NCT05040295

A Single Dose Study To Test Two Pediatric Forms Of Ritlecitinib Compared With Adult Ritlecitinib In Healthy Adults

Completed Phase 1 Results posted Last updated 21 August 2023

What this trial tests

Phase 1 trial testing ritlecitinib in Healthy Participants in 12 participants. Completed in 19 November 2021.

Timeline

10 September 2021

Primary endpoint
19 November 2021

19 November 2021

Quick facts

Lead sponsor	Pfizer
Phase	Phase 1
Status	Completed
Study type	INTERVENTIONAL
Allocation	randomized
Design	crossover
Masking	none
Primary purpose	basic science
Enrollment	12
Start date	10 September 2021
Primary completion	19 November 2021
Estimated completion	19 November 2021
Sites	1 location across United States

Drugs / interventions tested

• ritlecitinib (ritlecitinib) — full drug profile →
• ritlecitinib (ritlecitinib) — full drug profile →
• ritlecitinib (ritlecitinib) — full drug profile →

Conditions studied

• Healthy Participants — all drugs for Healthy Participants →

Sponsor

Pfizer — full company profile →

Who can join

Adults 18 to 55, any sex, with 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.

Area Under the Plasma Concentration-Time Profile From Time 0 Extrapolated to Infinite Time (AUCinf) for Ritlecitinib Primary · Pre-dose, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, and 24 hours post dose on Day 1 in each period

Plasma AUCinf for ritlecitinib is reported. AUCinf was calculated as \[AUClast+(Clast\*/kel)\], where AUClast is the area under the plasma concentration-time profile from time 0 to the time of the Clast, Clast is the last quantifiable concentration, Clast\* is the predicted plasma concentration at the last quantifiable time point estimated 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.

Group	Value	95% CI
Treatment A: Ritlecitinib 30 mg Intact Adult Capsule	361.1	± 39
Treatment B: Ritlecitinib 3*10 mg Pediatric Capsules	370.1	± 40
Treatment C: Ritlecitinib 30 mg Spray Congealed Beads	385.1	± 38

Maximum Plasma Concentration (Cmax) for Ritlecitinib Primary · Pre-dose, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, and 24 hours post dose on Day 1 in each period

Plasma Cmax for ritlecitinib is reported.

Group	Value	95% CI
Treatment A: Ritlecitinib 30 mg Intact Adult Capsule	197.4	± 38
Treatment B: Ritlecitinib 3*10 mg Pediatric Capsules	199.6	± 37
Treatment C: Ritlecitinib 30 mg Spray Congealed Beads	177.9	± 30

Number of Participants With Treatment-Emergent Adverse Events (All Causalities and Treatment-Related) Secondary · Post first dose of study intervention on Period 1 Day 1 up to 35 days post last dose of study intervention on Period 3 Day 1 (maximum of 40 days)

An adverse event (AE) was any untoward medical occurrence attributed to study drug in a participant who received study drug. Treatment-related AE was any untoward medical occurrence attributed to study treatment in a participant who received study treatment. Treatment-emergent AEs (TEAEs) = between first dose of study treatment and up to 35 days after last dose that were absent before treatment or that worsened relative to pretreatment state. A serious AE (SAE) was an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient

Participants with AEs (All Causalities)

Group	Value	95% CI
Treatment A: Ritlecitinib 30 mg Intact Adult Capsule	2
Treatment B: Ritlecitinib 3*10 mg Pediatric Capsules	1
Treatment C: Ritlecitinib 30 mg Spray Congealed Beads	1

Participants with AEs (Treatment Related)

Group	Value	95% CI
Treatment A: Ritlecitinib 30 mg Intact Adult Capsule	0
Treatment B: Ritlecitinib 3*10 mg Pediatric Capsules	0
Treatment C: Ritlecitinib 30 mg Spray Congealed Beads	0

Participants with SAEs

Group	Value	95% CI
Treatment A: Ritlecitinib 30 mg Intact Adult Capsule	0
Treatment B: Ritlecitinib 3*10 mg Pediatric Capsules	0
Treatment C: Ritlecitinib 30 mg Spray Congealed Beads	0

Participants with Severe AEs

Group	Value	95% CI
Treatment A: Ritlecitinib 30 mg Intact Adult Capsule	0
Treatment B: Ritlecitinib 3*10 mg Pediatric Capsules	0
Treatment C: Ritlecitinib 30 mg Spray Congealed Beads	0

Number of Participants With Laboratory Abnormalities Without Regard to Baseline Abnormality Secondary · Baseline up to Period 3 Day 2 (maximum of 7 days)

Following parameters were analyzed for laboratory examination: hematology (hemoglobin, hematocrit, red blood cell count, platelet count, white blood cell count, total neutrophils, eosinophils, monocytes, basophils, lymphocytes, etc), chemistry (fasting glucose, calcium, sodium, potassium, chloride, total bilirubin, aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase, uric acid, total protein, albumin, etc), and urinalysis (glucose, protein, blood, ketones, nitrites, leukocyte esterase, etc). Baseline = the last pre-dose measurement before Period 1 Day 1 (ie, first dose o

Eosinophils/Leukocytes (%) >1.2*ULN

Group	Value	95% CI
Entire Study Population	1

Monocytes/Leukocytes (%) >1.2*ULN

Group	Value	95% CI
Entire Study Population	2

Bicarbonate (mEq/L) <0.9*LLN

Group	Value	95% CI
Entire Study Population	1

Ketones (No Unit) >=1

Group	Value	95% CI
Entire Study Population	1

URINE Hemoglobin (No Unit) >=1

Group	Value	95% CI
Entire Study Population	1

Nitrite (No Unit) >=1

Group	Value	95% CI
Entire Study Population	1

Leukocyte Esterase (No Unit) >=1

Group	Value	95% CI
Entire Study Population	1

URINE Leukocytes (/HPF) >=20

Group	Value	95% CI
Entire Study Population	1

Adverse events — posted to ClinicalTrials.gov

Time frame: Baseline (ie, post the first dose of study intervention) up to 35 days post last dose of study intervention (maximum of 40 days). Reporting threshold: 5%. Adverse-event reports describe events observed during the trial — not all are caused by the drug.

Treatment A: Ritlecitinib 30 mg Intact Adult Capsule

Serious: 0/12 (0%)

Deaths: 0/12

Treatment B: Ritlecitinib 3*10 mg Pediatric Capsules

Serious: 0/12 (0%)

Deaths: 0/12

Treatment C: Ritlecitinib 30 mg Spray Congealed Beads

Serious: 0/12 (0%)

Deaths: 0/12

Other adverse events (4 terms — click to expand)

Reaction	System	Treatment A: Ritlecitinib …	Treatment B: Ritlecitinib …	Treatment C: Ritlecitinib …
Vessel puncture site pain	General disorders	—	—	—
Fatigue	General disorders	—	—	—
Headache	Nervous system disorders	—	—	—
Somnolence	Nervous system disorders	—	—	—

Data from ClinicalTrials.gov NCT05040295 adverse events section.

Sponsor's own description

A phase I, single dose study to test two forms of pediatric ritlecitinib compared to adult ritlecitinib in healthy adults aged 18-55 years old. Approximately 12 adults will participate for approximately 2.5 months.

Publications & conference data

1 peer-reviewed publication reference this trial (live from Europe PMC):

1. Virtual Bioequivalence Assessment of Ritlecitinib Capsules with Incorporation of Observed Clinical Variability Using a Physiologically Based Pharmacokinetic Model.
   Saadeddin A, Purohit V, Huh Y, Wong M, et al · · 2024 · cited 14× · PMID 38267790 · DOI 10.1208/s12248-024-00888-9