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tofacitinib modified release

Phase 1

Healthy | Small molecule | Other |Pfizer, Inc.|Last Updated: Oct 29, 2020

Success Probability

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Market & Valuation

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Trial Design

RandomizedACTIVE_CONTROLLED
Total Trials3
Total Enrollment67

FDA Designations

No designations recorded

Clinical trial landscape

tofacitinib modified release · 3 trials · 1 indication

Phase 1 3
NCT04338711A Study In Adult Healthy Volunteers To Asses Once Daily (QD) Dosing With The Selected Age-Appropriate Modified Release (MR) FormulationsHealthy
COMPLETED23 Analytics
NCT02084875A Study To Evaluate The Effect Of Food On The Behavior Of Tofacitinib Modified Release 11 Milligram Tablets In Healthy Western And Japanese VolunteersHealthy
COMPLETED24 Analytics
NCT01731327A Phase 1 Study To Evaluate The Pharmacokinetics (PK), Safety, And Bioavailability Of A Modified-Release (MR) Formulation Of Tofacitinib In Healthy VolunteersHealthy
COMPLETED20 Analytics
PHASE1COMPLETED
A Study In Adult Healthy Volunteers To Asses Once Daily (QD) Dosing With The Selected Age-Appropriate Modified Release (MR) Formulations
HealthyUnlock trial analytics
PHASE1COMPLETED
A Study To Evaluate The Effect Of Food On The Behavior Of Tofacitinib Modified Release 11 Milligram Tablets In Healthy Western And Japanese Volunteers
HealthyUnlock trial analytics
PHASE1COMPLETED
A Phase 1 Study To Evaluate The Pharmacokinetics (PK), Safety, And Bioavailability Of A Modified-Release (MR) Formulation Of Tofacitinib In Healthy Volunteers
HealthyUnlock trial analytics

Study Endpoints

Primary Endpoints

Primary outcome: Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)] (AUCinf )
0.5, 1, 2, 3, 4, 5, 6, 9, 21, 24, 36, and 48 hours post dose

Area Under the Curve From Time Zero to Extrapolated Infinite Time \[AUC (0 - ∞)\]

Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast)
0.5, 1, 2, 3, 4, 5, 6, 9, 21, 24, 36, and 48 hours post dose

Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast) of Modified Release (MR) formulation compared to Immediate Release (IR) solution

Maximum Observed Plasma Concentration (Cmax)
predose, 0.5, 1, 2, 3, 4, 5, 6, 9, 21, 24, 36, and 48 hours post dose

Maximum (or peak) plasma concentration of MR formulation compared to IR solution

Time to Reach Maximum Observed Plasma Concentration (Tmax)
predose, 0.5, 1, 2, 3, 4, 5, 6, 9, 21, 24, 36, and 48 hours post dose

Maximum time to peak plasma concentration of MR formulation compared to IR solution

Area under the curve from time zero to infinity
48 hours post dose
Area under the plasma concentration-time profile from time zero to time of the last quantifiable concentration
48 hours post dose
AUCinf(dn): Area Under the Curve From Time Zero to Infinity, dose-normalized
72 hours post dose
Cmax(dn): Maximum Observed Plasma Concentration (Cmax), dose normalized
72 hours post dose

Secondary Endpoints

Number of Participants with Treatment-Emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)
Through study completion, approximately 3 months
Number of Treatment Emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs) Leading to Discontinuation
Through study completion, approximately 3 months
Number of Participants With Clinically Significan Change from Baseline in Physical Examination Findings
Through study completion, approximately 3 months
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Study Design & Arms

AllocationRANDOMIZED
MaskingNONE
ModelCROSSOVER
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Treatment AEXPERIMENTALSingle oral 10 mg dose of tofacitinib MR E1 administered in the fasted state.
Treatment BEXPERIMENTALSingle oral 10 mg dose of tofacitinib MR E2 administered in the fasted state.
Treatment CEXPERIMENTALSingle oral 10 mg dose of tofacitinib MR E3 administered in the fasted state.
Treatment DEXPERIMENTALSingle oral 10 mg dose of tofacitinib MR E1 administered in the fed state.
Treatment EEXPERIMENTALSingle oral 10 mg dose of tofacitinib MR E3 administered in the fed state.
Treatment FACTIVE_COMPARATORSingle oral 10 mg dose of tofacitinib IR Solution (10 mL of the 1 mg/mL solution) administered in the fasted state.
tofacitinib MR 11 mg FedEXPERIMENTALtofacitinib modified release (MR) 11 mg tablet administered with food.
tofacitinib MR 11 mg FastingEXPERIMENTALtofacitinib modified release (MR) 11 mg tablet administered without food.
Experimental Treatment AEXPERIMENTALA single dose of 11 mg tofacitinib modified-release (MR) administered in a fasting state.
Experimental Treatment BEXPERIMENTALA single dose of 22 mg tofacitinib modified-release (MR) administered in a fasting state.

Interventions

NameTypeDescription
tofacitinib modified release (MR)DRUGSingle oral 10 mg multi particulate dose of dose of tofacitinib MR with different levels of enteric coating (MR E1, MR E2, and MR E3) in the fasted state. Additionally, the lowest and highest enteric coating levels will also be evaluated in the fed state. Treatment F: a 10 mg oral dose of tofacitinib IR solution
tofacitinib modified-release (MR) formulationDRUGA single dose of tofacitinib modified release 11 mg tablet after receiving the standard FDA high fat/high calorie meal.
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Eligibility Criteria

Age Range18 Years to 55 Years
SexALL
Healthy VolunteersYes
Study Sites1

Inclusion Criteria: * Healthy male and/or female subjects of non-childbearing potential between the ages of 18 and 55 years, inclusive. * Female subjects of non-childbearing potential must meet at least 1 of the following criteria: 1. . Achieved postmenopausal status, defined as: cessation of re...

Countries:United StatesSingapore
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Frequently asked questions about tofacitinib modified release

What is tofacitinib modified release used for?

Tofacitinib modified release is an investigational small molecule being studied in healthy volunteers. It is a modified-release formulation of tofacitinib, and the Phase 1 trials evaluate its pharmacokinetics, safety, bioavailability, and the effect of food on its behavior. It is not approved and remains in clinical development.

Who makes tofacitinib modified release?

Tofacitinib modified release is being developed by Pfizer, Inc., traded on the New York Stock Exchange under the ticker PFE. Pfizer is conducting Phase 1 clinical trials of this modified-release formulation in healthy volunteers.

What phase is tofacitinib modified release in?

Tofacitinib modified release is in Phase 1 clinical development. All three completed trials are Phase 1 studies in healthy volunteers, and the drug is investigational, not FDA approved.

What clinical trials is tofacitinib modified release in?

Tofacitinib modified release has three completed Phase 1 trials: NCT01731327 in Singapore, NCT02084875 in the United States, and NCT04338711 in the United States. These studies enrolled a total of 67 healthy volunteers and evaluated pharmacokinetics, safety, bioavailability, food effects, and once-daily dosing.

Is tofacitinib modified release the same as tofacitinib?

Tofacitinib modified release is a modified-release formulation of tofacitinib, designed for once-daily dosing. The clinical trials compare it to other formulations of tofacitinib, but it is a distinct dosage form being studied separately in healthy volunteers.