Phase 1
Completed N=12
Relative Bioavailability Study of Nirmatrelvir/Ritonavir Oral Powder Relative to the Commercial Tablets and Estimation of the Effect of Food on Bioavailability of the Nirmatrelvir/Ritonavir Oral Powder in Healthy Participants.
Biological Availability
Source: ClinicalTrials.gov NCT05544786 ↗
Enrolled (actual)
12
Serious AEs
0.0%
Results posted
May 2024
Primary outcomePrimary: AUCinf of Nirmatrelvir Following the Administration of Nirmatrelvir/Ritonavir in Different Delivery Vehicles — 27090; 30650; 33030; 34000 nanogram*hour per milliliter (ng*hr/mL)
Summary
The purpose of this study is to estimate the relative bioavailability (rBA) of nirmatrelvir/ritonavir oral powder in 3 different food vehicles relative to the Paxlovid® tablets under fasted condition in healthy adult participants, and to estimate the effect of food on the rBA of the nirmatrelvir/ritonavir oral powder formulation. The study will also assess the safety, tolerability, and palatability of nirmatrelvir/ritonavir oral powder in healthy adult participants.
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY AUCinf of Nirmatrelvir Following the Administration of Nirmatrelvir/Ritonavir in Different Delivery Vehicles |
27090; 30650; 33030; 34000; 32810 | — |
| PRIMARY AUClast of Nirmatrelvir Following the Administration of Nirmatrelvir/Ritonavir in Different Delivery Vehicles |
26500; 30110; 32470; 33540; 32410 | — |
| PRIMARY Cmax of Nirmatrelvir Following the Administration of Nirmatrelvir/Ritonavir in Different Delivery Vehicles |
2862; 3156; 4034; 4287; 4208 | — |
| PRIMARY AUCinf of Ritonavir Following the Administration of Nirmatrelvir/Ritonavir in Different Delivery Vehicles |
4005; 3876; 3479; 3986; 3176 | — |
| PRIMARY AUClast of Ritonavir Following the Administration of Nirmatrelvir/Ritonavir in Different Delivery Vehicles |
3818; 3663; 3303; 3371; 2959 | — |
| PRIMARY Cmax of Ritonavir Following the Administration of Nirmatrelvir/Ritonavir in Different Delivery Vehicles |
398.4; 406.1; 368.1; 386.6; 280.7 | — |
| SECONDARY AUCinf of Nirmatrelvir Following the Administration of Nirmatrelvir/Ritonavir Mixed With Vanilla Pudding Under Fasted/Fed Conditions |
34000; 32810 | — |
| SECONDARY AUClast of Nirmatrelvir Following the Administration of Nirmatrelvir/Ritonavir Mixed With Vanilla Pudding Under Fasted/Fed Conditions |
33540; 32410 | — |
| SECONDARY Cmax of Nirmatrelvir Following the Administration of Nirmatrelvir/Ritonavir Mixed With Vanilla Pudding Under Fasted/Fed Conditions |
4287; 4208 | — |
| SECONDARY AUCinf of Ritonavir Following the Administration of Nirmatrelvir/Ritonavir Mixed With Vanilla Pudding Under Fasted/Fed Conditions |
3986; 3176 | — |
| SECONDARY AUClast of Ritonavir Following the Administration of Nirmatrelvir/Ritonavir Mixed With Vanilla Pudding Under Fasted/Fed Conditions |
3371; 2959 | — |
| SECONDARY Cmax of Ritonavir Following the Administration of Nirmatrelvir/Ritonavir Mixed With Vanilla Pudding Under Fasted/Fed Conditions |
386.6; 280.7 | — |
| SECONDARY Number of Participants With All-Causality and Treatment-Related Treatment-emergent Adverse Events (TEAEs) |
2; 4; 5; 2; 2; 0 | — |
| SECONDARY Number of Participants With Laboratory Test Abnormalities (Without Regard to Baseline Abnormality) |
0; 0; 0; 3; 2; 0 | — |
| SECONDARY Number of Participants With Clinically Significant Vital Signs |
0; 0; 0; 0; 0 | — |
| SECONDARY Number of Participants With Clinically Significant 12-Lead Electrocardiogram (ECG) Values |
0; 0; 0; 0; 0 | — |
| SECONDARY Number of Participants With Clinically Significant Physical Examination (PE) Values |
0; 0; 0; 0; 0 | — |
| SECONDARY Taste Assessment of Mouth Feel After Administration of Nirmatrelvir/Ritonavir in Different Delivery Vehicles |
66.8; 65.4; 56.3; 73.8; 60.3; 57.2 | — |
| SECONDARY Taste Assessment of Bitterness After Administration of Nirmatrelvir/Ritonavir in Different Delivery Vehicles |
75.3; 72.0; 61.4; 75.4; 66.5; 58.2 | — |
| SECONDARY Taste Assessment of Tongue/Mouth Burn After Administration of Nirmatrelvir/Ritonavir in Different Delivery Vehicles |
31.3; 36.3; 32.4; 33.9; 29.9; 29.8 | — |
| SECONDARY Taste Assessment of Throat Burn After Administration of Nirmatrelvir/Ritonavir in Different Delivery Vehicles |
30.9; 31.7; 26.4; 34.5; 37.5; 27.3 | — |
| SECONDARY Taste Assessment of Overall Liking After Administration of Nirmatrelvir/Ritonavir in Different Delivery Vehicles |
73.5; 65.0; 55.8; 74.7; 66.3; 55.9 | — |
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 (NCT05544786). 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.