A Phase 1 interventional study of PF-07258669 and Placebo in Healthy Participants, sponsored by Pfizer. Completed at 1 site in United States. Open to participants aged 18 Years to 55 Years, including healthy volunteers. Per ClinicalTrials.gov, last updated 2024-02-21.
Sponsored by Pfizer · Phase 1, Interventional, and Basic science
This study will be the first time PF-07258669 is administered to humans. The purpose of the study is to evaluate the safety, tolerability, and pharmacokinetics of PF-07258669 following administration of single oral doses to healthy adult participants.
Pfizer is the lead sponsor of 3,244 studies on the registry; 139 are open to participants now.
Of its 582 completed or terminated interventional studies of FDA-regulated products, 381 (65%) have results posted.
Counted across the registry records on this site, refreshed daily.
Exclusion Criteria:
Single dose administration of PF-07258669 and placebo; Within a cohort, participants will receive 3 doses of PF-07258669 and 1 dose of placebo.
Drug: PF-07258669 · Drug: Placebo
Single dose administration of PF-07258669 and placebo; Within a cohort, participants will receive 3 doses of PF-07258669 and 1 dose of placebo.
Drug: PF-07258669 · Drug: Placebo
Single dose administration of PF-07258669 and placebo; Within a cohort, participants will receive 3 doses of PF-07258669 and 1 dose of placebo.
Drug: PF-07258669 · Drug: Placebo
PF-07258669 will be prepared as an oral solution and/or suspension given in escalating single doses to be determined
Matching placebo will be prepared as an oral solution and/or suspension given in each cohort
Number of Participants With Treatment Emergent Adverse Events (TEAEs)
An adverse event (AE) was any untoward medical occurrence in a patient or clinical study subject, temporally associated with the use of study intervention, whether or not considered related to the study intervention. A serious AE (SAE) was defined as any untoward medical occurrence that, at any dose: resulted in death; was life-threatening; required inpatient hospitalization or prolongation of existing hospitalization; resulted in persistent disability/incapacity; was a congenital anomaly/birth defect; or other serious situations such as important medical events. TEAEs were events between first dose of study drug and up to follow-up visit that were absent before treatment or that worsened after treatment. AEs presented below were TEAEs. The investigator was required to use clinical judgment to assess the potential relationship between investigational product and each AE, to define an treatment-related AE.
Time frame: From first dose of study intervention (Day 1) to telephone Follow Up (28-35 days after lase dose of study intervention) (approximately up to 20 weeks)
Number of Participants With Clinical Laboratory Abnormalities (Without Regard to Baseline [BL] Abnormality)
Safety laboratory assessments included clinical chemistry, hematology, urinalysis, and other tests. Abnormality was determined at the investigator's discretion.
Time frame: From BL to onsite Follow Up visit (up to 9 days after last dose of study intervention) (approximately up to 17 weeks)
Number of Participants With Change From BL in Vital Signs Data Meeting the Pre-defined Categorical Summarization Criteria
Abnormality in change from BL in vital signs included: standing diastolic blood pressure (BP) increase and decrease from BL of \>=20mmHg, standing systolic BP increase and decrease from BL of \>=30mmHg, supine diastolic BP increase and decrease from BL of \>=20mmHg, supine systolic BP increase and decrease from BL of \>=30mmHg.
Time frame: From BL to onsite Follow Up visit (up to 9 days after last dose of study intervention) (approximately up to 17 weeks)
Number of Participants With Change From BL in Electrocardiogram (ECG) Data Meeting the Pre-defined Categorical Summarization Criteria
ECG assessments inlcuded PR, QT, QTcF intervals and QRS complex. ECG abnormalities in change from BL included: PR interval BL \>200msec and max \>=25% increase from BL, or BL \<=200msec and max \>=50% increase from BL, QRS interval percent change from BL \>=50%, QTcF change from BL \>=30 and \<=60msec, or change from BL \>60msec.
Time frame: From BL to onsite Follow Up visit (up to 9 days after last dose of study intervention) (approximately up to 17 weeks)
Number of Participants With Clinically-significant Change From BL in Neurological Examination Findings
The neurological exam consisted of assessment of higher cortical function, the cranial nerves, motor function, deep tendon reflexes, sensory exam, and coordination and gait, to the extent needed to assess the participant for any potential changes in neurological status, as determined by the investigator (or designee).
Time frame: From BL to onsite Follow Up visit (up to 9 days after last dose of study intervention) (approximately up to 17 weeks)
Maximum Observed Concentration (Cmax) of PF-07258669
Cmax is the maximum observed plasma concentration.
Time frame: At 0 (prior to dose), 0.17, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, 36, and 48 hours post dose on Day 1 in Periods 1 to 4
Area Under the Plasma Concentration-time Profile From Time 0 to the Time of the Last Quantifiable Concentration (AUClast) of PF-07258669
AUClast is the area under the plasma concentration-time profile from time 0 to the time of the last quantifiable concentration.
Time frame: At 0 (prior to dose), 0.17, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, 36, and 48 hours post dose on Day 1 in Periods 1 to 4
Area Under the Plasma Concentration Time Profile From Time 0 Extrapolated to Infinite Time (AUCinf) of PF-07258669
AUCinf is the area under the plasma concentration time profile from time 0 extrapolated to infinite time.
Time frame: At 0 (prior to dose), 0.17, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, 36, and 48 hours post dose on Day 1 in Periods 1 to 4
Time for Cmax (Tmax) of PF-07258669
Tmax is the time for Cmax.
Time frame: At 0 (prior to dose), 0.17, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, 36, and 48 hours post dose on Day 1 in Periods 1 to 4
Terminal Half-life (t1/2) of PF-07258669
t1/2 is the terminal half-life.
Time frame: At 0 (prior to dose), 0.17, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, 36, and 48 hours post dose on Day 1 in Periods 1 to 4
| Milestone | Cohort 1 | Cohort 2 | Cohort 3 |
|---|---|---|---|
| Started | 10 | 11 | 8 |
| Period 1 | 7 | 8 | 8 |
| Period 2 | 7 | 7 | 0 |
| Period 3 | 8 | 8 | 0 |
| Period 4 | 8 | 8 | 0 |
| Completed | 8 | 7 | 0 |
| Not completed | 2 | 4 | 8 |
| Withdrew: Study terminated by sponsor | 0 | 0 | 8 |
| Withdrew: Withdrawal by subject | 2 | 3 | 0 |
| Withdrew: Lost to follow-up | 0 | 1 | 0 |
An adverse event (AE) was any untoward medical occurrence in a patient or clinical study subject, temporally associated with the use of study intervention, whether or not considered related to the study intervention. A serious AE (SAE) was defined as any untoward medical occurrence that, at any dose: resulted in death; was life-threatening; required inpatient hospitalization or prolongation of existing hospitalization; resulted in persistent disability/incapacity; was a congenital anomaly/birth defect; or other serious situations such as important medical events. TEAEs were events between first dose of study drug and up to follow-up visit that were absent before treatment or that worsened after treatment. AEs presented below were TEAEs. The investigator was required to use clinical judgment to assess the potential relationship between investigational product and each AE, to define an treatment-related AE.
| Participants | Pooled Placebo | PF-07258669 0.1mg | PF-07258669 0.3mg | PF-07258669 1mg | PF-07258669 3mg | PF-07258669 10mg | PF-07258669 30mg | PF-07258669 100mg | PF-07258669 200mg | PF-07258669 300mg |
|---|---|---|---|---|---|---|---|---|---|---|
| All-causality TEAEs | 6 | 0 | 0 | 1 | 2 | 1 | 2 | 3 | 1 | 2 |
| Treatment-related TEAEs | 1 | 0 | 0 | 0 | 1 | 0 | 1 | 1 | 1 | 0 |
Safety laboratory assessments included clinical chemistry, hematology, urinalysis, and other tests. Abnormality was determined at the investigator's discretion.
| Participants | Pooled Placebo | PF-07258669 0.1mg | PF-07258669 0.3mg | PF-07258669 1mg | PF-07258669 3mg | PF-07258669 10mg | PF-07258669 30mg | PF-07258669 100mg | PF-07258669 200mg | PF-07258669 300mg |
|---|---|---|---|---|---|---|---|---|---|---|
| Number of Participants With Clinical Laboratory Abnormalities (Without Regard to Baseline [BL] Abnormality) | 14 | 5 | 3 | 4 | 4 | 6 | 5 | 6 | 6 | 3 |
Abnormality in change from BL in vital signs included: standing diastolic blood pressure (BP) increase and decrease from BL of \>=20mmHg, standing systolic BP increase and decrease from BL of \>=30mmHg, supine diastolic BP increase and decrease from BL of \>=20mmHg, supine systolic BP increase and decrease from BL of \>=30mmHg.
| Participants | Pooled Placebo | PF-07258669 0.1mg | PF-07258669 0.3mg | PF-07258669 1mg | PF-07258669 3mg | PF-07258669 10mg | PF-07258669 30mg | PF-07258669 100mg | PF-07258669 200mg | PF-07258669 300mg |
|---|---|---|---|---|---|---|---|---|---|---|
| Standing diastolic BP increase >=20mmHg | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Standing diastolic BP decrease >=20mmHg | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 |
| Standing systolic BP increase >=30mmHg | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 1 |
| Standing systolic BP decrease >=30mmHg | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 |
| Supine diastolic BP increase >=20mmHg | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Supine diastolic BP decrease >=20mmHg | 1 | 0 | 0 | 1 | 0 | 0 | 0 | 1 | 0 | 0 |
| Supine systolic BP increase >=30mmHg | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Supine systolic BP decrease >=30mmHg | 1 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 1 | 1 |
ECG assessments inlcuded PR, QT, QTcF intervals and QRS complex. ECG abnormalities in change from BL included: PR interval BL \>200msec and max \>=25% increase from BL, or BL \<=200msec and max \>=50% increase from BL, QRS interval percent change from BL \>=50%, QTcF change from BL \>=30 and \<=60msec, or change from BL \>60msec.
| Participants | Pooled Placebo | PF-07258669 0.1mg | PF-07258669 0.3mg | PF-07258669 1mg | PF-07258669 3mg | PF-07258669 10mg | PF-07258669 30mg | PF-07258669 100mg | PF-07258669 200mg | PF-07258669 300mg |
|---|---|---|---|---|---|---|---|---|---|---|
| PR interval %change >=25/50% (BL >200msec and >=25% increase or BL <=200msec and >=50% increase) | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| QRS interval %change >=50% | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| QTcF change >=30 and <=60msec | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| QTcF change >60msec | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
The neurological exam consisted of assessment of higher cortical function, the cranial nerves, motor function, deep tendon reflexes, sensory exam, and coordination and gait, to the extent needed to assess the participant for any potential changes in neurological status, as determined by the investigator (or designee).
| Participants | Pooled Placebo | PF-07258669 0.1mg | PF-07258669 0.3mg | PF-07258669 1mg | PF-07258669 3mg | PF-07258669 10mg | PF-07258669 30mg | PF-07258669 100mg | PF-07258669 200mg | PF-07258669 300mg |
|---|---|---|---|---|---|---|---|---|---|---|
| Number of Participants With Clinically-significant Change From BL in Neurological Examination Findings | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
Cmax is the maximum observed plasma concentration.
| nanogram per milliliter (ng/mL) | PF-07258669 0.1mg | PF-07258669 0.3mg | PF-07258669 1mg | PF-07258669 3mg | PF-07258669 10mg | PF-07258669 30mg | PF-07258669 100mg | PF-07258669 200mg | PF-07258669 300mg |
|---|---|---|---|---|---|---|---|---|---|
| Maximum Observed Concentration (Cmax) of PF-07258669 | 0.8439 ± 13 | 3.053 ± 35 | 10.72 ± 40 | 26.48 ± 35 | 53.30 ± 24 | 188.1 ± 3 | 573.4 ± 45 | 1173 ± 41 | 1604 ± 64 |
AUClast is the area under the plasma concentration-time profile from time 0 to the time of the last quantifiable concentration.
| nanogram*hour per milliliter (ng*hr/mL) | PF-07258669 0.1mg | PF-07258669 0.3mg | PF-07258669 1mg | PF-07258669 3mg | PF-07258669 10mg | PF-07258669 30mg | PF-07258669 100mg | PF-07258669 200mg | PF-07258669 300mg |
|---|---|---|---|---|---|---|---|---|---|
| Area Under the Plasma Concentration-time Profile From Time 0 to the Time of the Last Quantifiable Concentration (AUClast) of PF-07258669 | 2.421 ± 13 | 7.826 ± 30 | 27.83 ± 27 | 75.84 ± 29 | 182.2 ± 16 | 584.8 ± 11 | 2148 ± 12 | 4013 ± 21 | 5764 ± 34 |
AUCinf is the area under the plasma concentration time profile from time 0 extrapolated to infinite time.
| nanogram*hour per milliliter (ng*hr/mL) | PF-07258669 0.1mg | PF-07258669 0.3mg | PF-07258669 1mg | PF-07258669 3mg | PF-07258669 10mg | PF-07258669 30mg | PF-07258669 100mg | PF-07258669 200mg | PF-07258669 300mg |
|---|---|---|---|---|---|---|---|---|---|
| Area Under the Plasma Concentration Time Profile From Time 0 Extrapolated to Infinite Time (AUCinf) of PF-07258669 | 2.659 ± 14 | 8.252 ± 28 | 28.55 ± 28 | 76.63 ± 28 | 183.0 ± 15 | 586.9 ± 11 | 2156 ± 12 | 4033 ± 21 | 6036 ± 32 |
Tmax is the time for Cmax.
| hour | PF-07258669 0.1mg | PF-07258669 0.3mg | PF-07258669 1mg | PF-07258669 3mg | PF-07258669 10mg | PF-07258669 30mg | PF-07258669 100mg | PF-07258669 200mg | PF-07258669 300mg |
|---|---|---|---|---|---|---|---|---|---|
| Time for Cmax (Tmax) of PF-07258669 | 1.00 (1.00 to 1.50) | 1.00 (0.500 to 1.00) | 0.750 (0.500 to 1.00) | 0.750 (0.500 to 1.00) | 1.00 (0.500 to 1.00) | 1.00 (1.00 to 1.00) | 1.00 (0.500 to 1.50) | 1.25 (1.00 to 2.00) | 1.00 (0.500 to 1.50) |
t1/2 is the terminal half-life.
| hour | PF-07258669 0.1mg | PF-07258669 0.3mg | PF-07258669 1mg | PF-07258669 3mg | PF-07258669 10mg | PF-07258669 30mg | PF-07258669 100mg | PF-07258669 200mg | PF-07258669 300mg |
|---|---|---|---|---|---|---|---|---|---|
| Terminal Half-life (t1/2) of PF-07258669 | 2.508 ± 0.92446 | 3.828 ± 0.92253 | 4.572 ± 0.93360 | 5.013 ± 0.52812 | 5.558 ± 0.78987 | 6.698 ± 1.6508 | 6.415 ± 1.5912 | 6.880 ± 1.9697 | 12.99 ± 10.045 |
Collected over From first dose of study intervention (Day 1) to telephone Follow Up (28-35 days after lase dose of study intervention) (approximately up to 20 weeks). Non-serious events are listed at a 5% frequency threshold.
| Group | Deaths | Serious | Other |
|---|---|---|---|
| Pooled Placebo | 0/18 (0%) | 0/18 (0%) | 6/18 (33.3%) |
| PF-07258669 0.1mg | 0/5 (0%) | 0/5 (0%) | 0/5 (0%) |
| PF-07258669 0.3mg | 0/5 (0%) | 0/5 (0%) | 0/5 (0%) |
| PF-07258669 1mg | 0/6 (0%) | 0/6 (0%) | 1/6 (16.7%) |
| PF-07258669 3mg | 0/6 (0%) | 0/6 (0%) | 2/6 (33.3%) |
| PF-07258669 10mg | 0/6 (0%) | 0/6 (0%) | 1/6 (16.7%) |
| PF-07258669 30mg | 0/5 (0%) | 0/5 (0%) | 2/5 (40%) |
| PF-07258669 100mg | 0/6 (0%) | 0/6 (0%) | 3/6 (50%) |
| PF-07258669 200mg | 0/6 (0%) | 0/6 (0%) | 1/6 (16.7%) |
| PF-07258669 300mg | 0/6 (0%) | 0/6 (0%) | 2/6 (33.3%) |
| Event | Pooled Placebo | PF-07258669 0.1mg | PF-07258669 0.3mg | PF-07258669 1mg | PF-07258669 3mg | PF-07258669 10mg | PF-07258669 30mg | PF-07258669 100mg | PF-07258669 200mg | PF-07258669 300mg |
|---|---|---|---|---|---|---|---|---|---|---|
| Upper respiratory tract infectionInfections and infestations | 0/18 | 0/5 | 0/5 | 0/6 | 0/6 | 0/6 | 0/5 | 2/6 | 0/6 | 0/6 |
| Blood triglycerides increasedInvestigations | 1/18 | 0/5 | 0/5 | 0/6 | 0/6 | 0/6 | 1/5 | 1/6 | 1/6 | 0/6 |
| Dermatitis contactSkin and subcutaneous tissue disorders | 1/18 | 0/5 | 0/5 | 0/6 | 0/6 | 1/6 | 1/5 | 0/6 | 0/6 | 0/6 |
| Atrioventricular block first degreeCardiac disorders | 0/18 | 0/5 | 0/5 | 1/6 | 0/6 | 0/6 | 0/5 | 0/6 | 0/6 | 0/6 |
| PalpitationsCardiac disorders | 0/18 | 0/5 | 0/5 | 0/6 | 0/6 | 0/6 | 0/5 | 0/6 | 0/6 | 1/6 |
| SARS-CoV-2 test positiveInvestigations | 0/18 | 0/5 | 0/5 | 0/6 | 0/6 | 0/6 | 0/5 | 0/6 | 0/6 | 1/6 |
| DermatitisSkin and subcutaneous tissue disorders | 0/18 | 0/5 | 0/5 | 0/6 | 1/6 | 0/6 | 0/5 | 0/6 | 0/6 | 0/6 |
| Orthostatic hypotensionVascular disorders | 0/18 | 0/5 | 0/5 | 0/6 | 1/6 | 0/6 | 0/5 | 0/6 | 0/6 | 0/6 |
| NauseaGastrointestinal disorders | 1/18 | 0/5 | 0/5 | 0/6 | 0/6 | 0/6 | 0/5 | 0/6 | 0/6 | 0/6 |
| Noninfective gingivitisGastrointestinal disorders | 1/18 | 0/5 | 0/5 | 0/6 | 0/6 | 0/6 | 0/5 | 0/6 | 0/6 | 0/6 |
All randomized participants who received a dose of study intervention
| Age, Continuous(Years) | Cohort 1 | Cohort 2 | Cohort 3 | Total |
|---|---|---|---|---|
| Median | 39.5 (23.0 to 54.0) | 42.0 (34.0 to 52.0) | 32.5 (20.0 to 56.0) | 40.0 (20.0 to 56.0) |
| Age, Customized(Participants) | Cohort 1 | Cohort 2 | Cohort 3 | Total |
|---|---|---|---|---|
| 18-44 Years | 6 | 8 | 5 | 19 |
| 45-60 Years | 4 | 3 | 3 | 10 |
| Sex: Female, Male(Participants) | Cohort 1 | Cohort 2 | Cohort 3 | Total |
|---|---|---|---|---|
| Female | 3 | 2 | 4 | 9 |
| Male | 7 | 9 | 4 | 20 |
| Race/Ethnicity, Customized(Participants) | Cohort 1 | Cohort 2 | Cohort 3 | Total |
|---|---|---|---|---|
| White | 9 | 10 | 7 | 26 |
| Black or African American | 1 | 1 | 1 | 3 |
Documents are hosted by the registry — open the source record to download them.
Plan to share: No — 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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