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NCT05263921

Relative Bioavailability Study of PF-07321332/Ritonavir Oral Powder Relative to the Commercial Tablets in Healthy Participants

Completed Phase 1 Results posted Last updated 6 June 2024
What this trial tests

Phase 1 trial testing PF-07321332/ritonavir in Bioavailability in 12 participants. Completed in 19 May 2022.

Timeline
10 March 2022
Primary endpoint
19 May 2022
19 May 2022

Quick facts

Lead sponsorPfizer
PhasePhase 1
StatusCompleted
Study typeINTERVENTIONAL
Allocationrandomized
Designcrossover
Maskingnone
Primary purposebasic science
Enrollment12
Start date10 March 2022
Primary completion19 May 2022
Estimated completion19 May 2022
Sites1 location across United States

Drugs / interventions tested

Conditions studied

Sponsor

Pfizer — full company profile →

Who can join

18 and older, any sex, with Bioavailability. 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 Nirmatrelvir/Ritonavir in Different Delivery Vehicles Under Fasted Conditions 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 period

Area under the plasma concentration time profile from time 0 extrapolated to infinity (AUCinf) was measured. AUCinf was determined by AUClast + (Clast/kel), where Clast is the predicted plasma concentration at the last quantifiable time point estimated from the log-linear regression analysis.

GroupValue95% CI
Nirmatrelvir/Ritonavir 300/100 mg Commercial Tablets28670± 36
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Water30780± 25
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Applesauce33170± 33
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Vanilla Pudding36020± 27
AUClast of Nirmatrelvir Following the Administration of Nirmatrelvir/Ritonavir in Different Delivery Vehicles Under Fasted Conditions 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 period

Area under the plasma concentration time profile from time 0 to the time of the last quantifiable concentration (Clast) was measured. AUClast was determined by Linear/Log trapezoidal method.

GroupValue95% CI
Nirmatrelvir/Ritonavir 300/100 mg Commercial Tablets27790± 36
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Water30230± 27
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Applesauce32180± 33
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Vanilla Pudding35580± 27
Cmax of Nirmatrelvir Following the Administration of Nirmatrelvir/Ritonavir in Different Delivery Vehicles Under Fasted Conditions 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 period

Maximum plasma concentration (Cmax) was measured. Cmax was observed directly from data.

GroupValue95% CI
Nirmatrelvir/Ritonavir 300/100 mg Commercial Tablets2817± 31
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Water3254± 23
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Applesauce4025± 22
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Vanilla Pudding4572± 19
AUCinf of Ritonavir Following the Administration of Nirmatrelvir/Ritonavir in Different Delivery Vehicles Under Fasted Conditions 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 period

Area under the plasma concentration time profile from time 0 extrapolated to infinity (AUCinf) was measured. AUCinf was determined by AUClast + (Clast/kel), where Clast is the predicted plasma concentration at the last quantifiable time point estimated from the log-linear regression analysis.

GroupValue95% CI
Nirmatrelvir/Ritonavir 300/100 mg Commercial Tablets4843± 28
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Water5414± 30
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Applesauce4979± 45
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Vanilla Pudding5271± 26
AUClast of Ritonavir Following the Administration of Nirmatrelvir/Ritonavir in Different Delivery Vehicles Under Fasted Conditions 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 period

Area under the plasma concentration time profile from time 0 to the time of the last quantifiable concentration (Clast) was measured. AUClast was determined by Linear/Log trapezoidal method.

GroupValue95% CI
Nirmatrelvir/Ritonavir 300/100 mg Commercial Tablets4588± 29
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Water5108± 32
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Applesauce4757± 46
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Vanilla Pudding4998± 26
Cmax of Ritonavir Following the Administration of Nirmatrelvir/Ritonavir in Different Delivery Vehicles Under Fasted Conditions 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 period

Maximum plasma concentration (Cmax) was measured. Cmax was observed directly from data.

GroupValue95% CI
Nirmatrelvir/Ritonavir 300/100 mg Commercial Tablets536.9± 41
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Water598.2± 42
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Applesauce579.8± 45
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Vanilla Pudding640.5± 30
Number of Participants With Treatment-Emergent Adverse Event Secondary · Baseline up to Follow-up (35 days after last dose administration), an average of 10 weeks.

Adverse events (AEs): any untoward medical occurrence in a clinical investigation participant administered a product, without regard to relatedness. Treatment-emergent AEs (TEAEs): AEs which occurred for the first time during the effective duration of treatment or AEs that increased in severity during treatment. Serious AEs (SAEs) were any untoward medical occurrence at any dose that resulted in death; was life-threatening; required inpatient hospitalization or caused prolongation of existing hospitalization; resulted in persistent or significant disability/incapacity (substantial disruption o

All-causality TEAEs
GroupValue95% CI
Nirmatrelvir/Ritonavir 300/100 mg Commercial Tablets6
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Water2
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Applesauce1
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Vanilla Pudding4
Treatment-related TEAEs
GroupValue95% CI
Nirmatrelvir/Ritonavir 300/100 mg Commercial Tablets3
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Water2
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Applesauce1
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Vanilla Pudding1
Number of Participants With Laboratory Abnormalities Secondary · Screening, Period 1 Day -1, Period 4 Day 4 and early termination/discontinuation.

Participants analyzed in the laboratory abnormalities were with at least one observation of the given laboratory test while on study treatment or during lag time. Number of participants with laboratory abnormalities were number of participants with a laboratory abnormality meeting specified criteria while on study treatment or during lag time. Hematology, chemistry, urinalysis and other (SARS-CoV-2 RT-PCR, Urine drug screening, Pregnancy test (β hCG), eGFR \[CKD-EPI\], aPTT, PT-INR, Fibrinogen, At Screening only: FSH, HBsAg, HBsAb, HBcAb, HCVAb, HIV) were assessed.

Urinalysis: pH (>8)
GroupValue95% CI
Nirmatrelvir/Ritonavir 300/100 mg Commercial Tablets0
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Water1
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Applesauce0
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Vanilla Pudding0
Urinalysis: Urine hemoglobin (≥1)
GroupValue95% CI
Nirmatrelvir/Ritonavir 300/100 mg Commercial Tablets1
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Water0
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Applesauce0
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Vanilla Pudding0
Urinalysis: Nitrite (≥1)
GroupValue95% CI
Nirmatrelvir/Ritonavir 300/100 mg Commercial Tablets0
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Water1
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Applesauce0
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Vanilla Pudding0
Urinalysis: Leukocyte Esterase (≥1)
GroupValue95% CI
Nirmatrelvir/Ritonavir 300/100 mg Commercial Tablets1
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Water0
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Applesauce0
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Vanilla Pudding0
Number of Participants With Clinically Significant Vital Sign Values Secondary · Screening, Day 1 of each period and early termination/discontinuation.

Participants with clinically significant vital sign values were with at least one observation of vital signs, which met pre-specified criteria while on study treatment or during lag time.

GroupValue95% CI
Nirmatrelvir/Ritonavir 300/100 mg Commercial Tablets0
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Water0
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Applesauce0
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Vanilla Pudding0
Number of Participants With Clinically Significant Physical Examination Values Secondary · Screening and Period 1 Day -1.

Participants with clinically significant physical examination values were with at least one observation of physical examination, which met pre-specified criteria while on study treatment or during lag time.

GroupValue95% CI
Nirmatrelvir/Ritonavir 300/100 mg Commercial Tablets0
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Water0
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Applesauce0
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Vanilla Pudding0
Number of Participants With Clinically Significant Abnormal Electrocardiogram Values Secondary · Screening, Period 1 Day 1 and Period 4 Day 4.

Participants with clinically significant electrocardiogram (ECG) values were with at least one observation of ECG, which met pre-specified criteria while on study treatment or during lag time.

GroupValue95% CI
Nirmatrelvir/Ritonavir 300/100 mg Commercial Tablets0
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Water0
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Applesauce0
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Vanilla Pudding0
Taste Assessment of Mouth Feel After Administration of Nirmatrelvir/Ritonavir in Different Delivery Vehicles Secondary · 1, 5, 10, 20 min after tasting each study intervention on Day 1 of each period.

Participants reviewed the taste questionnaire and instructions prior to the first taste assessment to treatments (B, C, D) on Period 1 Day 1. Each participant completed the Taste Assessment Survey immediately following dosing (within 1 min) and at 5, 10, and 20 minutes post oral administration of PF-07321332/ritonavir oral powder. For the taste assessment in the study, the data used in the analysis were transcribed and rescaled to a score from 0 to 100 from the raw measurements on the Taste Assessment Questionnaire. The score of 0 was considered Favorable and the score of 100 was considered No

1 min
GroupValue95% CI
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Water61.3± 31.25
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Applesauce53.5± 28.42
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Vanilla Pudding49.5± 31.30
5 min
GroupValue95% CI
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Water63.2± 36.52
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Applesauce55.2± 32.56
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Vanilla Pudding57.5± 34.18
10 min
GroupValue95% CI
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Water61.2± 35.96
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Applesauce52.5± 38.92
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Vanilla Pudding51.6± 37.29
20min
GroupValue95% CI
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Water60.5± 35.06
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Applesauce52.0± 37.26
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Vanilla Pudding48.5± 35.41

Adverse events — posted to ClinicalTrials.gov

Time frame: Baseline up to Follow-up (35 days after last dose administration), an average of 10 weeks.. Reporting threshold: 5%. Adverse-event reports describe events observed during the trial — not all are caused by the drug.

Nirmatrelvir/Ritonavir 300/100 mg Commercial Tablets
Serious: 0/11 (0%)
Deaths: 0/11
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Water
Serious: 0/11 (0%)
Deaths: 0/11
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Applesauce
Serious: 0/12 (0%)
Deaths: 0/12
Nirmatrelvir/Ritonavir 300/100 mg Oral Powder Mixed With Vanilla Pudding
Serious: 0/11 (0%)
Deaths: 0/11
Other adverse events (15 terms — click to expand)

ReactionSystemNirmatrelvir/Ritonavir 300…Nirmatrelvir/Ritonavir 300…Nirmatrelvir/Ritonavir 300…Nirmatrelvir/Ritonavir 300…
DysgeusiaNervous system disorders————
HeadacheNervous system disorders————
DiarrhoeaGastrointestinal disorders————
GastritisGastrointestinal disorders————
NauseaGastrointestinal disorders————
Abdominal pain upperGastrointestinal disorders————
Dry mouthGastrointestinal disorders————
Vessel puncture site bruiseGeneral disorders————
Vessel puncture site painGeneral disorders————
Incision site complicationInjury, poisoning and procedural complications————
ArthralgiaMusculoskeletal and connective tissue disorders————
ParaesthesiaNervous system disorders————
Tension headacheNervous system disorders————
Vulvovaginal burning sensationReproductive system and breast disorders————
Dry skinSkin and subcutaneous tissue disorders————

Data from ClinicalTrials.gov NCT05263921 adverse events section.

Sponsor's own description

The purpose of this study is to estimate the relative bioavailability of PF-07321332/ritonavir oral powder relative to the commercial tablet formulation under fasted condition in healthy adult participants. The study will also assess the effect of 3 different food vehicles on the relative bioavailability of the PF-07321332/ritonavir oral powder formulation as well as the safety, tolerability, and palatability of PF-07321332/ritonavir oral powder in healthy adult participants.

Publications & conference data

3 peer-reviewed publications reference this trial (live from Europe PMC):

  1. Oral antiviral treatments for COVID-19: opportunities and challenges.
    Rahmah L, Abarikwu SO, Arero AG, Essouma M, et al · · 2022 · cited 53× · PMID 35871712 · DOI 10.1007/s43440-022-00388-7
  2. Inhibitors of SARS-CoV-2 Main Protease (Mpro) as Anti-Coronavirus Agents.
    Zagórska A, Czopek A, Fryc M, Jończyk J. · · 2024 · cited 19× · PMID 39062511 · DOI 10.3390/biom14070797
  3. A Clinical Insight on New Discovered Molecules and Repurposed Drugs for the Treatment of COVID-19.
    Banerjee S, Banerjee D, Singh A, Kumar S, et al · · 2023 · cited 9× · PMID 36851211 · DOI 10.3390/vaccines11020332

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Data sources for this page

Drug Landscape aggregates and links these public records for informational use only. Always verify against the primary source before clinical or regulatory decisions. Canonical URL: https://druglandscape.com/trial/NCT05263921.

Primary sources · FDA · ClinicalTrials.gov · EMA · SEC EDGAR · ChEMBL · Wikidata · full sourcing