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Phase 1 N=8 Randomized Double-blind Basic Science

A Study to Learn About the Study Medicine Called CTB+AVP in Healthy Adult People.

Healthy

Enrolled (actual)
8
Serious AEs
0.0%
Results posted
Oct 2024
Primary outcome: Primary: Maximum Observed Concentration (Cmax) of Cis-Ceftibuten (CTB): Part 1 — 18170; 25470; 30510; 27120 Nanogram per milliliter (ng/mL)

Study Design & Population

Study type
Interventional
Phase
Phase 1
Interventions
Placebo (Drug); PF-07612577 (Drug); PF-06264006 (Drug)
Age
Adult · 18+ yrs
Sex
All
Sponsor
Pfizer
Primary completion
Jun 2023

Outcome Measures

OutcomeResultp-value
PRIMARY
Maximum Observed Concentration (Cmax) of Cis-Ceftibuten (CTB): Part 1
18170; 25470; 30510; 27120; 44990
PRIMARY
Time for Cmax (Tmax) of CTB: Part 1
3.21; 4.03; 3.50; 5.05; 4.01
PRIMARY
Area Under the Plasma Concentration Time Curve From Time Zero to the Time of Last Quantifiable Concentration (AUClast) of CTB: Part 1
94050; 154100; 171800; 183600; 319200
PRIMARY
Dose-Normalized Cmax (Cmax[dn]) of CTB: Part 1
45.45; 31.83; 38.16; 22.61; 28.12
PRIMARY
Dose-Normalized AUClast (AUClast[dn]) of CTB: Part 1
235.2; 192.9; 214.9; 152.9; 199.6
PRIMARY
Area Under the Plasma Concentration-Time Curve From Time Zero Extrapolated to Infinity (AUCinf) of CTB: Part 1
94730; 155800; 173200; 184900; 321900
PRIMARY
Dose-Normalized AUCinf (AUCinf[dn]) of CTB: Part 1
236.9; 194.6; 216.7; 153.8; 200.9
PRIMARY
Terminal Half-Life (t1/2) of CTB: Part 1
3.073; 2.708; 2.908; 3.138; 3.180
PRIMARY
Apparent Volume of Distribution (Vz/F) of CTB: Part 1
18.44; 19.70; 19.10; 29.28; 22.72
PRIMARY
Apparent Clearance (CL/F) of CTB: Part 1
4.221; 5.136; 4.620; 6.492; 4.973
PRIMARY
Maximum Observed Concentration (Cmax) of AVP, Avibactam (AVI) and Hydroxy Pivalic Acid (HPA): Part 1
NA; NA; NA; 3856; 5955; 6714
PRIMARY
Dose-Normalized AUClast (AUClast[dn]) of AVP, AVI and HPA: Part 1
NA; NA; NA; 36.10; 40.91; 41.67
PRIMARY
Time for Cmax (Tmax) of AVP, AVI and HPA: Part 1
NA; NA; 4.01; 3.50; 4.50; 4.01
PRIMARY
Dose-Normalized Cmax (Cmax[dn]) of AVP, AVI and HPA: Part 1
NA; NA; NA; 6.388; 6.583; 7.422
PRIMARY
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
NA; NA; NA; 21760; 37000; 37680
PRIMARY
Area Under the Plasma Concentration-Time Curve From Time Zero Extrapolated to Infinity (AUCinf) of AVP, AVI and HPA: Part 1
22050; 38060; 38090; 10220; 18440; 17950
PRIMARY
Dose-Normalized AUCinf (AUCinf[dn]) of AVP, AVI and HPA: Part 1
36.58; 42.10; 42.11; 37.86; 45.59; 44.35
PRIMARY
Terminal Half-Life (t1/2) of AVP, AVI and HPA: Part 1
4.043; 5.302; 3.632; 4.218; 5.347; 3.853
PRIMARY
Apparent Volume of Distribution (Vz/F) of AVP, AVI and HPA : Part 1
154.6; 175.0; 121.5; 157.6; 163.2; 122.7
PRIMARY
Apparent Clearance (CL/F) of AVP, AVI and HPA: Part 1
27.35; 23.75; 23.75; 26.44; 21.92; 22.53
PRIMARY
Number of Participants With Treatment Emergent Adverse Events (TEAEs), Severe TEAEs and Related TEAEs: Part 1
2; 0; 3; 1; 0; 0
PRIMARY
Number of Participants With Withdrawals Due to TEAEs: Part 1
0; 0; 0; 0; 0; 0
PRIMARY
Number of Participants With Laboratory Test Abnormalities: Part 1
1; 0; 0; 1; 0; 1
PRIMARY
Number of Participants With Clinically Significant Changes in Vital Signs Abnormalities: Part 1
0; 0; 0; 0; 0; 0
PRIMARY
Number of Participants With Electrocardiogram (ECG) Abnormalities: Part 1
0; 0; 0; 0; 0; 0
PRIMARY
Maximum Observed Concentration (Cmax) of Cis-CTB and Trans-CTB: Part 2
14610; 22730; 17270; 22630; 45640; 20680
PRIMARY
Time for Cmax (Tmax) of Cis-CTB and Trans-CTB: Part 2
2.54; 3.53; 2.53; 2.80; 3.53; 3.28
PRIMARY
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
64640; 113100; 67730; 104200; 224300; 93590
PRIMARY
Dose-Normalized Cmax (Cmax[dn]) of Cis-CTB and Trans-CTB : Part 2
36.56; 28.43; 43.22; 56.59; 57.06; 51.72
PRIMARY
Dose-Normalized AUCtau (AUCtau[dn]) of Cis-CTB and Trans-CTB: Part 2
161.6; 141.6; 169.5; 260.4; 280.7; 234.2
PRIMARY
Terminal Half-Life (t1/2) of Cis-CTB and Trans-CTB on Day 7: Part 2
3.710; 3.930; 3.030; 4.040
PRIMARY
Apparent Volume of Distribution (Vz/F) of Cis-CTB and Trans-CTB : Part 2
16.5; 15.6; 15.37; 16.5; 11.5; 14.8
PRIMARY
Apparent Clearance (CL/F) of Cis-CTB and Trans-CTB: Part 2
4.61; 4.89; 5.014; 3.844; 3.579; 4.283
PRIMARY
Maximum Observed Concentration (Cmax) of AVP, AVI and HPA: Part 2
NA; NA; NA; NA; NA; NA
PRIMARY
Area Under the Plasma Concentration Time Curve From Time Zero to Time Tau, the Dosing Interval (AUCtau) of AVP, AVI and HPA: Part 2
29480; 27920; 22530; 39570; 45130; 29920
PRIMARY
Time for Cmax (Tmax) of AVP, AVI and HPA: Part 2
NA; 4.02; 4.00; 4.49; 2.77; 2.50
PRIMARY
Dose-Normalized Cmax (Cmax[dn]) of AVP, AVI and HPA: Part 2
NA; NA; NA; NA; NA; NA
PRIMARY
Dose-Normalized AUCtau (AUCtau[dn]) of AVP, AVI and HPA: Part 2
32.63; 30.88; 37.37; 43.77; 49.92; 49.62
PRIMARY
Terminal Half-Life (t1/2) of AVP, AVI and HPA on Day 7: Part 2
6.473; 8.165; 7.150; 6.270; NA; 5.965
PRIMARY
Apparent Volume of Distribution (Vz/F) of AVP, AVI and HPA: Part 2
63.23; NA; 58.04; 64.02; 228.7; 275.1
PRIMARY
Apparent Clearance (CL/F) of AVP, AVI and HPA: Part 2
30.65; 32.38; 26.76; 22.86; 20.02; 20.13
PRIMARY
Number of Participants With TEAEs, Severe TEAEs and Related TEAEs: Part 2
5; 2; 4; 1; 5; 2
PRIMARY
Number of Participants With Withdrawals Due to TEAEs: Part 2
2; 0; 0; 0; 0; 1
PRIMARY
Number of Participants With Laboratory Test Abnormalities: Part 2
0; 0; 0; 0; 1; 0
PRIMARY
Number of Participants With Clinically Significant Changes in Vital Signs Abnormalities: Part 2
0; 0; 0; 0; 0; 0
PRIMARY
Number of Participants With Electrocardiogram (ECG) Abnormalities: Part 2
0; 0; 0; 0; 0; 0
SECONDARY
Amount Excreted in Urine as Unchanged Drug Over the Dosing Interval Tau (Aetau) of Cis-CTB, Trans-CTB, AVP, AVI and HPA: Part 2
181.8; 48.23; 295.6; 22.01
SECONDARY
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
45.40; 12.08; 32.68; 5.434
SECONDARY
Renal Clearance (CLr) of Cis-CTB, Trans-CTBa, AVP, AVI and HPA: Part 2
2.501; 6.657; 10.61; 1.390
SECONDARY
Maximum Observed Concentration (Cmax) of Cis-CTB, AVP, AVI and HPA in Japanese and Chinese Cohorts: Part 2
13660; 19540; 22080; NA; 21330; NA
SECONDARY
Time for Cmax (Tmax) of Cis-CTB, AVP, AVI and HPA in Japanese and Chinese Cohorts: Part 2
4.03; 3.05; 3.03; NA; 2.03; NA
SECONDARY
Area Under the Plasma Concentration Time Curve From Time Zero to Time Tau, the Dosing Interval (AUCtau) of Cis-CTB, AVP, AVI and HPA in Japanese and Chinese Cohorts: Part 2
52630; 84790; 92920; NA; 90270; NA
SECONDARY
Dose-Normalized Cmax (Cmax[dn]) of Cis-CTB, AVP, AVI and HPA in Japanese and Chinese Cohorts: Part 2
34.16; 48.90; 55.21; NA; 53.35; NA
SECONDARY
Dose-Normalized AUCtau (AUCtau[dn]) of Cis-CTB, AVP, AVI and HPA in Japanese and Chinese Cohorts: Part 2
131.5; 212.0; 232.3; NA; 225.9; NA
SECONDARY
Terminal Half-Life (t1/2) of Cis-CTB, AVP, AVI and HPA in Japanese and Chinese Cohorts: Part 2
2.788; NA; 5.734; NA; 5.290; NA
SECONDARY
Apparent Volume of Distribution (Vz/F) of Cis-CTB, AVP, AVI and HPA in Japanese and Chinese Cohorts: Part 2
NA; 12.82; 17.33; NA; NA; NA
SECONDARY
Apparent Clearance (CL/F) of Cis-CTB, AVP, AVI and HPA in Japanese and Chinese Cohorts: Part 2
NA; 4.303; NA; 4.428; NA; 40.66

Summary

The purpose of this clinical trial is to learn about the pharmacokinetics, safety and tolerability of various single- and multiple-doses of CTB+AVP in healthy adult participants. CTB+AVP is a study medicine that is being developed to treat people with complicated urinary tract infections. This study is seeking healthy adult male and female participants, 18-60 years of age, with a body weight > 50 kg and a BMI of 17.5 to 30.5 kg/m2. Participants in Part-1 of the study will receive increasing single doses of CTB and/or AVP. Participants in Part-2 will receive increasing multiple doses of CTB+AVP three times a day for 7 days. The study team will monitor how each participant is doing with the study treatments via close monitoring in an in-patient setting. Experiences of people receiving CTB+AVP will be compared to those of people who do not. This will help determine if CTB+AVP is safe and well-tolerated at each dose of the study medicine. Participants will take part in this study for a maximum of 12 weeks for Part-1 (up to 4 weeks for screening, up to 3 weeks of taking study medicine and up to 5 weeks for safety follow-up visit) and for a maximum of 10 weeks for Part-2 (up to 4 weeks for screening, up to 1 week of taking study medicine and up to 5 weeks for safety follow-up visit). During the duration of the study, blood samples for study medicine levels, and various measures for monitoring safety such as blood samples for clinical laboratory measurements, electrocardiograms and vital sign measurements will be taken.

Eligibility Criteria

Inclusion Criteria

  • BMI of 17.5 to 30.5 kg/m2; and a total body weight >50 kg (110 lb)
  • For optional Japanese cohort only: Japanese participants who have 4 Japanese biologic grandparents who were born in Japan
  • For optional Chinese cohort only: Chinese participants who were born in mainland China, and both parents are of Chinese descent.

Exclusion Criteria

  • Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurological, or allergic disease (including drug allergies, but excluding untreated, asymptomatic, seasonal allergies at the time of dosing)
  • Known allergy to the cephalosporin group of antibiotics
  • History of HIV infection, hepatitis B, or hepatitis C; positive testing for HIV, HBsAg, or HCVAb. Hepatitis B vaccination is allowed
  • Other medical or psychiatric condition including recent (within the past year) or active suicidal ideation/behavior or laboratory abnormality [or other conditions or situations related to COVID-19 pandemic (eg, Contact with positive case, residence, or travel to an area with high incidence)] that may increase the risk of study participation or, in the investigator's judgment, make the participant inappropriate for the study
  • A positive urine drug test
  • Positive test result for SARS-CoV-2 infection at the time of screening or Day -1
View full record on ClinicalTrials.gov →

Data sourced from ClinicalTrials.gov (NCT05554237). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication.

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