Phase 1
Completed N=15
Relative Bioavailability Study of Nirmatrelvir/Ritonavir 4 Different Fixed Dose Combination Tablets Relative to the Commercial Tablets in Healthy Participants
Biological Availability · Healthy Participants
Source: ClinicalTrials.gov NCT05525910 ↗
Enrolled (actual)
15
Serious AEs
0.0%
Results posted
Sep 2024
Primary outcomePrimary: 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) — 27040; 29350; 30680; 28200 nanogram*hour per milliliter (ng*hr/mL)
Summary
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.
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY 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) |
27040; 29350; 30680; 28200; 33660 | — |
| PRIMARY 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) |
26620; 28890; 30350; 27630; 33060 | — |
| PRIMARY 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) |
2709; 3111; 3181; 3051; 3556 | — |
| PRIMARY 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) |
3420; 3230; 3453; 2921; 4130 | — |
| PRIMARY 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) |
3224; 3044; 3297; 2735; 3821 | — |
| PRIMARY 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) |
371.3; 334.2; 374.5; 319.5; 411.3 | — |
| SECONDARY Number of Participants With All-Causality and Treatment-Related TEAEs |
2; 0; 2; 1; 2; 0 | — |
| SECONDARY Number of Participants With Clinically Significant Laboratory Abnormalities in Hematology, Chemistry, and Urinalysis |
0; 0; 0; 1; 0; 0 | — |
| SECONDARY Number of Participants With Clinically Significant Change From Baseline in Vital Signs |
0; 0; 0; 0; 0 | — |
| SECONDARY Number of Participants With Clinically Significant Physical Examination Values |
0; 0; 0; 0; 0 | — |
| SECONDARY Number of Participants With Clinically Significant Abnormal 12-Lead Electrocardiogram (ECG) |
0; 0; 0; 0; 0 | — |
Eligibility Criteria
Inclusion Criteria
- Participants who are overtly healthy as determined by medical evaluation including medical history, physical examination (PE), laboratory tests, vital signs and standard 12 lead ECGs.
- Body mass index (BMI) of 17.5 to 30.5 kg/m2; and a total body weight >50 kg (110 lb).
- Participants who are willing and able to comply with all scheduled visits, treatment plan, laboratory tests, lifestyle considerations, and other study procedures
Exclusion Criteria
- Positive test result for SARS-CoV-2 infection at the time of Screening or Day -1.
- 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).
- Clinically relevant abnormalities requiring treatment (eg, acute myocardial infarction, unstable ischemic conditions, evidence of ventricular dysfunction, serious tachy or brady arrhythmias) or indicating serious underlying heart disease (eg, prolonged PR interval, cardiomyopathy, heart failure greater than New York Heart Association (NYHA) 1, underlying structural heart disease, Wolff Parkinson-White syndrome).
- Any condition possibly affecting drug absorption (eg, gastrectomy, cholecystectomy).
- History of human immunodeficiency virus (HIV) infection, hepatitis B, or hepatitis C; positive testing for HIV, hepatitis B surface antigen (HBsAg), or hepatitis B surface antibody (HCVAb). Hepatitis B vaccination is allowed.
- Use of prescription or nonprescription drugs and dietary and herbal supplements within 7 days or 5 half lives (whichever is longer) prior to the first dose of study intervention.
- Participant who have received a COVID-19 vaccine within 7 days before screening or admission, or who are to be vaccinated with a COVID-19 vaccine at any time during the study confinement period.
- A positive urine drug test.
Data sourced from ClinicalTrials.gov (NCT05525910). 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. Informational only — not medical advice.