries@pfizer.com |
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| ID | Term |
|---|---|
| D000077547 | Crizotinib |
| ID | Term |
|---|---|
| D010880 | Piperidines |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D006571 | Heterocyclic Compounds |
| D000631 | Aminopyridines |
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| PF-02341066 | Drug | Cohort 2: a 250 mg single dose of PF-02341066 administered as 1 x 50 mg IRT and 2 x 100 mg IRTs. |
|
| PF-02341066 | Drug | Cohort 3: a 400 mg single dose of PF-02341066 administered as 4 x 100 mg IRTs. |
|
| Apparent Volume of Distribution (Vz/F) of Crizotinib | Vz/F of crizotinib is obtained from a Dose / (AUCinf *kel). Kel = terminal phase elimination rate constant | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
| Dose Normalized AUC(0-inf) of Crizotinib | Dose normalized (to 150 mg dose) AUC(0-inf) is obtained from AUC(0-inf) / (Dose/150). | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
| Dose Normalized AUClast of Crizotinib | Dose normalized (to 150 mg dose) AUClast is obtained from AUClast / (Dose/150). | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
| Dose Normalized Cmax of Crizotinib | Dose normalized (to 150 mg dose) Cmax is obtained from Cmax / (Dose/150). | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
| Area Under the Plasma Concentration-time Profile From Time Zero Extrapolated to Infinite Time (AUC0-inf) of Plasma Active Metabolite (PF-06260182) | AUC(0-inf) of PF-06260182 is estimated from the PF-06260182 concentration. It is obtained from AUClast plus (Clast/kel). AUClast = area under the plasma concentration-time curve from zero time until the last measurable concentration. Clast = the last quantifiable concentration. Kel = terminal phase elimination rate constant. | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
| Area Under the Plasma Concentration-time Profile From Time Zero to the Time of the Last Quantifiable Concentration (AUClast) of Plasma Active Metabolite (PF-06260182) | AUClast of crizotinib is estimated from the crizotinib concentration. It is obtained from Linear/Log trapezoidal method. | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
| Maximum Plasma Concentration (Cmax) of Plasma Active Metabolite (PF-06260182) | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
| Time to Cmax (Tmax) of Plasma Active Metabolite (PF-06260182) | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
| Metabolite to Parent Ratio AUC(0-inf) | The metabolic ratio (MR) is calculated by first converting the AUC(0-inf) for both crizotinib and metabolite (PF-06260182) from mass units to molar units. | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
| Metabolite to Parent Ratio AUClast | The metabolic ratio (MR) is calculated by first converting the AUClast for both crizotinib and metabolite (PF-06260182) from mass units to molar units. | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
| Metabolite to Parent Ratio Cmax | The metabolic ratio (MR) is calculated by first converting the Cmax for both crizotinib and metabolite (PF-06260182) from mass units to molar units. | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
| BG002 | Crizotinib 400 mg | A 400 mg single dose of crizotinib administered as four 100 mg IRTs. |
| BG003 | Total | Total of all reporting groups |
| Participants |
|
| Sex: Female, Male | Count of Participants | Participants |
|
A 250 mg single dose of crizotinib administered as one 50 mg IRT and two 100 mg IRTs
| OG002 | Crizotinib 400 mg | A 400 mg single dose of crizotinib administered as four 100 mg IRTs. |
|
|
| Primary | Area Under the Plasma Concentration-time Profile From Time Zero to the Time of the Last Quantifiable Concentration (AUClast) of Crizotinib | AUClast of crizotinib is estimated from the crizotinib concentration. It is obtained from Linear/Log trapezoidal method. | Posted | Geometric Mean | Standard Deviation | ng*hr/mL | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
|
|
|
| Primary | Maximum Plasma Concentration (Cmax) of Crizotinib | Posted | Geometric Mean | Standard Deviation | ng/mL | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
|
|
|
| Primary | Time to Cmax (Tmax) of Crizotinib | Posted | Median | Full Range | ng/mL | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
|
|
|
| Primary | Terminal Elimination Half-life (t1/2) of Crizotinib | t1/2 of crizotinib is the time measured for the plasma concentration to decrease by one half. It is obtained from a Loge(2)/kel. Kel = terminal phase elimination rate constant | Posted | Mean | Standard Deviation | hours | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
|
|
|
| Primary | Apparent Oral Clearance (CL/F) of Crizotinib | CL/F of crizotinib is obtained from a Dose per AUCinf. | Posted | Geometric Mean | Standard Deviation | liter per hour | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
|
|
|
| Primary | Apparent Volume of Distribution (Vz/F) of Crizotinib | Vz/F of crizotinib is obtained from a Dose / (AUCinf *kel). Kel = terminal phase elimination rate constant | Posted | Geometric Mean | Standard Deviation | Liter | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
|
|
|
| Primary | Dose Normalized AUC(0-inf) of Crizotinib | Dose normalized (to 150 mg dose) AUC(0-inf) is obtained from AUC(0-inf) / (Dose/150). | Posted | Geometric Mean | Standard Deviation | ng*hr/mL | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
|
|
|
| Primary | Dose Normalized AUClast of Crizotinib | Dose normalized (to 150 mg dose) AUClast is obtained from AUClast / (Dose/150). | Posted | Geometric Mean | Standard Deviation | ng*hr/mL | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
|
|
|
| Primary | Dose Normalized Cmax of Crizotinib | Dose normalized (to 150 mg dose) Cmax is obtained from Cmax / (Dose/150). | Posted | Geometric Mean | Standard Deviation | ng/mL | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
|
|
|
| Primary | Area Under the Plasma Concentration-time Profile From Time Zero Extrapolated to Infinite Time (AUC0-inf) of Plasma Active Metabolite (PF-06260182) | AUC(0-inf) of PF-06260182 is estimated from the PF-06260182 concentration. It is obtained from AUClast plus (Clast/kel). AUClast = area under the plasma concentration-time curve from zero time until the last measurable concentration. Clast = the last quantifiable concentration. Kel = terminal phase elimination rate constant. | Posted | Geometric Mean | Standard Deviation | ng*hr/mL | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
|
|
|
| Primary | Area Under the Plasma Concentration-time Profile From Time Zero to the Time of the Last Quantifiable Concentration (AUClast) of Plasma Active Metabolite (PF-06260182) | AUClast of crizotinib is estimated from the crizotinib concentration. It is obtained from Linear/Log trapezoidal method. | Posted | Geometric Mean | Standard Deviation | ng*hr/mL | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
|
|
|
| Primary | Maximum Plasma Concentration (Cmax) of Plasma Active Metabolite (PF-06260182) | Posted | Geometric Mean | Standard Deviation | ng/mL | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
|
|
|
| Primary | Time to Cmax (Tmax) of Plasma Active Metabolite (PF-06260182) | Posted | Median | Full Range | ng/mL | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
|
|
|
| Primary | Metabolite to Parent Ratio AUC(0-inf) | The metabolic ratio (MR) is calculated by first converting the AUC(0-inf) for both crizotinib and metabolite (PF-06260182) from mass units to molar units. | Posted | Geometric Mean | Standard Deviation | ratio | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
|
|
|
| Primary | Metabolite to Parent Ratio AUClast | The metabolic ratio (MR) is calculated by first converting the AUClast for both crizotinib and metabolite (PF-06260182) from mass units to molar units. | Posted | Geometric Mean | Standard Deviation | ratio | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
|
|
|
| Primary | Metabolite to Parent Ratio Cmax | The metabolic ratio (MR) is calculated by first converting the Cmax for both crizotinib and metabolite (PF-06260182) from mass units to molar units. | Posted | Geometric Mean | Standard Deviation | ratio | 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose |
|
|
|
| 0 |
| 6 |
| 2 |
| 6 |
| EG001 | Crizotinib 250 mg | A 250 mg single dose of crizotinib administered as one 50 mg IRT and two 100 mg IRTs | 0 | 6 | 0 | 6 |
| EG002 | Crizotinib 400 mg | A 400 mg single dose of crizotinib administered as four 100 mg IRTs. | 0 | 6 | 1 | 6 |
| Alanine aminotransferase increased | Investigations | MedDRA 13.1 | Systematic Assessment |
|
| Epistaxis | Respiratory, thoracic and mediastinal disorders | MedDRA 13.1 | Systematic Assessment |
|
Pfizer has the right to review disclosures, requesting a delay of less than 60 days. Investigator will postpone single center publications until after disclosure of pooled data (all sites), less than 12 months from study completion/termination at all participating sites. Investigator may not disclose previously undisclosed confidential information other than study results.
| D011725 |
| Pyridines |