HealthyPhase 1NCT03137134
A Study to Evaluate the Effects of Food and Esomeprazole on the Pharmacokinetics of Crizotinib in a Coated Microsphere Formulation.
A Phase 1 study testing Crizotinib and Esomeprazole in people with Healthy, run by Pfizer at 1 site in United States.
Trial summary
This study will estimate the effect of food and the proton pump inhibitor, esomeprazole on the pharmacokinetics of crizotinib in a coated microsphere formulation. Read more about this study
- Who is it for?
- Ages 18 to 55 yearsHealthy volunteers can take part
- Conditions the study is for
- Healthy
- What is being tested?
- Crizotinib and Esomeprazole
- Could I receive a placebo?
- No, everyone receives an active treatment
- How many people
- 18 participants
- Where
- 1 siteUnited States
- Study dates
- 20 Jun 2017to 17 Oct 2017
- Phase
- Phase 1
- Are there results?
- None posted in the registry
Key requirements
Who can take part, as listed by the sponsor. Only the study team can confirm whether you are eligible, so take this list to your doctor.
- Ages 18 to 55 years
- All sexes
- Healthy volunteers accepted
- Adult
Who may be able to join
- Healthy male subjects and female subjects of nonchildbearing potential between 18 and 55 years old.
- Body mass index (BMI) of 17.5 to 30.5 kg/m2; and a total body weight >50 kg (110 lb).
- Evidence of a personally signed and dated informed consent document indicating that the subject has been informed of all pertinent aspects of the study.
- Subjects who are willing and able to comply with all scheduled visits, treatment plan, laboratory tests and other study procedures.
Who cannot join
- 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).
- Any condition possibly affecting drug absorption (eg, gastrectomy).
- A positive urine drug test.
- Subjects who currently smoke.
- History of regular alcohol consumption exceeding 7 drinks/week for female subjects or 14 drinks/week for male subjects (1 drink = 5 ounces [150 mL] of wine or 12 ounces [360 mL] of beer or 1.5 ounces [45 mL] of hard liquor) within 6 months before screening.
- Subjects with history of known sensitivity to esomeprazole or substituted benzimidazoles.
Show all 19Show fewer
- Treatment with an investigational drug within 30 days or 5 half-lives preceding the first dose of study drug.
- Screening supine BP greater than or equal to 140 mm Hg (systolic) or greater than or equal to 90 mm Hg (diastolic), following at least 5 minutes of supine rest.
- Screening supine 12-lead triplicate ECG demonstrating a corrected time from the beginning of the Q wave to the end of the T wave corresponding to electrical systole (QTc) interval >450 msec or a QRS complex >120 msec.
- Subjects with ANY of the following abnormalities in clinical laboratory tests at screening, as assessed by the study-specific laboratory and confirmed by a single repeat test, if deemed necessary:
- Aspartate aminotransferase (AST) or ALT level greater than or equal to 1.5 × upper limit of normal (ULN);
- Total bilirubin (TBili) level greater than or equal to 1.5 × ULN; subjects with a history of Gilbert's syndrome may have direct bilirubin measured and would be eligible for this study provided the direct bilirubin level is less than or equal to ULN.
- Male subjects who are unwilling or unable to use 2 highly effective methods of contraception as outlined in this protocol for the duration of the study and for at least 90 days after the last dose of investigational product.
- Use of prescription or nonprescription drugs and dietary supplements within 7 days or 5 half-lives (whichever is longer) prior to the first dose of IP.
- Blood donation (excluding plasma donations) of approximately 1 pint (500 mL) or more within 60 days prior to dosing.
- History of human immunodeficiency virus (HIV), hepatitis B, or hepatitis C; positive testing for HIV, hepatitis B surface antigen (HepBsAg), hepatitis B core antibody (HepBcAb), or hepatitis C antibody (HCVAb).
- Unwilling or unable to comply with the criteria in the Lifestyle Requirements section of this protocol.
- Subjects who are investigator site staff members directly involved in the conduct of the study and their family members, site staff members otherwise supervised by the investigator, or subjects who are Pfizer employees, including their family members, directly involved in the conduct of the study.
- Other acute or chronic medical or psychiatric condition including recent (within the past year) or active suicidal ideation or behavior or laboratory abnormality that may increase the risk associated with study participation or crizotinib cMS and/or esomeprazole administration or may interfere with the interpretation of study results and, in the judgment of the investigator, would make the subject inappropriate for entry into this study.
Trial locations and contacts
1 site in 1 country.
United States1 site
Pfizer New Haven Clinical Research Unit
New Haven, Connecticut, 06511
About this study
Official title: A Phase 1, Open-label, Single Dose Study To Evaluate The Effects Of Food And The Proton Pump Inhibitor, Esomeprazole, On The Pharmacokinetics Of Crizotinib In A Coated Microsphere Formulation In Adult Healthy Volunteers
This study will estimate the effect of food and the proton pump inhibitor, esomeprazole on the pharmacokinetics of crizotinib in a coated microsphere formulation.
Read the detailed description
This study is an open-label, randomized, 4-period, 5-treatment, 6-sequence study in adult healthy volunteers. Subjects will receive up to four separate single oral 300 mg doses of a coated microsphere (cMS) formulation of crizotinib. Period 1 through Period 3 will evaluate the effect of food, and, the effect of multiple doses of a gastrointestinal acid reducing agent, esomeprazole, in fasted state, on the pharmacokinetics (PK) of crizotinib cMS. Period 4 will evaluate whether apple sauce or orange juice may reduce the effect of multiple doses of esomeprazole on the PK of crizotinib cMS, if there is an effect.
- Conditions
- Healthy
- Being tested
- Crizotinib, Esomeprazole
What participants receive
What participants receive. In a randomised study each person is assigned to one group by chance.
CrizotinibDrug
Crizotinib in a coated microsphere formulation
EsomeprazoleDrug
Proton pump inhibitor, esomeprazole
| Study group | Role | What they receive |
|---|---|---|
| Treatment A | Active comparator | (reference) Crizotinib cMS 300 mg in fasted state Receives: Drug: Crizotinib |
| Treatment B | Experimental | (test) Crizotinib cMS 300 mg in fed state Receives: Drug: Crizotinib |
| Treatment C | Experimental | (test) 5 days of esomeprazole 40 mg followed by crizotinib cMS 300 mg in fasted state Receives: Drug: Crizotinib; Drug: Esomeprazole |
| Treatment D | Experimental | (test) 5 days of esomeprazole 40 mg followed by crizotinib cMS 300 mg with apple sauce. Receives: Drug: Crizotinib; Drug: Esomeprazole |
| Treatment E | Experimental | (test) 5 days of esomeprazole 40 mg followed by crizotinib cMS 300 mg with orange juice Receives: Drug: Crizotinib; Drug: Esomeprazole |
What is being measured
The primary outcome is the main question the study is designed to answer.
Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast)
Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast)
Measured: Crizotinib pre-dose, 1, 2, 4, 6, 8, 10, 12, 24, 48, 96 hours post-dose
Area Under the Curve From Time Zero to Extrapolated Infinite Time (AUCinf)
AUCinf = Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0-inf). It is obtained from AUC (0-t) plus AUC (t-inf).
Measured: Crizotinib pre-dose, 1, 2, 4, 6, 8, 10, 12, 24, 48, 96 hours post-dose
Maximum Observed Plasma Concentration (Cmax)
Measured: Crizotinib pre-dose, 1, 2, 4, 6, 8, 10, 12, 24, 48, 96 hours post-dose
Secondary outcomes (8)
Time to Reach Maximum Observed Plasma Concentration (Tmax)
Measured: Crizotinib pre-dose, 1, 2, 4, 6, 8, 10, 12, 24, 48, 96 hours post-dose
Time of last observed concentration (Tlast)
Measured: Crizotinib pre-dose, 1, 2, 4, 6, 8, 10, 12, 24, 48, 96 hours post-dose
Plasma Decay Half-Life (t1/2)
Plasma decay half-life is the time measured for the plasma concentration to decrease by one half.
Measured: Crizotinib pre-dose, 1, 2, 4, 6, 8, 10, 12, 24, 48, 96 hours post-dose
Apparent Oral Clearance (CL/F)
Clearance of a drug is a measure of the rate at which a drug is metabolized or eliminated by normal biological processes. Clearance obtained after oral dose (apparent oral clearance) is influenced by the fraction of the dose absorbed. Clearance was estimated from population pharmacokinetic (PK) modeling. Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the blood.
Measured: Crizotinib pre-dose, 1, 2, 4, 6, 8, 10, 12, 24, 48, 96 hours post-dose
Apparent Volume of Distribution (Vz/F)
Volume of distribution is defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired plasma concentration of a drug. Apparent volume of distribution after oral dose (Vz/F) is influenced by the fraction absorbed.
Measured: Crizotinib pre-dose, 1, 2, 4, 6, 8, 10, 12, 24, 48, 96 hours post-dose
Number of Participants With Clinical Laboratory Abnormalities
Measured: Baseline up to 35 calendar days after the last crizotinib dose
Number of Participants With Abnormal Electrocardiogram (ECG)
Measured: Baseline up to 35 calendar days after the last crizotinib dose
Number of Adverse Events by Severity
An AE was any untoward medical occurrence attributed to study drug in a participant who received study drug. AEs are classified according to the severity in 3 categories a) mild - AEs does not interfere with participant's usual function b) moderate - AEs interferes to some extent with participant's usual function c) severe - AEs interferes significantly with participant's usual function.
Measured: Baseline up to 35 calendar days after the last crizotnib dose
Timeline
From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.
- First posted2 May 2017
- Study start20 Jun 2017
- Primary completion19 Sep 2017
- Study completion17 Oct 2017
Resources
- Official record on ClinicalTrials.govThe registry entry this page is built from, with its full change history.
- Publications (1)Papers the sponsor has linked to this study.
- Other trials for HealthyStudies of the same condition, open and under way.
- More trials run by PfizerThe sponsor's other registered studies.
- What the trial phases meanHow a treatment moves from first tests in people to approval.
More details
For doctors and researchers: how the study is designed, who runs it, and its registry IDs.
Study design
- Study type
- Interventional
- Phase
- Phase 1
- Primary purpose
- Basic science
- Allocation
- Randomised
- Intervention model
- Crossover
- Masking
- None (open label)
- Enrolment
- 18 participants (actual)
Sponsor and investigators
- Lead sponsor
- Pfizer
- Sponsor type
- Industry (pharma, biotech, devices)
- Responsible party
- Sponsor
- Investigators
- Pfizer CT.gov Call Center, Study director, Pfizer
IDs, dates and publications
- ClinicalTrials.gov ID
- NCT03137134
- Sponsor's protocol ID
- A8081066
- Other IDs
- PPI/FE
- Status last verified
- Oct 2017
- First submitted
- 26 Apr 2017
- Last updated
- 31 Oct 2017
- Results posted
- No
- Data monitoring committee
- No
- FDA-regulated drug
- Yes
- FDA-regulated device
- No
- Individual data sharing
- No: Information relating to our policy on data sharing and the process for requesting data can be found at the following link: http://www.pfizer.com/research/clinical\_trials/trial\_data\_and\_results/data\_requests
Publications
Bartlett JA, Culver N, Santangelo M, Prpich A, Long E, Sagawa K, Shanker R, Xu H, Wilner K. Development of a Taste-Masked, Dose-Flexible, Multiparticulate Pediatric Dosage Form: Case Study of Crizotinib, a Challenging Pediatric Formulation. Pharmaceut Med. 2026 May;40(3):193-207. doi: 10.1007/s40290-026-00604-2. Epub 2026 Apr 1.
PubMed 41920422
Study at a glance
From the registry record, last updated by the sponsor on 31 Oct 2017. Recruitment status is as the sponsor reported it: confirm with the study team.
- Official title
- A Phase 1, Open-label, Single Dose Study To Evaluate The Effects Of Food And The Proton Pump Inhibitor, Esomeprazole, On The Pharmacokinetics Of Crizotinib In A Coated Microsphere Formulation In Adult Healthy Volunteers
- ClinicalTrials.gov ID
- NCT03137134
- Acronym / sponsor ID
- A8081066
- Conditions
- Healthy
- Phase
- Phase 1
- Study type
- Interventional
- Recruitment status
- Completed
- Enrolment
- 18 participants (actual)
- Lead sponsor
- PfizerIndustry (pharma, biotech, devices)
- Study start
- 20 Jun 2017 (actual)
- Primary completion
- 19 Sep 2017 (actual)
- Study completion
- 17 Oct 2017 (actual)
- First posted
- 2 May 2017 (actual)
- Results
- Not posted in the source record
Clinical summary
The research question as the sponsor registered it. This describes what the study plans to test, not what it found.
This study will estimate the effect of food and the proton pump inhibitor, esomeprazole on the pharmacokinetics of crizotinib in a coated microsphere formulation.
Detailed description
This study is an open-label, randomized, 4-period, 5-treatment, 6-sequence study in adult healthy volunteers. Subjects will receive up to four separate single oral 300 mg doses of a coated microsphere (cMS) formulation of crizotinib. Period 1 through Period 3 will evaluate the effect of food, and, the effect of multiple doses of a gastrointestinal acid reducing agent, esomeprazole, in fasted state, on the pharmacokinetics (PK) of crizotinib cMS. Period 4 will evaluate whether apple sauce or orange juice may reduce the effect of multiple doses of esomeprazole on the PK of crizotinib cMS, if there is an effect.
Study design
- Primary purpose
- Basic science
- Allocation
- Randomised
- Intervention model
- Crossover
- Masking
- None (open label)
- Number of arms
- 5
| Arm | Type | Receives |
|---|---|---|
| Treatment A | Active comparator | Drug: Crizotinib(reference) Crizotinib cMS 300 mg in fasted state |
| Treatment B | Experimental | Drug: Crizotinib(test) Crizotinib cMS 300 mg in fed state |
| Treatment C | Experimental | Drug: Crizotinib, Drug: Esomeprazole(test) 5 days of esomeprazole 40 mg followed by crizotinib cMS 300 mg in fasted state |
| Treatment D | Experimental | Drug: Crizotinib, Drug: Esomeprazole(test) 5 days of esomeprazole 40 mg followed by crizotinib cMS 300 mg with apple sauce. |
| Treatment E | Experimental | Drug: Crizotinib, Drug: Esomeprazole(test) 5 days of esomeprazole 40 mg followed by crizotinib cMS 300 mg with orange juice |
Who may qualify
- Ages
- 18 to 55 years
- Sex
- All
- Healthy volunteers
- Accepted
- Age groups
- Adult
Key inclusion criteria (4 listed)
- Healthy male subjects and female subjects of nonchildbearing potential between 18 and 55 years old.
- Body mass index (BMI) of 17.5 to 30.5 kg/m2; and a total body weight >50 kg (110 lb).
- Evidence of a personally signed and dated informed consent document indicating that the subject has been informed of all pertinent aspects of the study.
- Subjects who are willing and able to comply with all scheduled visits, treatment plan, laboratory tests and other study procedures.
Key exclusion criteria (19 listed)
- 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).
- Any condition possibly affecting drug absorption (eg, gastrectomy).
- A positive urine drug test.
- Subjects who currently smoke.
- History of regular alcohol consumption exceeding 7 drinks/week for female subjects or 14 drinks/week for male subjects (1 drink = 5 ounces [150 mL] of wine or 12 ounces [360 mL] of beer or 1.5 ounces [45 mL] of hard liquor) within 6 months before screening.
Eligibility is decided by the study team after screening; this overview does not establish that a patient qualifies. Full inclusion and exclusion criteria.
Interventions
| Intervention | Type | Arms |
|---|---|---|
| CrizotinibCrizotinib in a coated microsphere formulation | Drug | Treatment A, Treatment B, Treatment C, Treatment D, Treatment E |
| EsomeprazoleProton pump inhibitor, esomeprazole | Drug | Treatment C, Treatment D, Treatment E |
Primary outcome
Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast)
Time frame: Crizotinib pre-dose, 1, 2, 4, 6, 8, 10, 12, 24, 48, 96 hours post-dose
Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast)
Area Under the Curve From Time Zero to Extrapolated Infinite Time (AUCinf)
Time frame: Crizotinib pre-dose, 1, 2, 4, 6, 8, 10, 12, 24, 48, 96 hours post-dose
AUCinf = Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0-inf). It is obtained from AUC (0-t) plus AUC (t-inf).
Maximum Observed Plasma Concentration (Cmax)
Time frame: Crizotinib pre-dose, 1, 2, 4, 6, 8, 10, 12, 24, 48, 96 hours post-dose
8 secondary outcomes
Time to Reach Maximum Observed Plasma Concentration (Tmax)
Time frame: Crizotinib pre-dose, 1, 2, 4, 6, 8, 10, 12, 24, 48, 96 hours post-dose
Time of last observed concentration (Tlast)
Time frame: Crizotinib pre-dose, 1, 2, 4, 6, 8, 10, 12, 24, 48, 96 hours post-dose
Plasma Decay Half-Life (t1/2)
Time frame: Crizotinib pre-dose, 1, 2, 4, 6, 8, 10, 12, 24, 48, 96 hours post-dose
Apparent Oral Clearance (CL/F)
Time frame: Crizotinib pre-dose, 1, 2, 4, 6, 8, 10, 12, 24, 48, 96 hours post-dose
Apparent Volume of Distribution (Vz/F)
Time frame: Crizotinib pre-dose, 1, 2, 4, 6, 8, 10, 12, 24, 48, 96 hours post-dose
Number of Participants With Clinical Laboratory Abnormalities
Time frame: Baseline up to 35 calendar days after the last crizotinib dose
Number of Participants With Abnormal Electrocardiogram (ECG)
Time frame: Baseline up to 35 calendar days after the last crizotinib dose
Number of Adverse Events by Severity
Time frame: Baseline up to 35 calendar days after the last crizotnib dose
Results and safety
The study is completed, but results are not available in the source record. That does not mean the treatment did or did not work.
Research links
- Official record on ClinicalTrials.govLast updated by the sponsor 31 Oct 2017.
- Derived from this study: PubMed 41920422Bartlett JA, Culver N, Santangelo M, Prpich A, Long E, Sagawa K, Shanker R, Xu H, Wilner K. Development of a Taste-Masked, Dose-Flexible, Multiparticulate Pediatric Dosage Form: Case Study of Crizotinib, a Challenging Pediatric Formulation. Pharmaceut Med. 2026 May;40(3):193-207. doi: 10.1007/s40290-026-00604-2. Epub 2026 Apr 1.
- To obtain contact information for a study center near you, click here.Link provided by the sponsor.
- Individual participant dataSharing planned: No. Information relating to our policy on data sharing and the process for requesting data can be found at the following link: http://www.pfizer.com/research/clinical_trials/trial_data_and_results/data_requests
Related trials for Healthy
Recruiting
THE EFFECTS OF GAME-BASED EXERCISE PROGRAMS
Physical Activity, Body Image
Not yet recruitingPhase 1
A Phase I Study of GLR2053 Tablets in Chinese Healthy Adult Participants
Atopic Dermatitis
Recruiting
Colon-delivered Riboflavin and Gut Microbiota Composition
Microbiome Dysbiosis, Gut Health
Not yet recruiting
Neuroergonomic Analysis of a Brain-Computer Interface Device (BCI)
Healthy Volunteers - Male and Female
RecruitingPhase 1
First-in-Human Trial to Assess REGN20423 in Healthy Adult Participants and Adult Participants With Atopic Dermatitis
Healthy Volunteer, Atopic Dermatitis
Referral and contact
AzTrials does not enrol participants or take referrals. Contact the study team or a site listed below; they decide who can take part. This study is not recruiting at the moment.
Pfizer CT.gov Call Center study director
Pfizer
1 site in 1 country: see every site and its status.
Questions about this trial
What is this clinical trial studying?
A Phase 1 study testing Crizotinib and Esomeprazole in people with Healthy, run by Pfizer at 1 site in United States.
The full registered description is in the About this study section and the official record.
Who may be eligible to take part?
The sponsor lists 4 inclusion and 19 exclusion criteria. Eligibility is decided by the study team after screening, so read the full criteria and contact a listed site.
Is this clinical trial currently recruiting?
The record says: finished, as of the sponsor's last update on 31 Oct 2017. Status can change between updates, so confirm with the study contact before making plans.
Where is the study taking place?
The record lists 1 site in United States. Whether a site is taking part right now should be confirmed with that site. See every site.
What are the possible benefits and risks?
They depend on the study and the treatment, and no study can promise a benefit. The study team explains the known risks during informed consent, before anyone joins; the record itself does not list them.
What does this phase mean?
Phase 1 studies test a treatment in a small group of people for the first time or in a new way, mainly to check safety and find the right dose.
Not every study follows the same path, and some studies (observational studies, device studies) have no phase.
Are results available for this study?
The study is completed, but results are not available in the source record. That does not mean the treatment did or did not work.
How can a doctor refer a patient or contact the research team?
The record lists no contact. The official record names the sponsor, who can be asked directly. AzTrials does not enrol participants or take referrals.
What does the primary outcome measure?
Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) (time frame: Crizotinib pre-dose, 1, 2, 4, 6, 8, 10, 12, 24, 48, 96 hours post-dose). The study lists 3 primary outcomes in all. It is what the study was designed to measure, not a finding.
Where can I read the original study information?
On the ClinicalTrials.gov record for NCT03137134, which also lists 1 linked publication.
Does a listing mean the treatment is approved or proven to work?
No. A listing means the study is registered. It does not show that the treatment is safe, works, or is approved by a regulator.
How often is this information updated?
AzTrials copies changed records from ClinicalTrials.gov every night and reloads the whole registry every week. The sponsor last updated this record on 31 Oct 2017.