Relative Bioavailability Study of Nirmatrelvir/Ritonavir 4 Different Fixed Dose Combination Tablets Relative to the Commercial Tablets in Healthy Participants
CompletedPhase 1Results postedLast updated 19 September 2024
What this trial tests
Phase 1 trial testing Nirmatrelvir/ ritonavir in Biological Availability in 15 participants. Completed in 7 November 2022.
18 and older, any sex, with Biological Availability or Healthy Participants. Patients with the condition only — healthy volunteers not accepted.
Results — posted to ClinicalTrials.gov
Per-arm endpoint measurements with 95% confidence intervals where reported. Source: trial results section.
AUCinf of Nirmatrelvir Following the Administration of 4 Different Nirmatrelvir/Ritonavir FDC Tablets (Test Formulations) Compared to the Nirmatrelvir/Ritonavir 300(2*150)/100 mg Tablets (Reference Formulation)Primary· 0 (pre-dose), 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 16, 24, 48 and 72 hours post-dose on Day 1 of each treatment period
AUCinf was defined as area under the plasma concentration-time profile from time 0 extrapolated to infinite time. AUCinf for nirmatrelvir was calculated by AUClast + (Clast/kel), where Clast was the predicted plasma concentration at the last quantifiable time point 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.
Nirmatrelvir/Ritonavir 2*(150/50 mg) High Disintegrant
30680
± 21
Nirmatrelvir/Ritonavir 2*(150/50 mg) HDL
28200
± 40
Nirmatrelvir/Ritonavir 3*(100/33.3 mg)
33660
± 29
AUClast of Nirmatrelvir Following the Administration of 4 Different Nirmatrelvir/Ritonavir FDC Tablets (Test Formulations) Compared to the Nirmatrelvir/Ritonavir 300(2*150)/100 mg Tablets (Reference Formulation)Primary· 0 (pre-dose), 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 16, 24, 48 and 72 hours post-dose on Day 1 of each treatment period
AUClast was defined as area under the plasma concentration-time profile from time 0 to the time of the last quantifiable concentration (Clast). AUClast for nirmatrelvir was calculated by Linear/Log trapezoidal method.
Nirmatrelvir/Ritonavir 2*(150/50 mg) High Disintegrant
30350
± 21
Nirmatrelvir/Ritonavir 2*(150/50 mg) HDL
27630
± 42
Nirmatrelvir/Ritonavir 3*(100/33.3 mg)
33060
± 31
Cmax of Nirmatrelvir Following the Administration of 4 Different Nirmatrelvir/Ritonavir FDC Tablets (Test Formulations) Compared to the Nirmatrelvir/Ritonavir 300(2*150)/100 mg Tablets (Reference Formulation)Primary· 0 (pre-dose), 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 16, 24, 48 and 72 hours post-dose on Day 1 of each treatment period
Cmax was defined as maximum plasma concentration. Cmax for nirmatrelvir was observed directly from data.
Nirmatrelvir/Ritonavir 2*(150/50 mg) High Disintegrant
3181
± 24
Nirmatrelvir/Ritonavir 2*(150/50 mg) HDL
3051
± 42
Nirmatrelvir/Ritonavir 3*(100/33.3 mg)
3556
± 41
AUCinf of Ritonavir Following the Administration of 4 Different Nirmatrelvir/Ritonavir FDC Tablets (Test Formulations) Compared to the Nirmatrelvir/Ritonavir 300(2*150)/100 mg Tablets (Reference Formulation)Primary· 0 (pre-dose), 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 16, 24, 48 and 72 hours post-dose on Day 1 of each treatment period
AUCinf was defined as area under the plasma concentration-time profile from time 0 extrapolated to infinite time. AUCinf for ritonavir was calculated by AUClast + (Clast/kel), where Clast was the predicted plasma concentration at the last quantifiable time point 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.
Nirmatrelvir/Ritonavir 2*(150/50 mg) High Disintegrant
3453
± 54
Nirmatrelvir/Ritonavir 2*(150/50 mg) HDL
2921
± 85
Nirmatrelvir/Ritonavir 3*(100/33.3 mg)
4130
± 62
AUClast of Ritonavir Following the Administration of 4 Different Nirmatrelvir/Ritonavir FDC Tablets (Test Formulations) Compared to the Nirmatrelvir/Ritonavir 300(2*150)/100 mg Tablets (Reference Formulation)Primary· 0 (pre-dose), 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 16, 24, 48 and 72 hours post-dose on Day 1 of each treatment period
AUClast was defined as area under the plasma concentration-time profile from time 0 to the time of the last quantifiable concentration (Clast). AUClast for ritonavir was calculated by Linear/Log trapezoidal method.
Nirmatrelvir/Ritonavir 2*(150/50 mg) High Disintegrant
3297
± 53
Nirmatrelvir/Ritonavir 2*(150/50 mg) HDL
2735
± 87
Nirmatrelvir/Ritonavir 3*(100/33.3 mg)
3821
± 66
Cmax of Ritonavir Following the Administration of 4 Different Nirmatrelvir/Ritonavir FDC Tablets (Test Formulations) Compared to the Nirmatrelvir/Ritonavir 300(2*150)/100 mg Tablets (Reference Formulation)Primary· 0 (pre-dose), 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 16, 24, 48 and 72 hours post-dose on Day 1 of each treatment period
Cmax was defined as maximum plasma concentration. Cmax for ritonavir was observed directly from data.
Nirmatrelvir/Ritonavir 2*(150/50 mg) High Disintegrant
374.5
± 47
Nirmatrelvir/Ritonavir 2*(150/50 mg) HDL
319.5
± 84
Nirmatrelvir/Ritonavir 3*(100/33.3 mg)
411.3
± 77
Number of Participants With All-Causality and Treatment-Related TEAEsSecondary· From the first dose of study treatment up to 35 days after last dose of study treatment (ie, up to 51 days)
An AE was any untoward medical occurrence in a participant who received study treatment without regard to possibility of causal relationship. Treatment-related AE was any untoward medical occurrence attributed to study treatment in a participant who received study treatment. Relatedness to study treatment was assessed by the investigator. A serious adverse event (SAE) was an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or signific
Nirmatrelvir/Ritonavir 2*(150/50 mg) High Disintegrant
0
Nirmatrelvir/Ritonavir 2*(150/50 mg) HDL
0
Nirmatrelvir/Ritonavir 3*(100/33.3 mg)
0
Number of Participants With Clinically Significant Laboratory Abnormalities in Hematology, Chemistry, and UrinalysisSecondary· From baseline up to Day 4 of Period 4 (approximately 17 days)
Hematology included hemoglobin, hematocrit, red blood cell, mean corpuscular volume, mean corpuscular hemoglobin, mean corpuscular hemoglobin concentration, platelet and white blood cell count, total neutrophils, eosinophils, etc. Chemistry included blood urea nitrogen, creatinine, glucose, calcium, sodium, potassium, chloride, bicarbonate, aspartate aminotransferase, alanine aminotransferase, total bilirubin, alkaline phosphatase, uric acid, albumin, total protein, fibrinogen, etc. Urinalysis included pH, glucose, protein, blood, ketones, nitrites, leukocyte esterase, microscopy and culture.
Neutrophils (10^9/L) <0.8*lower limit of normal (LLN)
Nirmatrelvir/Ritonavir 2*(150/50 mg) High Disintegrant
0
Nirmatrelvir/Ritonavir 2*(150/50 mg) HDL
1
Nirmatrelvir/Ritonavir 3*(100/33.3 mg)
0
Number of Participants With Clinically Significant Change From Baseline in Vital SignsSecondary· From baseline up to Day 4 of Period 4 (approximately 16 days)
Vital signs (temperature, pulse rate and blood pressure) were obtained with participants following at least 5 minutes of supine rest. Clinical significance of vital signs was determined at the investigator's discretion. Baseline was defined as pre-dose measurement taken on Day 1 of each period.
Nirmatrelvir/Ritonavir 2*(150/50 mg) High Disintegrant
0
Nirmatrelvir/Ritonavir 2*(150/50 mg) HDL
0
Nirmatrelvir/Ritonavir 3*(100/33.3 mg)
0
Number of Participants With Clinically Significant Physical Examination ValuesSecondary· From baseline up to 35 days after last dose of study treatment (ie, up to 51 days)
A complete physical examination (PE) included, at a minimum, height, weight, head, ears, eyes, nose, mouth, skin, heart and lung examinations, lymph nodes, and gastrointestinal, musculoskeletal, and neurological systems. A brief PE included, at a minimum, assessments of general appearance, the respiratory and cardiovascular systems, and participant-reported symptoms. Clinical significance of physical examination values was determined at the investigator's discretion.
Nirmatrelvir/Ritonavir 2*(150/50 mg) High Disintegrant
0
Nirmatrelvir/Ritonavir 2*(150/50 mg) HDL
0
Nirmatrelvir/Ritonavir 3*(100/33.3 mg)
0
Number of Participants With Clinically Significant Abnormal 12-Lead Electrocardiogram (ECG)Secondary· From baseline up to Day 4 of Period 4 (approximately 16 days)
A 12-lead ECG was obtained using an ECG machine that automatically calculated the heart rate and measured pulse rate, QT, and QTc intervals and QRS complex. All scheduled ECGs were performed after the participant had rested quietly for at least 5 minutes in a supine position. Clinical significance of ECG values was determined at the investigator's discretion. Baseline was defined as pre-dose measurement taken on Day 1 of Period 1.
Nirmatrelvir/Ritonavir 2*(150/50 mg) High Disintegrant
0
Nirmatrelvir/Ritonavir 2*(150/50 mg) HDL
0
Nirmatrelvir/Ritonavir 3*(100/33.3 mg)
0
Adverse events — posted to ClinicalTrials.gov
Time frame: From the first dose of study treatment up to 35 days after last dose of study treatment (ie, up to 51 days).
Reporting threshold: 5%.
Adverse-event reports describe events observed during the trial — not all are caused by the drug.
The purpose of this study is to estimate the relative bioavailability of nirmatrelvir/ritonavir of 4 different FDC tablet formulations relative to the commercial tablet formulation under fasted conditions in healthy adult participants.
Publications & conference data
No peer-reviewed publications indexed yet for this trial. Completed trials usually publish results within 12-18 months.
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Sponsor: as reported to ClinicalTrials.gov by Pfizer
Last refreshed: 19 September 2024
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