A Study to Evaluate the Study Medication (Etrasimod) When Mixed With Food in Healthy Participants

A PHASE 1, OPEN-LABEL, RANDOMIZED, SINGLE DOSE, CROSSOVER STUDY TO ESTIMATE THE RELATIVE BIOAVAILABILITY OF ETRASIMOD (PF-07915503) MINI TABLETS IN WATER AND 3 FOOD VEHICLES COMPARED TO THE ETRASIMOD (PF-07915503) CLINICAL IR TABLETS UNDER FASTED CONDITIONS, AND TO EVALUATE MINI TABLET PALATABILITY IN HEALTHY ADULT PARTICIPANTS

The purpose of this study is to compare how healthy adults process Etrasimod when taken in different forms. One form is Etrasimod taken without food. The other form is Etrasimod mixed with water and 3 different foods. The types of food used are applesauce, chocolate pudding or yogurt.

The study is seeking participants who are:

• Aged 18 or older
• Male or female who are healthy as determined by medical assessment
• Body-mass index (BMI) of 16 to 32, and a total body weight > 50kg.

The study will take up to 2.5 months, including the screening period. Participants will have to stay at the study clinic for at least 45 days. This includes 5 study periods in total.

Participants will take Etrasimod as a tablet by mouth without food. Participants will also take Etrasimod sprinkled in soft food or water. Blood samples will be taken both before and after participants take Etrasimod. Participants will also answer questions for taste assessment purposes. A follow-up phone call will be made 20 to 27 days after the last study period.

Study Overview

• Status: Completed
• Conditions: Healthy Participants
• Intervention / Treatment: Drug: Estraimod Immediate Release (IR); Drug: Etrasimod Mini Tab in water; Drug: Etrasimod Mini Tab in chocolate pudding; Drug: Etrasimod Mini Tab in yogurt; Drug: Etrasimod Mini Tab in applesauce

• Study Type: Interventional
• Enrollment (Actual): 16
• Phase: Phase 1

Contacts and Locations

Study Locations

• Belgium
  • Bruxelles-capitale, Région DE
    • Brussels, Bruxelles-capitale, Région DE, Belgium, B-1070
      • Pfizer Clinical Research Unit - Brussels

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: Adult; Older Adult
• Accepts Healthy Volunteers: Yes

Description

Inclusion Criteria:

• Healthy participants
• BMI 16 to 32 kg/m2
• body weight more than 50kg

Exclusion Criteria:

• Ongoing or past history of significant medical conditions
• Eye disorders such as macular edema or uveitis
• Ongoing or recent infections
• Use of prescription or non prescription medications within 7 days of first dose
• Smoking or using nicotine products equivalent to more than 5 cigarettes per day
• History of severe allergic or anaphylactic reactions

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

4

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Sequence 1; Single oral dose of etrasimod 2 mg clinical IR tablet under fasted conditions (Reference) followed by single oral dose of etrasimod 2 mg mini tablets mixed with applesauce under fasted conditions (Test 1) followed by single oral dose of etrasimod 2 mg mini tablets mixed with chocolate pudding under fasted conditions (Test 2) followed by single oral dose of etrasimod 2 mg mini tablets mixed with water under fasted conditions (Test 3) followed by single oral dose of etrasimod 2 mg mini tablets mixed with yogurt under fasted conditions (Test 4)	Drug: Estraimod Immediate Release (IR); an immediate release tablet; Drug: Etrasimod Mini Tab in water; very small tablet mixed in water; Drug: Etrasimod Mini Tab in chocolate pudding; very small tablet mixed in chocolate pudding; Drug: Etrasimod Mini Tab in yogurt; Very small tablet mixed in yogurt; Drug: Etrasimod Mini Tab in applesauce; Very small tablet mixed in applesauce
Experimental: Sequence 2; Single oral dose of etrasimod 2 mg mini tablets mixed with applesauce under fasted conditions (Test 1) followed by single oral dose of etrasimod 2 mg mini tablets mixed with water under fasted conditions (Test 3) followed by single oral dose of etrasimod 2 mg clinical IR tablet under fasted conditions (Reference) followed by single oral dose of etrasimod 2 mg mini tablets mixed with chocolate pudding under fasted conditions (Test 2) followed by single oral dose of etrasimod 2 mg mini tablets mixed with yogurt under fasted conditions (Test 4)	Drug: Estraimod Immediate Release (IR); an immediate release tablet; Drug: Etrasimod Mini Tab in water; very small tablet mixed in water; Drug: Etrasimod Mini Tab in chocolate pudding; very small tablet mixed in chocolate pudding; Drug: Etrasimod Mini Tab in yogurt; Very small tablet mixed in yogurt; Drug: Etrasimod Mini Tab in applesauce; Very small tablet mixed in applesauce
Experimental: Sequence 3; Single oral dose of etrasimod 2 mg mini tablets mixed with chocolate pudding under fasted conditions (Test 2). Followed by single oral dose of etrasimod 2 mg clinical IR tablet under fasted conditions (Reference).followed by single oral dose of etrasimod 2 mg mini tablets mixed with water under fasted conditions (Test 3). Followed by single oral dose of etrasimod 2 mg mini tablets mixed with applesauce under fasted conditions (Test 1) Followed by single oral dose of etrasimod 2 mg mini tablets mixed with yogurt under fasted conditions (Test 4)	Drug: Estraimod Immediate Release (IR); an immediate release tablet; Drug: Etrasimod Mini Tab in water; very small tablet mixed in water; Drug: Etrasimod Mini Tab in chocolate pudding; very small tablet mixed in chocolate pudding; Drug: Etrasimod Mini Tab in yogurt; Very small tablet mixed in yogurt; Drug: Etrasimod Mini Tab in applesauce; Very small tablet mixed in applesauce
Experimental: Sequence 4; Single oral dose of etrasimod 2 mg mini tablets mixed with water under fasted conditions (Test 3). Followed by single oral dose of etrasimod 2 mg mini tablets mixed with chocolate pudding under fasted conditions (Test 2). Followed by single oral dose of etrasimod 2 mg mini tablets mixed with applesauce under fasted conditions (Test 1). Followed by single oral dose of etrasimod 2 mg clinical IR tablet under fasted conditions (Reference). Followed by single oral dose of etrasimod 2 mg mini tablets mixed with yogurt under fasted conditions (Test 4)	Drug: Estraimod Immediate Release (IR); an immediate release tablet; Drug: Etrasimod Mini Tab in water; very small tablet mixed in water; Drug: Etrasimod Mini Tab in chocolate pudding; very small tablet mixed in chocolate pudding; Drug: Etrasimod Mini Tab in yogurt; Very small tablet mixed in yogurt; Drug: Etrasimod Mini Tab in applesauce; Very small tablet mixed in applesauce

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Area Under the Plasma Concentration-Time Curve From Time Zero to the Time of the Last Quantifiable Concentration (AUClast) of Etrasimod	AUClast was calculated using linear/log trapezoidal method.	At pre-dose and 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose on Day 1 of each period
Area Under the Concentration-time Curve From Time Zero Extrapolated to Infinity (AUCinf) of Etrasimod	AUCinf was calculated as AUClast + (Clast*/kel), where Clast is 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 loglinear concentration-time curve.	At pre-dose and 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose on Day 1 of each period
Maximum Observed Plasma Concentration (Cmax) for Etrasimod		At pre-dose and 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose on Day 1 of each period

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Change From Baseline in Heart Rate at 1, 2, 3, 4, 5, 6, 8 and 24 Hours on Day 1	Heart rate was measured in beats per minute.	Baseline, 1, 2, 3, 4, 5, 6, 8 and 24 hours post dose on Day 1
Number of Participants With Treatment Emergent Adverse Events (TEAEs)	An adverse event (AE) was any untoward medical occurrence in a participant or clinical study participant, temporally associated with the use of study intervention, whether or not considered related to the study intervention. TEAEs were any AEs that occurred following start of treatment. A serious adverse event (SAE) was defined as any untoward medical occurrence that at any dose, met one or more of the criteria: resulted in death, life-threatening, required inpatient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, congenital anomaly/birth defect. AEs included SAEs and all non-SAEs.	From start of study treatment up to 28-35 days after last dose of study treatment (maximum up to 72 days)
Number of Participants With Clinical Laboratory Abnormalities	Clinical laboratory abnormalities test criteria included haematology: lymphocytes (10^3/ mm^3) and lymphocytes/leukocytes percentage (%) less than (<) 0.8* lower limit of normal (LLN), neutrophils, eosinophils, monocytes (10^3/mm^3), eosinophils/leukocytes monocytes/leukocytes (%) more than (>) 1.2* upper limit of normal (ULN); clinical chemistry: bicarbonate milliequivalents per liter (mEq/L) > 1.1* ULN; Urinalysis: urine hemoglobin, nitrite, leukocyte esterase greater than or equal to (>=) 1 and squamous epithelial cells /low power field (/LPF) > 4. Number of participants meeting any clinical laboratory abnormalities criteria is reported in this outcome measure.	Up to Day 45
Number of Participants According to Categorization of Vital Signs Results	Supine blood pressure (SBP) and pulse rate (PR) were measured. Vital sign criteria included: Systolic BP: <90 millimeter of mercury [mmHg]; Systolic BP change from baseline: maximum increase and decrease >=30 mmHg; Diastolic BP < 50 mmHg; Diastolic BP change from baseline: maximum decrease and increase >=20 mmHg; pulse rate <40 and >120 beats per minute.	Up to Day 45
Number of Participants According to Categorization of Electrocardiograms (ECGs) Findings	Standard 12-lead ECGs were used to measure PR interval, QT interval, QTc corrected using Fridericia's formula (QTcF), and QRS complex. ECG abnormalities were categorized as: QTcF interval, aggregate (milliseconds [msec]) 450 < Value <= 480, 480 < value <= 500, value > 500; 30 <= Change <= 60; Change > 60. Participants with any ECG abnormality criteria were reported in this outcome measure.	Up to Day 45
Assessment of Mouth Feel Based on Palatability Questionnaire	Participants were required to answer mouth feel (such as grittiness, stickiness, waxiness) of the product tasted. The score ranged from 0 (favorable) to 100 (not favorable), where higher scores indicated worse mouth feel.	At 1, 5, 10 and 20 minutes after tasting dose in each vehicle on Day 1 of each period
Assessment of Bitterness Based on Palatability Questionnaire	Participants were required to tell about the degree of bitterness of the product tasted. The score ranged from 0 (favorable) to 100 (not favorable), where higher scores indicated worse bitterness.	At 1, 5, 10 and 20 minutes after tasting dose in each vehicle on Day 1 of each period
Assessment of Tongue/Mouth Burns Based on Palatability Questionnaire	Participants were required to tell about the degree of palatability attribute of tongue/mouth burns of the product tasted. The score ranged from 0 (favorable) to 100 (not favorable), where higher scores indicated more tongue/mouth burns.	At 1, 5, 10 and 20 minutes after tasting dose in each vehicle on Day 1 of each period
Assessment of Likeness of Throat Burn Based on Palatability Questionnaire	Participants were required to tell the palatability attribute of throat burn of the product tasted. The score ranged from 0 (favorable) to 100 (not favorable), where higher scores indicated more throat burn.	At 1, 5, 10 and 20 minutes after tasting dose in each vehicle on Day 1 of each period
Assessment of Overall Liking Based on Palatability Questionnaire	Participants were required to tell the palatability attribute of overall liking of the product tasted. The score ranged from 0 (favorable) to 100 (not favorable), where higher scores indicated less overall liking.	At 1, 5, 10 and 20 minutes after tasting dose in each vehicle on Day 1 of each period

Collaborators and Investigators

• Sponsor: Pfizer
• Investigators: Study Director: Pfizer CT.gov Call Center, Pfizer

Publications and helpful links

Helpful Links

• To obtain contact information for a study center near you, click here.

Study record dates

Study Major Dates

• Study Start (Actual): September 4, 2023
• Primary Completion (Actual): January 4, 2024
• Study Completion (Actual): January 4, 2024

Study Registration Dates

• First Submitted: June 29, 2023
• First Submitted That Met QC Criteria: July 20, 2023
• First Posted (Actual): July 21, 2023

Study Record Updates

• Last Update Posted (Actual): March 25, 2025
• Last Update Submitted That Met QC Criteria: February 7, 2025
• Last Verified: February 1, 2025

More Information

Terms related to this study

• Keywords: adult; bioavailability; etrasimod
• Other Study ID Numbers: C5041034; 2023-504411-32-00 (Registry Identifier: CTIS (EU))

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: NO
• IPD Plan Description: Pfizer will provide access to individual de-identified participant data and related study documents (e.g. protocol, Statistical Analysis Plan (SAP), Clinical Study Report (CSR)) upon request from qualified researchers, and subject to certain criteria, conditions, and exceptions. Further details on Pfizer's data sharing criteria and process for requesting access can be found at: https://www.pfizer.com/science/clinical_trials/trial_data_and_results/data_requests.

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: Yes
• Studies a U.S. FDA-regulated device product: No