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PF-07612577

Phase 1

Healthy | Small molecule | Other |Pfizer, Inc.|Last Updated: Oct 10, 2024

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Trial Design

RandomizedDouble-BlindPLACEBO_CONTROLLEDDMC
Total Trials1
Total Enrollment42

FDA Designations

No designations recorded

Clinical trial landscape

PF-07612577 · 1 trial · 1 indication

Phase 1 1
NCT05554237A Study to Learn About the Study Medicine Called CTB+AVP in Healthy Adult People.Healthy
COMPLETED42 Analytics
PHASE1COMPLETED
A Study to Learn About the Study Medicine Called CTB+AVP in Healthy Adult People.
HealthyUnlock trial analytics

Study Endpoints

Primary Endpoints

Maximum Observed Concentration (Cmax) of Cis-Ceftibuten (CTB): Part 1
pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,14 and 24 hours post dose
Time for Cmax (Tmax) of CTB: Part 1
pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,14 and 24 hours post dose
Area Under the Plasma Concentration Time Curve From Time Zero to the Time of Last Quantifiable Concentration (AUClast) of CTB: Part 1
pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,14 and 24 hours post dose

AUClast was determined using the linear/log trapezoidal method.

Dose-Normalized Cmax (Cmax[dn]) of CTB: Part 1
pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,14 and 24 hours post dose

Dose-normalized Cmax was determined as Cmax/Dose.

Dose-Normalized AUClast (AUClast[dn]) of CTB: Part 1
pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,14 and 24 hours post dose

AUClast(dn) was determined as AUClast/Dose.

Area Under the Plasma Concentration-Time Curve From Time Zero Extrapolated to Infinity (AUCinf) of CTB: Part 1
pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,14 and 24 hours post dose

AUCinf was calculated as AUClast + (Clast/kel), where Clast is the predicted plasma concentration at the last quantifiable time point from the log-linear regression analysis.

Dose-Normalized AUCinf (AUCinf[dn]) of CTB: Part 1
pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,14 and 24 hours post dose

AUCinf(dn) was calculated as AUCinf/Dose.

Terminal Half-Life (t1/2) of CTB: Part 1
pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,14 and 24 hours post dose

T1/2 was calculated as loge(2)/kel, where kel is the terminal phase rate constant calculated by a linear regression of the log-linear concentration-time curve.

Apparent Volume of Distribution (Vz/F) of CTB: Part 1
pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,14 and 24 hours post dose

Vz/F was calculated as Dose/(AUCinf \* kel) where kel is the terminal phase rate constant calculated by a linear regression of the log-linear concentration-time curve.

Apparent Clearance (CL/F) of CTB: Part 1
pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,14 and 24 hours post dose

CL/F was calculated as Dose/AUCinf.

Maximum Observed Concentration (Cmax) of AVP, Avibactam (AVI) and Hydroxy Pivalic Acid (HPA): Part 1
pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,14 and 24 hours post dose

The lower limit of quantification for AVP was 1.0 ng/mL.

Dose-Normalized AUClast (AUClast[dn]) of AVP, AVI and HPA: Part 1
pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,14 and 24 hours post dose

AUClast(dn) was determined as AUClast/Dose. The lower limit of quantification for AVP was 1.0 ng/mL.

Time for Cmax (Tmax) of AVP, AVI and HPA: Part 1
pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,14 and 24 hours post dose

The lower limit of quantification for AVP was 1.0 ng/mL.

Dose-Normalized Cmax (Cmax[dn]) of AVP, AVI and HPA: Part 1
pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,14 and 24 hours post dose

Dose-normalized Cmax was determined as Cmax/Dose. The lower limit of quantification for AVP was 1.0 ng/mL.

Area Under the Plasma Concentration Time Curve From Time Zero to the Time of Last Quantifiable Concentration (AUClast) of AVP, AVI and HPA: Part 1
pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,14 and 24 hours post dose

AUClast was determined using the linear/log trapezoidal method. The lower limit of quantification for AVP was 1.0 ng/mL.

Area Under the Plasma Concentration-Time Curve From Time Zero Extrapolated to Infinity (AUCinf) of AVP, AVI and HPA: Part 1
pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,14 and 24 hours post dose

AUCinf was calculated as AUClast + (Clast/kel), where Clast is the predicted plasma concentration at the last quantifiable time point from the log-linear regression analysis.

Dose-Normalized AUCinf (AUCinf[dn]) of AVP, AVI and HPA: Part 1
pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,14 and 24 hours post dose

AUCinf(dn) was calculated as AUCinf/Dose.

Terminal Half-Life (t1/2) of AVP, AVI and HPA: Part 1
pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,14 and 24 hours post dose

T1/2 was calculated as loge(2)/kel, where kel is the terminal phase rate constant calculated by a linear regression of the log-linear concentration-time curve.

Apparent Volume of Distribution (Vz/F) of AVP, AVI and HPA : Part 1
pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,14 and 24 hours post dose

Vz/F was calculated as Dose/(AUCinf \* kel) where kel is the terminal phase rate constant calculated by a linear regression of the log-linear concentration-time curve.

Apparent Clearance (CL/F) of AVP, AVI and HPA: Part 1
pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,14 and 24 hours post dose

CL/F was calculated as Dose/AUCinf.

Number of Participants With Treatment Emergent Adverse Events (TEAEs), Severe TEAEs and Related TEAEs: Part 1
From start of treatment up to 28 to 35 days post last dose of study intervention (approximately 52 days)

An adverse event (AE) was any untoward medical occurrence in a participant, temporally associated with the use of study intervention, whether or not considered related to the study intervention. TEAEs were are any untoward medical incidence in a participant during administered study intervention, whether or not these events are related to study intervention. Severe TEAEs were defined as type of AE that interrupted usual activities of daily life (ADL), or significantly affects clinical status, or may require intensive therapeutic intervention. Related TEAEs are defined as all TEAEs considered by the investigator to have at least a 'possible' relationship with the study intervention.

Number of Participants With Withdrawals Due to TEAEs: Part 1
From start of treatment up to 28 to 35 days post last dose of study intervention (approximately 52 days)

An AE was any untoward medical occurrence in a participant, temporally associated with the use of study intervention, whether or not considered related to the study intervention. TEAEs were are any untoward medical incidence in a participant during administered study intervention, whether or not these events are related to study intervention.

Number of Participants With Laboratory Test Abnormalities: Part 1
Up to 24 hours post-dose

The laboratory abnormalities with non-zero participants were reported and it included: monocytes or leukocytes (greater than \[\>\] 1.2\* upper limit of normal \[ULN\]), urine hemoglobin scalar (greater than or equal to \[\>=1\]) and leukocyte esterase scalar (\>=1).

Number of Participants With Clinically Significant Changes in Vital Signs Abnormalities: Part 1
Up to 24 hours post-dose

Vital signs included blood pressure and pulse rate and were measured in a supine position after approximately 5 minutes of rest for the participant. Clinically significant changes in vital signs were determined by the investigator.

Number of Participants With Electrocardiogram (ECG) Abnormalities: Part 1
Up to 24 hours post-dose

Twelve lead ECGs were collected using an ECG machine that automatically calculated heart rate and measured PR interval, QRS duration, QT interval, QT interval correct by Bazzette's formula (QTcB) and QT interval correct by Frederica formula QTcF. ECG abnormalities included: PR interval aggregate (millisecond \[msec\], maximum \[max.\] \>=300; baseline \> 200 and max. increase \>= 25 percent (%); baseline \> 200 and max. increase \>= 25%), QRS duration aggregate (msec, max \>=140; max. increase \>= 50%), QT interval aggregate (msec, value \> 500), QTCB interval aggregate and QTCF interval aggregate (msec, 450 \< max \<= 480; 480 \< max. \<= 500; max. \> 500; 30 \< max. increase \<= 60; max. increase \> 60).

Maximum Observed Concentration (Cmax) of Cis-CTB and Trans-CTB: Part 2
pre-dose,0.5,1,1.5,2,2.5,3,4,6 and 8 hours post dose on Day 1 and 6; pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,16 and 24 hours post dose on Day 7
Time for Cmax (Tmax) of Cis-CTB and Trans-CTB: Part 2
pre-dose,0.5,1,1.5,2,2.5,3,4,6 and 8 hours post dose on Day 1 and 6; pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,16 and 24 hours post dose on Day 7
Area Under the Plasma Concentration Time Curve From Time Zero to Time Tau, the Dosing Interval (AUCtau) of Cis-CTB and Trans-CTB: Part 2
pre-dose,0.5,1,1.5,2,2.5,3,4,6 and 8 hours post dose on Day 1 and 6; pre-dose,0.5,1,1.5,2,2.5,3,4,6 and 8 hours post dose on Day 7

Area under the plasma concentration time profile from time zero to time tau, the dosing interval, where tau is equal to 8 hours for three times daily (TID) dosing.

Dose-Normalized Cmax (Cmax[dn]) of Cis-CTB and Trans-CTB : Part 2
pre-dose,0.5,1,1.5,2,2.5,3,4,6 and 8 hours post dose on Day 1 and 6; pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,16 and 24 hours post dose on Day 7

Dose-normalized Cmax was determined as Cmax/Dose.

Dose-Normalized AUCtau (AUCtau[dn]) of Cis-CTB and Trans-CTB: Part 2
pre-dose,0.5,1,1.5,2,2.5,3,4,6 and 8 hours post dose on Day 1 and 6; pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,16 and 24 hours post dose on Day 7

Area under the plasma concentration time profile from time zero to time tau, the dosing interval, where tau is equal to 8 hours for three times daily (TID) dosing.

Terminal Half-Life (t1/2) of Cis-CTB and Trans-CTB on Day 7: Part 2
pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,16 and 24 hours post dose on Day 7

T1/2 was calculated as loge(2)/kel, where kel is the terminal phase rate constant calculated by a linear regression of the log-linear concentration-time curve.

Apparent Volume of Distribution (Vz/F) of Cis-CTB and Trans-CTB : Part 2
pre-dose,0.5,1,1.5,2,2.5,3,4,6 and 8 hours post dose on Day 1 and 6; pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,16 and 24 hours post dose on Day 7

Vz/F was calculated as Dose/(AUCinf \* kel) where kel is the terminal phase rate constant calculated by a linear regression of the log-linear concentration-time curve.

Apparent Clearance (CL/F) of Cis-CTB and Trans-CTB: Part 2
pre-dose,0.5,1,1.5,2,2.5,3,4,6 and 8 hours post dose on Day 1 and 6; pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,16 and 24 hours post dose on Day 7

CL/F was calculated as Dose/AUCinf.

Maximum Observed Concentration (Cmax) of AVP, AVI and HPA: Part 2
pre-dose,0.5,1,1.5,2,2.5,3,4,6 and 8 hours post dose on Day 1 and 6; pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,16 and 24 hours post dose on Day 7

The lower limit of quantification for AVP was 1.0 ng/mL.

Area Under the Plasma Concentration Time Curve From Time Zero to Time Tau, the Dosing Interval (AUCtau) of AVP, AVI and HPA: Part 2
pre-dose,0.5,1,1.5,2,2.5,3,4,6 and 8 hours post dose on Day 1 and 6; pre-dose,0.5,1,1.5,2,2.5,3,4,6 and 8 hours post dose on Day 7

Area under the plasma concentration time profile from time zero to time tau, the dosing interval, where tau is equal to 8 hours for three times daily (TID) dosing.

Time for Cmax (Tmax) of AVP, AVI and HPA: Part 2
pre-dose,0.5,1,1.5,2,2.5,3,4,6 and 8 hours post dose on Day 1 and 6; pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,16 and 24 hours post dose on Day 7

The lower limit of quantification for AVP was 1.0 ng/mL.

Dose-Normalized Cmax (Cmax[dn]) of AVP, AVI and HPA: Part 2
pre-dose,0.5,1,1.5,2,2.5,3,4,6 and 8 hours post dose on Day 1 and 6; pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,16 and 24 hours post dose on Day 7

Dose-normalized Cmax was determined as Cmax/Dose. The lower limit of quantification for AVP was 1.0 ng/mL.

Dose-Normalized AUCtau (AUCtau[dn]) of AVP, AVI and HPA: Part 2
pre-dose,0.5,1,1.5,2,2.5,3,4,6 and 8 hours post dose on Day 1 and 6; pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,16 and 24 hours post dose on Day 7

Area under the plasma concentration time profile from time zero to time tau, the dosing interval, where tau is equal to 8 hours for three times daily (TID) dosing.

Terminal Half-Life (t1/2) of AVP, AVI and HPA on Day 7: Part 2
pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,16 and 24 hours post dose on day 7

T1/2 was calculated as loge(2)/kel, where kel is the terminal phase rate constant calculated by a linear regression of the log-linear concentration-time curve. The lower limit of quantification for HPA was 10.0 ng/mL.

Apparent Volume of Distribution (Vz/F) of AVP, AVI and HPA: Part 2
pre-dose,0.5,1,1.5,2,2.5,3,4,6 and 8 hours post dose on Day 1 and 6; pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,16 and 24 hours post dose on Day 7

Vz/F was calculated as Dose/(AUCinf \* kel) where kel is the terminal phase rate constant calculated by a linear regression of the log-linear concentration-time curve. The lower limit of quantification for AVI and HPA was 10.0 ng/mL.

Apparent Clearance (CL/F) of AVP, AVI and HPA: Part 2
pre-dose,0.5,1,1.5,2,2.5,3,4,6 and 8 hours post dose on Day 1 and 6; pre-dose,0.5,1,1.5,2,2.5,3,4,6,8,12,16 and 24 hours post dose on Day 7

CL/F was calculated as Dose/AUCinf.

Number of Participants With TEAEs, Severe TEAEs and Related TEAEs: Part 2
From start of treatment up to 28 to 35 days post last dose of study intervention (approximately 42 days)

An AE was any untoward medical occurrence in a participant, temporally associated with the use of study intervention, whether or not considered related to the study intervention. TEAEs were are any untoward medical incidence in a participant during administered study intervention, whether or not these events are related to study intervention. Severe TEAEs were defined as type of AE that interrupted usual ADL, or significantly affects clinical status, or may require intensive therapeutic intervention. Related TEAEs are defined as all TEAEs considered by the investigator to have at least a 'possible' relationship with the study intervention.

Number of Participants With Withdrawals Due to TEAEs: Part 2
From start of treatment up to 28 to 35 days post last dose of study intervention (approximately 42 days)

An AE was any untoward medical occurrence in a participant, temporally associated with the use of study intervention, whether or not considered related to the study intervention. TEAEs were any untoward medical incidence in a participant during administered study intervention, whether or not these events are related to study intervention.

Number of Participants With Laboratory Test Abnormalities: Part 2
From start of treatment up to Day 7

The laboratory abnormalities with non-zero participants were reported and it included: neutrophils/ leukocytes (less than \[\<\] 0.8x lower limit of normal \[LLN\]), eosinophils/leukocytes (\>1.2x ULN), monocytes/leukocytes (\>1.2x ULN), bicarbonate (\>1.1x ULN), urine glucose (\>=1), ketones scalar (\>=1), urine hemoglobin scalar (\>=1), leukocyte esterase scalar (\>=1).

Number of Participants With Clinically Significant Changes in Vital Signs Abnormalities: Part 2
From start of treatment up to Day 7

Vital signs included blood pressure and pulse rate and were measured in a supine position after approximately 5 minutes of rest for the participant. Clinically significant changes in vital signs were determined by the investigator.

Number of Participants With Electrocardiogram (ECG) Abnormalities: Part 2
From start of treatment up to Day 7

Twelve lead ECGs were collected using an ECG machine that automatically calculated heart rate and measured PR interval, QRS duration, QT interval, QT interval correct by Bazzette's formula (QTcB) and QT interval correct by Frederica formula QTcF. ECG abnormalities included: PR interval aggregate (millisecond \[msec\], maximum \[max.\] \>=300; baseline \> 200 and max. increase \>= 25 percent (%); baseline \> 200 and max. increase \>= 25%), QRS duration aggregate (msec, max \>=140; max. increase \>= 50%), QT interval aggregate (msec, value \> 500), QTCB interval aggregate and QTCF interval aggregate (msec, 450 \< max \<= 480; 480 \< max. \<= 500; max. \> 500; 30 \< max. increase \<= 60; max. increase \> 60).

Secondary Endpoints

Amount Excreted in Urine as Unchanged Drug Over the Dosing Interval Tau (Aetau) of Cis-CTB, Trans-CTB, AVP, AVI and HPA: Part 2
anytime between 0 to 8 hours post dose on Day 6
Percent of Dose Excreted in Urine as Unchanged Drug Over the Dosing Interval Tau (Aetau%) of Cis-CTB, Trans-CTB, AVP, AVI and HPA: Part 2
anytime between 0 to 8 hours post dose on Day 6
Renal Clearance (CLr) of Cis-CTB, Trans-CTBa, AVP, AVI and HPA: Part 2
anytime between 0 to 8 hours post dose on Day 6
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Study Design & Arms

AllocationRANDOMIZED
MaskingDOUBLE
ModelSEQUENTIAL
PurposeBASIC_SCIENCE

Treatment Arms

ArmTypeDescription
PF-07612577EXPERIMENTALPart-1: Dose 1, Dose 2, Dose 4, Dose 5 Part-2: Cohort 2-5
PlaceboPLACEBO_COMPARATORPart-1: Dose 1-5 Part-2: Cohort 2-4
PF-06264006EXPERIMENTALPart-1: Dose 3, Dose 5

Interventions

NameTypeDescription
PlaceboDRUGPlacebo
PF-07612577DRUGPF-07612577
PF-06264006DRUGPF-06264006
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Eligibility Criteria

Age Range18 Years to 60 Years
SexALL
Healthy VolunteersYes
Study Sites1

Inclusion Criteria: 1. BMI of 17.5 to 30.5 kg/m2; and a total body weight \>50 kg (110 lb) 2. For optional Japanese cohort only: Japanese participants who have 4 Japanese biologic grandparents who were born in Japan 3. For optional Chinese cohort only: Chinese participants who were born in mainland...

Countries:Belgium
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Frequently asked questions about PF-07612577

What is PF-07612577?

PF-07612577 is an investigational small molecule being developed by Pfizer, Inc. (PFE). It is currently in Phase 1 clinical development. The drug is being studied in healthy adult volunteers, and it is not yet approved by regulatory authorities.

What is PF-07612577 used for?

PF-07612577 is being studied for use in healthy adult volunteers. The Phase 1 clinical trial is designed to evaluate the study medicine in this population. It is an investigational drug, meaning it is not yet approved for any medical condition.

Who makes PF-07612577?

PF-07612577 is being developed by Pfizer, Inc., a biopharmaceutical company traded on the New York Stock Exchange under the ticker symbol PFE. The drug is currently in Phase 1 clinical development.

What phase is PF-07612577 in?

PF-07612577 is in Phase 1 clinical development. The Phase 1 trial has been completed. The drug is investigational and has not been approved by the FDA or any other regulatory agency.

What clinical trials is PF-07612577 in?

PF-07612577 has one completed Phase 1 clinical trial, identified as NCT05554237. This trial was a randomized, double-blind, placebo-controlled study conducted in Belgium, enrolling 42 healthy adult participants aged 18 years and older.

Is PF-07612577 the same as CTB+AVP?

PF-07612577 is the study medicine referred to as CTB+AVP in the clinical trial titled "A Study to Learn About the Study Medicine Called CTB+AVP in Healthy Adult People." The trial identifier NCT05554237 corresponds to this study.