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The purpose of this study is to compare the amount of PF-07081532 in blood after taking two different forms of PF-07081532. This study is seeking participants who are at least 18 years of age and are overweight and/or obese. All study participants will receive a total of 2 single doses of this study medication in either form. Form A consists of a PF-07081532 20 mg immediate release tablet and a PF-07081532 60 mg immediate release tablet. Form B consists of a PF-07081532 80 mg immediate release tablet. Each single dose will be separated by a minimum of 6 days. The amount of PF-07081532 in the blood for 4 days after taking each single dose will be compared between the two different formulations of PF-07081532.
The total time that participants will take part in this study is about 70 days. The first visit is a screening visit to ensure that participants are appropriately qualified for the study. This will occur up to 28 days before the first single dose. Participants will be admitted into the clinic one day prior to the first single dose and will remain in the clinic for a total of 11 days. The study team will phone the participants 28 to 35 days after the last dose of study medication.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Formulation A (Reference) followed by Formulation B (Test) | Experimental |
| |
| Formulation B (Test) followed by Formulation A (Reference) | Experimental |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Formulation A (PF-07081532 20 mg plus 60 mg) | Drug | Formulation A: administered as a 20 mg immediate release tablet and a 60 mg immediate release tablet |
|
| Measure | Description | Time Frame |
|---|---|---|
| Pharmacokinetics Parameter - Area Under the Concentration-Time Curve to Infinity (AUCinf) of PF-07081532 | AUCinf is the area under the concentration-time curve to infinity. AUCinf was calculated by AUClast + (Clast*/kel), where Clast* is the predicted plasma concentration at the last quantifiable time point estimated from the log-linear regression analysis and kel is the terminal phase rate constant calculated by a linear regression of the log-linear concentration time curve. | Pre-dose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48, 72, and 96 hours post dose on Day 1 of Period 1 and Period 2 |
| Pharmacokinetics Parameter - Area Under the Plasma Concentration-Time Profile From Time 0 to the Time of the Last Quantifiable Concentration (AUClast) of PF-07081532 | AUClast is the area under the plasma concentration-time profile from time 0 to the time of the last quantifiable concentration. AUClast was calculated by Linear/Log trapezoidal method. | Pre-dose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48, 72, and 96 hours post dose on Day 1 of Period 1 and Period 2 |
| Pharmacokinetics Parameter - Maximum Observed Concentration (Cmax) of PF-07081532 | Cmax is the maximum observed concentration. | Pre-dose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48, 72, and 96 hours post dose of Day 1 Period 1 and Period 2. |
| Measure | Description | Time Frame |
|---|---|---|
| Number of Participants With Treatment-Emergent Adverse Events (TEAEs) (All-Causality and Treatment-Related) | An adverse event (AE) is any untoward medical occurrence in a clinical study participant, temporally associated with the use of study intervention, whether or not considered related to the study intervention. A serious adverse event (SAE) was defined as an AE: 1. resulting in death, 2. was life-threatening, 3. required inpatient hospitalization or prolongation of existing hospitalization, 4. resulted in persistent disability, 5. was a congenital anomaly/birth defect, or considered to be an important medical event. Treatment-related AE was any untoward medical occurrence attributed to study intervention in a participant who received study intervention. Treatment-emergent are events between first dose of study intervention and up to 28-35 days after last dose that were absent before treatment or that worsened relative to pretreatment state. |
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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 |
|---|---|---|---|---|---|---|
| New Haven Clinical Research Unit | 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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Pfizer will provide access to individual de-identified participant data and related study documents (e.g. protocol, Statistical Analysis Plan (SAP), Clinical Study Report (CSR)) upon request from qualified researchers, and subject to certain criteria, conditions, and exceptions. Further details on Pfizer's data sharing criteria and process for requesting access can be found at: https://www.pfizer.com/science/clinical\_trials/trial\_data\_and\_results/data\_requests.
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A total of 20 participants were enrolled and treated in the study. All 20 participants completed the study.
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| ID | Title | Description |
|---|---|---|
| FG000 | Sequence 1 | Participants in Sequence 1 received a single dose of PF-07081532 20 mg immediate release tablet and 60 mg immediate release tablet (Formulation A) on Period 1 Day 1, and then received a single dose of PF-07081532 80 mg immediate release tablet (Formulation B) on Period 2 Day 1, with a minimum washout period of 6 days between the 2 doses. |
| FG001 | Sequence 2 | Participants in Sequence 2 received a single dose of PF-07081532 80 mg immediate release tablet (Formulation B) on Period 1 Day 1, and then received a single dose of PF-07081532 20 mg immediate release tablet and 60 mg immediate release tablet (Formulation A) on Period 2 Day 1, with a minimum washout period of 6 days between the 2 doses. |
| Title | Milestones | Reasons Not Completed | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Period 1 |
| |||||||||||||
| Period 2 |
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This group includes all participants who enrolled in this study and received at least 1 dose of study intervention regardless of the arms they assigned to.
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| ID | Title | Description |
|---|---|---|
| BG000 | All Participants | This group includes all participants who enrolled in this study and received at least 1 dose of study intervention. |
| 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 | Pharmacokinetics Parameter - Area Under the Concentration-Time Curve to Infinity (AUCinf) of PF-07081532 | AUCinf is the area under the concentration-time curve to infinity. AUCinf was calculated by AUClast + (Clast*/kel), where Clast* is the predicted plasma concentration at the last quantifiable time point estimated from the log-linear regression analysis and kel is the terminal phase rate constant calculated by a linear regression of the log-linear concentration time curve. | All participants who took at least 1 dose of study intervention and in whom at least 1 of the PK parameters of interest were reported. Here "Number of Participants Analyzed" signifies participants who contributed to this outcome measure. | Posted | Geometric Mean | Geometric Coefficient of Variation | nanogram*hour/milliliter (ng*hr/mL) | Pre-dose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48, 72, and 96 hours post dose on Day 1 of Period 1 and Period 2 |
|
From the first dose up to 28 to 35 days after administration of the final dose of study intervention (maximum of 51 days)
Same event may appear as both an AE and SAE. However, what is presented are distinct events. An event may be categorized as serious in one participant and as non-serious in another, or a participant may have experienced both a serious and non-serious event. Analysis performed on safety set.
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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 | Formulation A | Formulation A was administrated as PF-07081532 20 mg immediate release tablet + 60 mg immediate release tablet. Participants in Sequence 1 received Formulation A in Period 1, Participants in Sequence 2 received Formulation A in Period 2. |
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| Term | Organ System | Source Vocabulary | Assessment Type | Notes | Statistical Information |
|---|---|---|---|---|---|
| Constipation | Gastrointestinal disorders | MedDRA version 25.1 | 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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| Type | Includes Protocol | Includes SAP | Includes ICF | Document Label | Document Date | Document Uploaded Date | Document File Name |
|---|---|---|---|---|---|---|---|
| Prot | Yes | No | No | Study Protocol | Nov 30, 2022 | Mar 5, 2024 | Prot_000.pdf |
| SAP | No | Yes | No | Statistical Analysis Plan | Jan 19, 2023 | Mar 5, 2024 | SAP_001.pdf |
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| ID | Term |
|---|---|
| D050177 | Overweight |
| D009765 | Obesity |
| ID | Term |
|---|---|
| D044343 | Overnutrition |
| D009748 | Nutrition Disorders |
| D009750 | Nutritional and Metabolic Diseases |
| D001835 | Body Weight |
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PF-07081532 80 mg will be provided in 2 different oral formulations (A and B). Formulation A will be administered as a PF-07081532 20 mg immediate release tablet and a 60 mg immediate release tablet. Formulation B will be administered as a PF-07081532 80 mg immediate release tablet. The overall design is a randomized, open-label, single dose, 2-period, 2-sequence, crossover study.
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(open label)
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| Formulation B (PF-07081532 80 mg) | Drug | Formulation B: administered as a 80 mg immediate release tablet |
|
| From the first dose up to 28 to 35 days after administration of the final dose of study intervention (maximum of 51 days) |
| Number of Participants With Laboratory Abnormalities | Participants with laboratory abnormalities that met pre-specified criteria: Urate (millimole/Liter) > 1.2*ULN (upper limit of normal) and Monocytes/Leukocytes (%) > 1.2*ULN. | Baseline (Day 1) up to Period 2 Day 5 |
| Number of Participants Meeting Pre-Specified Criteria of Vital Signs | Pre-specified criteria of vital signs included: Systolic blood pressure (BP): minimum (min) <90 mmHg, change from baseline (CfB) maximum (max) decrease or increase >=30mmHg; Diastolic BP min <50mmHg, CfB max decrease or increase >=20mmHg; supine pulse rate: min < 40 beats per minute (bpm), max > 120 bpm. | Baseline (Day 1) up to Period 2 Day 5 |
| Number of Participants Meeting Pre-Specified Criteria of Electrocardiogram (ECGs) | The pre-specified criteria of ECG included: PR interval, aggregated: value >=300 msec, %change >= 25/50% msec; QRS duration, aggregated: value>=200 msec, %changes >= 25/50% msec; QTCF interval, aggregated: 450<=value<480 msec, 480<=value<500 msec, value>=500 msec, 30<=changes<60msec, and changes>=60msec. | Baseline (Day 1) up to Period 2 Day 5 |
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| Participants |
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| Age, Continuous | Mean | Standard Deviation | years |
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| Sex: Female, Male | Count of Participants | Participants |
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| Ethnicity (NIH/OMB) | Count of Participants | Participants |
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| Race (NIH/OMB) | Count of Participants | Participants |
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| Body Mass Index | BMI is a person's weight in kilograms divided by the square of height in meters. | Median | Full Range | kg/m^2 |
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Formulation A was administrated as PF-07081532 20 mg immediate release tablet and 60 mg immediate release tablet. Participants in Sequence 1 received Formulation A in Period 1, participants in Sequence 2 received Formulation A in Period 2. |
| OG001 | Formulation B | Formulation B was administrated as PF-07081532 80 mg immediate release tablet. Participants in Sequence 1 received Formulation B in Period 2, participants in Sequence 2 received Formulation B in Period 1. |
|
|
|
| Primary | Pharmacokinetics Parameter - Area Under the Plasma Concentration-Time Profile From Time 0 to the Time of the Last Quantifiable Concentration (AUClast) of PF-07081532 | AUClast is the area under the plasma concentration-time profile from time 0 to the time of the last quantifiable concentration. AUClast was calculated by Linear/Log trapezoidal method. | All participants who took at least 1 dose of study intervention and in whom at least 1 of the PK parameters of interest were reported. Here "Number of Participants Analyzed" signifies participants who contributed to this outcome measure. | Posted | Geometric Mean | Geometric Coefficient of Variation | ng*hr/mL | Pre-dose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48, 72, and 96 hours post dose on Day 1 of Period 1 and Period 2 |
|
|
|
|
| Primary | Pharmacokinetics Parameter - Maximum Observed Concentration (Cmax) of PF-07081532 | Cmax is the maximum observed concentration. | All participants who took at least 1 dose of study intervention and in whom at least 1 of the PK parameters of interest were reported. Here "Number of Participants Analyzed" signifies participants who contributed to this outcome measure. | Posted | Geometric Mean | Geometric Coefficient of Variation | nanogram/milliliter (ng/mL) | Pre-dose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48, 72, and 96 hours post dose of Day 1 Period 1 and Period 2. |
|
|
|
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| Secondary | Number of Participants With Treatment-Emergent Adverse Events (TEAEs) (All-Causality and Treatment-Related) | An adverse event (AE) is any untoward medical occurrence in a clinical study participant, temporally associated with the use of study intervention, whether or not considered related to the study intervention. A serious adverse event (SAE) was defined as an AE: 1. resulting in death, 2. was life-threatening, 3. required inpatient hospitalization or prolongation of existing hospitalization, 4. resulted in persistent disability, 5. was a congenital anomaly/birth defect, or considered to be an important medical event. Treatment-related AE was any untoward medical occurrence attributed to study intervention in a participant who received study intervention. Treatment-emergent are events between first dose of study intervention and up to 28-35 days after last dose that were absent before treatment or that worsened relative to pretreatment state. | All participants who take at least 1 dose of study intervention. | Posted | Count of Participants | Participants | From the first dose up to 28 to 35 days after administration of the final dose of study intervention (maximum of 51 days) |
|
|
|
| Secondary | Number of Participants With Laboratory Abnormalities | Participants with laboratory abnormalities that met pre-specified criteria: Urate (millimole/Liter) > 1.2*ULN (upper limit of normal) and Monocytes/Leukocytes (%) > 1.2*ULN. | All participants who took at least 1 dose of study intervention. Here "Number of Participants Analyzed" signifies participants who contributed to this outcome measure. | Posted | Count of Participants | Participants | Baseline (Day 1) up to Period 2 Day 5 |
|
|
|
| Secondary | Number of Participants Meeting Pre-Specified Criteria of Vital Signs | Pre-specified criteria of vital signs included: Systolic blood pressure (BP): minimum (min) <90 mmHg, change from baseline (CfB) maximum (max) decrease or increase >=30mmHg; Diastolic BP min <50mmHg, CfB max decrease or increase >=20mmHg; supine pulse rate: min < 40 beats per minute (bpm), max > 120 bpm. | All participants who took at least 1 dose of study intervention. | Posted | Count of Participants | Participants | Baseline (Day 1) up to Period 2 Day 5 |
|
|
|
| Secondary | Number of Participants Meeting Pre-Specified Criteria of Electrocardiogram (ECGs) | The pre-specified criteria of ECG included: PR interval, aggregated: value >=300 msec, %change >= 25/50% msec; QRS duration, aggregated: value>=200 msec, %changes >= 25/50% msec; QTCF interval, aggregated: 450<=value<480 msec, 480<=value<500 msec, value>=500 msec, 30<=changes<60msec, and changes>=60msec. | All participants who took at least 1 dose of study intervention. | Posted | Count of Participants | Participants | Baseline (Day 1) up to Period 2 Day 5 |
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|
| 0 |
| 20 |
| 0 |
| 20 |
| 9 |
| 20 |
| EG001 | Formulation B | Formulation B was administrated as PF-07081532 80 mg immediate release tablet. Participants in Sequence 1 received Formulation B in Period 2, Participants in Sequence 2 received Formulation B in Period 1. | 0 | 20 | 0 | 20 | 8 | 20 |
| Dyspepsia | Gastrointestinal disorders | MedDRA version 25.1 | Non-systematic Assessment |
|
| Nausea | Gastrointestinal disorders | MedDRA version 25.1 | Non-systematic Assessment |
|
| Vomiting | Gastrointestinal disorders | MedDRA version 25.1 | Non-systematic Assessment |
|
| Dizziness | Nervous system disorders | MedDRA version 25.1 | Non-systematic Assessment |
|
| Dysgeusia | Nervous system disorders | MedDRA version 25.1 | Non-systematic Assessment |
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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.
| D012816 |
| Signs and Symptoms |
| D013568 | Pathological Conditions, Signs and Symptoms |
| All-Causality Treatment-Emergent SAE |
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| Treatment-Related Treatment-Emergent SAE |
|