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The rationale for this study is to investigate the absorption, metabolism and excretion of [14C]PF 02341066 and characterize plasma, fecal and urinary radioactivity, and identify any metabolites, if possible, of [14C]PF 02341066 in humans.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| 1 | Experimental |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| PF-02341066 | Drug | oral suspension, single 250 mg dose of PF 02341066 containing approximately 100 µCi of [14C]PF 02341066 |
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| Measure | Description | Time Frame |
|---|---|---|
| Maximum Observed Plasma Concentration (Cmax) | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hours (hrs), 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose | |
| Time to Reach Maximum Observed Plasma Concentration (Tmax) | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose | |
| Area Under the Curve From Time Zero to Last Quantifiable Plasma Concentration (AUClast) | Area under the concentration time-curve from zero to the last measured plasma concentration (AUClast). | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
| Area Under the Plasma Concentration Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)] | AUC (0 - ∞) = Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - ∞). It is obtained from AUC (0 - t) plus AUC (t - ∞). | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
| Plasma Decay Half Life (t1/2) | Plasma Decay half-life is the time measured for the concentration to decrease by one half. | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
| Apparent Oral Clearance (CL/F) of Plasma PF-02341066 | Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the body. Clearance obtained after oral dose (apparent oral clearance) is influenced by the fraction of the dose absorbed. |
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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 | New Haven | Connecticut | 06511 | United States |
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| Label | URL |
|---|---|
| To obtain contact information for a study center near you, click here. | View source |
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| ID | Title | Description |
|---|---|---|
| FG000 | PF-02341066 250 mg | Single oral dose of PF-02341066 250 milligram (mg) containing 100 micro-curie (μCi) Carbon -14[14C]. |
| Title | Milestones | Reasons Not Completed | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Overall Study |
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| ID | Title | Description |
|---|---|---|
| BG000 | PF-02341066 250 mg | Single oral dose of PF-02341066 250 mg containing 100 μCi [14C]. |
| Units | Counts |
|---|---|
| Participants |
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| Title | Description | Population Description | Parameter Type | Dispersion Type | Unit of Measure | Calculate Percentage | Denominator Units Selected | Denominators | Classes |
|---|---|---|---|---|---|---|---|---|---|
| Age Continuous | Mean |
| 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 | Maximum Observed Plasma Concentration (Cmax) | The Pharmacokinetic (PK) parameter analysis population included all treated participants who had at least 1 of the PK parameters of primary interest. | Posted | Geometric Mean | Standard Deviation | ng/mL | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hours (hrs), 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
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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 | PF-02341066 250 mg | Single oral dose of PF-02341066 250 mg containing 100 μCi [14C]. |
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| Term | Organ System | Source Vocabulary | Assessment Type | Notes | Statistical Information |
|---|---|---|---|---|---|
| Abdominal discomfort | Gastrointestinal disorders | MedDRA 13.0 | Non-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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| Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
| Apparent Volume of Distribution (V/F) in Plasma | Volume of distribution is defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired blood concentration of a drug. Apparent volume of distribution after oral dose (V/F) is influenced by the fraction absorbed. | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
| Renal Clearance (CLr) of PF-02341066 | CLr is the volume of plasma from which a substance is completely removed by the kidney in a given amount of time. | Predose, 0 to 4, 4 to 8, 8 to 16, 16 to 24 to 36, 36 to 48 hrs and then after every 24 hrs until up to 480 hrs post-dose |
| Total Amount of Unchanged Drug Excreted in the Urine From Time Zero to Infinite Time (Ae) | Ae = concentration of unchanged drug excreted in the urine multiplied by volume of unchanged drug excreted in urine. | Predose, 0 to 4, 4 to 8, 8 to 16, 16 to 24 to 36, 36 to 48 hrs and then after every 24 hrs until up to 480 hrs post-dose |
| Total Amount of Unchanged Drug Excreted in the Urine Expressed as Percent of Dose From Time Zero to Infinite Time [Ae(%)] | Predose, 0 to 4, 4 to 8, 8 to 16, 16 to 24 to 36, 36 to 48 hrs and then after every 24 hrs until up to 480 hrs post-dose |
| Maximum Observed Concentration in Plasma Radioactivity (Cmax) | Radioactivity corresponds to 100 μCi [14C]PF-02341066. | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
| Time to Reach Maximum Observed Plasma Radioactivity Concentration (Tmax) | Radioactivity corresponds to 100 μCi [14C]PF-02341066. | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
| Area Under the Curve From Time Zero to Last Quantifiable Plasma Radioactivity Concentration (AUClast) | Area under the concentration time-curve from zero to the last measured plasma concentration. Radioactivity corresponds to 100 μCi [14C]PF-02341066. | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
| Area Under the Plasma Radioactivity Concentration Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)] | Area under the concentration curve from time zero to extrapolated infinite time [AUC (0 - ∞)] in plasma. Radioactivity corresponds to 100 μCi [14C]PF-02341066. | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
| Decay Half Life (t1/2) of Radioactivity in Plasma | Plasma decay half-life is the time measured for the plasma radioactivity concentration to decrease by one half. Radioactivity corresponds to 100 μCi [14C]PF-02341066. | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
| Apparent Oral Clearance (CL/F) of Plasma Radioactivity | Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the body. Clearance obtained after oral dose (apparent oral clearance) is influenced by the fraction of the dose absorbed. Radioactivity corresponds to 100 μCi [14C]PF-02341066. | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
| Apparent Volume of Distribution (V/F) in Plasma Radioactivity | Volume of distribution is defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired blood concentration of a drug. Apparent volume of distribution after oral dose (V/F) is influenced by the fraction absorbed. Radioactivity corresponds to 100 μCi [14C]PF-02341066. | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
| Maximum Observed Concentration of Radioactivity in Whole Blood (Cmax) | Radioactivity corresponds to 100 μCi [14C]PF-02341066. | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
| Time to Reach Maximum Observed Concentration (Tmax) of Radioactivity in Whole Blood | Time to Reach Maximum Observed Concentration (Tmax) of Radioactivity in whole blood. Radioactivity corresponds to 100 μCi [14C]PF-02341066. | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
| Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of Radioactivity in Whole Blood | Area under the concentration time-curve from zero to the last measured concentration (AUClast) in whole blood. Radioactivity corresponds to 100 μCi [14C]PF-02341066. | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
| Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)] of Radioactivity in Whole Blood | Area under the concentration curve from time zero to extrapolated infinite time [AUC (0 - ∞)] in whole blood. Radioactivity corresponds to 100 μCi [14C]PF-02341066. | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
| Decay Half-life (t1/2) of Radioactivity in Whole Blood | Decay half life (t1/2) is the time measured for the concentration to decrease by one half in whole blood. Radioactivity corresponds to 100 μCi [14C]PF-02341066. | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
| Apparent Oral Clearance of Radioactivity From Whole Blood (CL/F) | Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the body. Clearance obtained after oral dose (apparent oral clearance) is influenced by the fraction of the dose absorbed. Radioactivity corresponds to 100 μCi [14C]PF-02341066. | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
| Apparent Volume of Distribution of Radioactivity in Whole Blood (V/F) | Volume of distribution is defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired blood concentration of a drug. Apparent volume of distribution after oral dose (V/F) is influenced by the fraction absorbed. Radioactivity corresponds to 100 μCi [14C]PF-02341066. | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
| Total [14C] Data in Urine | Cumulative amount excreted in urine at specified intervals after administration of a single 250-mg (100 μCi) oral dose of [14C]PF-02341066. | Predose, 0 to 4, 4 to 8, 8 to 16, 16 to 24 to 36, 36 to 48 hrs and then after every 24 hrs until up to 480 hrs post-dose |
| Total [14C] Data in Feces | Cumulative amount excreted in feces at specified intervals after administration of a single 250-mg (100 μCi) oral dose of [14C]PF-02341066. | From Day 0 through pre-dose (Day1) and as passed through until up to 480 hrs post-dose |
| Overall Cumulative Percent Recovery of Radioactivity | Overall cumulative percent of radioactive dose recovered in urine, feces and toilet tissue at specified intervals after administration of a single 250-mg (100 μCi) oral dose of [14C]PF-02341066. | Pre-dose, 0 to 4, 4 to 8, 8 to 16, 16 to 24 to 36, 36 to 48 hrs and then after every 24 hrs until up to 480 hrs post-dose for urine and Day 0 through pre-dose (Day1) and as passed through until up to 480 hrs post-dose for feces |
| Identification and Profiling of Metabolites of [14C]PF-02341066 in Plasma | Identification was done by Radio-High Performance liquid chromatography (HPLC) chromatogram. Relative abundance (profiling) of metabolites in chromatogram were determined by dividing sum of radioactive content of fractions contributing to particular peak by sum of radioactive content of all fractions constructing the radio chromatogram. Metabolites accounting for an average of greater than or equal to (>=) 10% of total recoverable radioactivity in plasma were summarized. Radioactivity corresponds to 100 μCi [14C] PF-02341066. | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
| Identification and Profiling of Metabolites of [14C]PF-02341066 in Feces | In feces, metabolite abundance (profiling) was calculated by multiplying the fractional contribution of radioactive response for the peak in the Radio-HPLC chromatogram to the total radioactivity detected by the percent of administered dose recovered in the matrix. Only those metabolites that were a component of a chromatographic peak that accounted for an average of >=1% of the administered dose, were summarized. Radioactivity corresponds to 100 μCi [14C] PF-02341066. | From Day 0 through pre-dose (Day1) and as passed through until up to 480 hrs post-dose |
| Identification and Profiling of Metabolites of [14C]PF-02341066 in Urine | In urine, metabolite abundance (profiling) was calculated by multiplying the fractional contribution of radioactive response for the peak in the Radio-HPLC chromatogram to the total radioactivity detected by the percent of administered dose recovered in the matrix. Only those metabolites that were a component of a chromatographic peak that accounted for an average of >=1% of the administered dose, were summarized. Radioactivity corresponds to 100 μCi [14C] PF-02341066. | Predose, 0 to 4, 4 to 8, 8 to 16, 16 to 24 to 36, 36 to 48 hrs and then after every 24 hrs until up to 480 hrs post-dose |
| years |
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| Sex: Female, Male | Count of Participants | Participants |
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| Primary | Time to Reach Maximum Observed Plasma Concentration (Tmax) | The PK parameter analysis population included all treated participants who had at least 1 of the PK parameters of primary interest. | Posted | Median | Full Range | hr | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
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| Primary | Area Under the Curve From Time Zero to Last Quantifiable Plasma Concentration (AUClast) | Area under the concentration time-curve from zero to the last measured plasma concentration (AUClast). | The PK parameter analysis population included all treated participants who had at least 1 of the PK parameters of primary interest. | Posted | Geometric Mean | Standard Deviation | ng*hr/mL | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
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| Primary | Area Under the Plasma Concentration Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)] | AUC (0 - ∞) = Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - ∞). It is obtained from AUC (0 - t) plus AUC (t - ∞). | The PK parameter analysis population included all treated participants who had at least 1 of the PK parameters of primary interest. | Posted | Geometric Mean | Standard Deviation | ng*hr/mL | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
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| Primary | Plasma Decay Half Life (t1/2) | Plasma Decay half-life is the time measured for the concentration to decrease by one half. | The PK parameter analysis population included all treated participants who had at least 1 of the PK parameters of primary interest. | Posted | Mean | Standard Deviation | hr | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
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| Primary | Apparent Oral Clearance (CL/F) of Plasma PF-02341066 | Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the body. Clearance obtained after oral dose (apparent oral clearance) is influenced by the fraction of the dose absorbed. | The PK parameter analysis population included all treated participants who had at least 1 of the PK parameters of primary interest. | Posted | Geometric Mean | Standard Deviation | L/hr | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
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| Primary | Apparent Volume of Distribution (V/F) in Plasma | Volume of distribution is defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired blood concentration of a drug. Apparent volume of distribution after oral dose (V/F) is influenced by the fraction absorbed. | The PK parameter analysis population included all treated participants who had at least 1 of the PK parameters of primary interest. | Posted | Geometric Mean | Standard Deviation | L | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
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| Primary | Renal Clearance (CLr) of PF-02341066 | CLr is the volume of plasma from which a substance is completely removed by the kidney in a given amount of time. | The PK parameter analysis population included all treated participants who had at least 1 of the PK parameters of primary interest. | Posted | Geometric Mean | Standard Deviation | L/hr | Predose, 0 to 4, 4 to 8, 8 to 16, 16 to 24 to 36, 36 to 48 hrs and then after every 24 hrs until up to 480 hrs post-dose |
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| Primary | Total Amount of Unchanged Drug Excreted in the Urine From Time Zero to Infinite Time (Ae) | Ae = concentration of unchanged drug excreted in the urine multiplied by volume of unchanged drug excreted in urine. | The PK parameter analysis population included all treated participants who had at least 1 of the PK parameters of primary interest. | Posted | Geometric Mean | Standard Deviation | mg | Predose, 0 to 4, 4 to 8, 8 to 16, 16 to 24 to 36, 36 to 48 hrs and then after every 24 hrs until up to 480 hrs post-dose |
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| Primary | Total Amount of Unchanged Drug Excreted in the Urine Expressed as Percent of Dose From Time Zero to Infinite Time [Ae(%)] | The PK parameter analysis population included all treated participants who had at least 1 of the PK parameters of primary interest. | Posted | Geometric Mean | Standard Deviation | Percent dose of unchanged drug | Predose, 0 to 4, 4 to 8, 8 to 16, 16 to 24 to 36, 36 to 48 hrs and then after every 24 hrs until up to 480 hrs post-dose |
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| Primary | Maximum Observed Concentration in Plasma Radioactivity (Cmax) | Radioactivity corresponds to 100 μCi [14C]PF-02341066. | The radioactivity parameter analysis population included all treated participants who had at least 1 of the radioactivity parameters of primary interest. | Posted | Geometric Mean | Standard Deviation | nanogram-equivalent/milliliter(ng-eq/mL) | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
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| Primary | Time to Reach Maximum Observed Plasma Radioactivity Concentration (Tmax) | Radioactivity corresponds to 100 μCi [14C]PF-02341066. | The radioactivity parameter analysis population included all treated participants who had at least 1 of the radioactivity parameters of primary interest. | Posted | Median | Full Range | hr | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
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| Primary | Area Under the Curve From Time Zero to Last Quantifiable Plasma Radioactivity Concentration (AUClast) | Area under the concentration time-curve from zero to the last measured plasma concentration. Radioactivity corresponds to 100 μCi [14C]PF-02341066. | The radioactivity parameter analysis population included all treated participants who had at least 1 of the radioactivity parameters of primary interest. | Posted | Geometric Mean | Standard Deviation | ng-eq*hr/mL | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
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| Primary | Area Under the Plasma Radioactivity Concentration Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)] | Area under the concentration curve from time zero to extrapolated infinite time [AUC (0 - ∞)] in plasma. Radioactivity corresponds to 100 μCi [14C]PF-02341066. | Data was insufficient to analyze as only 2 participants were evaluable for the parameter. | Posted | Geometric Mean | Standard Deviation | ng-eq*hr/mL | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
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| Primary | Decay Half Life (t1/2) of Radioactivity in Plasma | Plasma decay half-life is the time measured for the plasma radioactivity concentration to decrease by one half. Radioactivity corresponds to 100 μCi [14C]PF-02341066. | Data was insufficient to analyze as only 2 participants were evaluable for the parameter. | Posted | Mean | Standard Deviation | hr | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
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| Primary | Apparent Oral Clearance (CL/F) of Plasma Radioactivity | Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the body. Clearance obtained after oral dose (apparent oral clearance) is influenced by the fraction of the dose absorbed. Radioactivity corresponds to 100 μCi [14C]PF-02341066. | Data was insufficient to analyze as only 2 participants were evaluable for the parameter. | Posted | Geometric Mean | Standard Deviation | L/hr | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
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| Primary | Apparent Volume of Distribution (V/F) in Plasma Radioactivity | Volume of distribution is defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired blood concentration of a drug. Apparent volume of distribution after oral dose (V/F) is influenced by the fraction absorbed. Radioactivity corresponds to 100 μCi [14C]PF-02341066. | Data was insufficient to analyze as only 2 participants were evaluable for the parameter. | Posted | Geometric Mean | Standard Deviation | L | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
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| Primary | Maximum Observed Concentration of Radioactivity in Whole Blood (Cmax) | Radioactivity corresponds to 100 μCi [14C]PF-02341066. | The radioactivity parameter analysis population included all treated participants who had at least 1 of the radioactivity parameters of primary interest. | Posted | Geometric Mean | Standard Deviation | ng-eq/mL | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
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| Primary | Time to Reach Maximum Observed Concentration (Tmax) of Radioactivity in Whole Blood | Time to Reach Maximum Observed Concentration (Tmax) of Radioactivity in whole blood. Radioactivity corresponds to 100 μCi [14C]PF-02341066. | The radioactivity parameter analysis population included all treated participants who had at least 1 of the radioactivity parameters of primary interest. | Posted | Median | Full Range | hr | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
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| Primary | Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of Radioactivity in Whole Blood | Area under the concentration time-curve from zero to the last measured concentration (AUClast) in whole blood. Radioactivity corresponds to 100 μCi [14C]PF-02341066. | The radioactivity parameter analysis population included all treated participants who had at least 1 of the radioactivity parameters of primary interest. | Posted | Geometric Mean | Standard Deviation | ng-eq*hr/mL | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
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| Primary | Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)] of Radioactivity in Whole Blood | Area under the concentration curve from time zero to extrapolated infinite time [AUC (0 - ∞)] in whole blood. Radioactivity corresponds to 100 μCi [14C]PF-02341066. | Data was insufficient to analyze as only 2 participants were evaluable for the parameter. | Posted | Geometric Mean | Standard Deviation | ng-eq*hr/mL | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
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| Primary | Decay Half-life (t1/2) of Radioactivity in Whole Blood | Decay half life (t1/2) is the time measured for the concentration to decrease by one half in whole blood. Radioactivity corresponds to 100 μCi [14C]PF-02341066. | Data was insufficient to analyze as only 2 participants were evaluable for the parameter. | Posted | Mean | Standard Deviation | hr | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
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| Primary | Apparent Oral Clearance of Radioactivity From Whole Blood (CL/F) | Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the body. Clearance obtained after oral dose (apparent oral clearance) is influenced by the fraction of the dose absorbed. Radioactivity corresponds to 100 μCi [14C]PF-02341066. | Data was insufficient to analyze as only 2 participants were evaluable for the parameter. | Posted | Geometric Mean | Standard Deviation | L/hr | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
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| Primary | Apparent Volume of Distribution of Radioactivity in Whole Blood (V/F) | Volume of distribution is defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired blood concentration of a drug. Apparent volume of distribution after oral dose (V/F) is influenced by the fraction absorbed. Radioactivity corresponds to 100 μCi [14C]PF-02341066. | Data was insufficient to analyze as only 2 participants were evaluable for the parameter. | Posted | Geometric Mean | Standard Deviation | L | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
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| Primary | Total [14C] Data in Urine | Cumulative amount excreted in urine at specified intervals after administration of a single 250-mg (100 μCi) oral dose of [14C]PF-02341066. | The radioactivity parameter analysis population included all treated participants who had at least 1 of the radioactivity parameters of primary interest. | Posted | Mean | Standard Deviation | ng-eq | Predose, 0 to 4, 4 to 8, 8 to 16, 16 to 24 to 36, 36 to 48 hrs and then after every 24 hrs until up to 480 hrs post-dose |
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| Primary | Total [14C] Data in Feces | Cumulative amount excreted in feces at specified intervals after administration of a single 250-mg (100 μCi) oral dose of [14C]PF-02341066. | The radioactivity parameter analysis population included all treated participants who had at least 1 of the radioactivity parameters of primary interest. | Posted | Mean | Standard Deviation | ng-eq | From Day 0 through pre-dose (Day1) and as passed through until up to 480 hrs post-dose |
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| Primary | Overall Cumulative Percent Recovery of Radioactivity | Overall cumulative percent of radioactive dose recovered in urine, feces and toilet tissue at specified intervals after administration of a single 250-mg (100 μCi) oral dose of [14C]PF-02341066. | The radioactivity parameter analysis population included all treated participants who had at least 1 of the radioactivity parameters of primary interest. | Posted | Mean | Standard Deviation | Percent recovery of radioactivity | Pre-dose, 0 to 4, 4 to 8, 8 to 16, 16 to 24 to 36, 36 to 48 hrs and then after every 24 hrs until up to 480 hrs post-dose for urine and Day 0 through pre-dose (Day1) and as passed through until up to 480 hrs post-dose for feces |
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| Primary | Identification and Profiling of Metabolites of [14C]PF-02341066 in Plasma | Identification was done by Radio-High Performance liquid chromatography (HPLC) chromatogram. Relative abundance (profiling) of metabolites in chromatogram were determined by dividing sum of radioactive content of fractions contributing to particular peak by sum of radioactive content of all fractions constructing the radio chromatogram. Metabolites accounting for an average of greater than or equal to (>=) 10% of total recoverable radioactivity in plasma were summarized. Radioactivity corresponds to 100 μCi [14C] PF-02341066. | The radioactivity parameter analysis population included all treated participants who had at least 1 of the radioactivity parameters of primary interest. | Posted | Number | Percentage of recovered radioactivity | Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose |
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| Primary | Identification and Profiling of Metabolites of [14C]PF-02341066 in Feces | In feces, metabolite abundance (profiling) was calculated by multiplying the fractional contribution of radioactive response for the peak in the Radio-HPLC chromatogram to the total radioactivity detected by the percent of administered dose recovered in the matrix. Only those metabolites that were a component of a chromatographic peak that accounted for an average of >=1% of the administered dose, were summarized. Radioactivity corresponds to 100 μCi [14C] PF-02341066. | The radioactivity parameter analysis population included all treated participants who had at least 1 of the radioactivity parameters of primary interest. | Posted | Number | Percentage of radioactive dose | From Day 0 through pre-dose (Day1) and as passed through until up to 480 hrs post-dose |
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| Primary | Identification and Profiling of Metabolites of [14C]PF-02341066 in Urine | In urine, metabolite abundance (profiling) was calculated by multiplying the fractional contribution of radioactive response for the peak in the Radio-HPLC chromatogram to the total radioactivity detected by the percent of administered dose recovered in the matrix. Only those metabolites that were a component of a chromatographic peak that accounted for an average of >=1% of the administered dose, were summarized. Radioactivity corresponds to 100 μCi [14C] PF-02341066. | The radioactivity parameter analysis population included all treated participants who had at least 1 of the radioactivity parameters of primary interest. | Posted | Number | Percentage of radioactive dose | Predose, 0 to 4, 4 to 8, 8 to 16, 16 to 24 to 36, 36 to 48 hrs and then after every 24 hrs until up to 480 hrs post-dose |
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| 0 |
| 6 |
| 6 |
| 6 |
| Abdominal pain upper | Gastrointestinal disorders | MedDRA 13.0 | Non-systematic Assessment |
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| Constipation | Gastrointestinal disorders | MedDRA 13.0 | Non-systematic Assessment |
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| Diarrhoea | Gastrointestinal disorders | MedDRA 13.0 | Non-systematic Assessment |
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| Dyspepsia | Gastrointestinal disorders | MedDRA 13.0 | Non-systematic Assessment |
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| Somnolence | Nervous system disorders | MedDRA 13.0 | Non-systematic Assessment |
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| Seborrhoeic dermatitis | Skin and subcutaneous tissue disorders | MedDRA 13.0 | Non-systematic Assessment |
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| Skin exfoliation | Skin and subcutaneous tissue disorders | MedDRA 13.0 | Non-systematic Assessment |
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Not provided
Not provided
Not provided
| D011725 |
| Pyridines |
| Title | Measurements |
|---|---|
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