A Phase 1 Study To Evaluate The Pharmacokinetics And Safety Of Three Modified Release And One Immediate Release Formulations Of Tofacitinib (CP-690,550) In Healthy Volunteers

A Phase 1, Randomized, Open Label, Partial Crossover Study To Evaluate The Pharmacokinetics (PK) And Safety Of Three Modified Release (MR) And One Immediate Release (IR) Formulations Of Tofacitinib (CP-690,550) In Healthy Volunteers

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT01499004

Enrollment

Registered

2011-12-26

Start date

2011-11-30

Completion date

2011-12-31

Last updated

2012-01-12

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Healthy

Keywords

tofacitinib, CP-690, 550, relative bioavailability, modified release, Phase 1

Brief summary

This study will explore the drug behavior and safety following a single dose of three different 22 milligram tofacitinib (CP-690,550) modified-release formulations in 30 healthy volunteers. These formulations will be compared to 10 milligram tofacitinib (CP-690-550) in an immediate-release formulation.

Interventions

DRUGtofacitinib (CP-690,550) modified-release formulation A

A single dose of 22 mg tofacitinib (CP-690,550) modified-release formulation A administered with food.

DRUGtofacitinib (CP-690,550) modified-release formulation B1

A single dose of 22 mg tofacitinib (CP-690,550) MR-B1 formulation administered with food

DRUGtofacitinib (CP-690,550) modified-release formulation B2

A single dose of 22 mg tofacitinib (CP-690,550) modified-release formulation B2 administered without food

DRUGtofacitinib (CP-690,550) immediate-release formulation

A single dose of 10 mg tofacitinib (CP-690,550) immediate-release formulation administered without food

Study design

Allocation

RANDOMIZED

Intervention model

CROSSOVER

Primary purpose

BASIC_SCIENCE

Masking

NONE

Eligibility

Sex/Gender

ALL

Age

21 Years to 55 Years

Healthy volunteers

Yes

Inclusion criteria

* Healthy male subjects and/or healthy females subjects who are of non-childbearing potential.

Exclusion criteria

* Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurologic, or allergic disease; * Clinically significant infections within the past 3 months

Design outcomes

Primary

Measure	Time frame
Tmax: Amount of time tofacitinib (CP-690,550) is at maximum plasma concentration	72 hours post dose
AUCinf: Area under the plasma concentration-time profile from time 0 exprapolated to infinite time	72 hours post dose
AUClast: Area under the plasma concentration-time profile from time 0 to the last with quantifiable concentration	72 hours post dose
Cmax: Maximum plasma concentration of tofacitinib (CP-690,550)	72 hours post dose
t1/2: The time required for one half of the total amount of tofacitinib (CP-690,550) to be removed from the plasma	72 hours post dose

Secondary

Measure	Time frame
Frel: Relative bioavailability (Frel) of tofacitinib (CP-690,550) in the modified-release formulations compared to the immediate release formulation	24 hours post dose

Countries

Singapore

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026