Co-Administration Of Methotrexate And CP-690,550
![]() |
The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Read our disclaimer for details. |
ClinicalTrials.gov Identifier: NCT01745055 |
Recruitment Status :
Completed
First Posted : December 7, 2012
Results First Posted : December 7, 2012
Last Update Posted : February 4, 2013
|
- Study Details
- Tabular View
- Study Results
- Disclaimer
- How to Read a Study Record
Condition or disease | Intervention/treatment | Phase |
---|---|---|
Rheumatoid Arthritis | Drug: CP-690,550 (tofacitinib) Drug: Methotrexate (MTX) | Phase 1 |
Study Type : | Interventional (Clinical Trial) |
Actual Enrollment : | 12 participants |
Allocation: | Non-Randomized |
Intervention Model: | Single Group Assignment |
Masking: | None (Open Label) |
Primary Purpose: | Basic Science |
Official Title: | A Phase 1, Open Label Study Of The Pharmacokinetics Of Multiple Doses Of Oral CP-690,550 And Single Doses Of Oral Methotrexate In Rheumatoid Arthritis Subjects |
Study Start Date : | April 2005 |
Actual Primary Completion Date : | June 2006 |
Actual Study Completion Date : | June 2006 |

Arm | Intervention/treatment |
---|---|
Experimental: CP-690,550 (tofacitinib) 30 mg q12h
Individual dose of methotrexate with the addition of CP-690,550 30 mg q12h
|
Drug: CP-690,550 (tofacitinib)
CP-690,550 30 mg q12h for 5 days Drug: Methotrexate (MTX) individual dose of methotrexate (stably dosed) |
- Area Under the Curve From Time Zero to 12 Hours [AUC (0-12)] for CP-690,550 [ Time Frame: 0 (pre-dose), 0.25, 0.5, 1, 2, 3, 4, 8 and 12 hours post-dose on Day 6 and Day 7 ]AUC (0-12)= area under the plasma concentration time-curve from time zero (pre-dose) to 12 hours (0-12).
- Maximum Observed Plasma Concentration (Cmax) for CP-690,550 [ Time Frame: 0 (pre-dose), 0.25, 0.5, 1, 2, 3, 4, 8 and 12 hours post-dose on Day 6 and Day 7 ]
- Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) for Methotrexate (MTX) [ Time Frame: 0 (pre-dose), 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 and 48 hours post-dose on Day 1 and Day 7 ]Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast).
- Maximum Observed Plasma Concentration (Cmax) for Methotrexate (MTX) [ Time Frame: 0 (pre-dose), 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8,12, 24 and 48 hours post-dose on Day 1 and Day 7 ]
- Time to Reach Maximum Observed Plasma Concentration (Tmax) for CP-690,550 [ Time Frame: 0 (pre-dose), 0.25, 0.5, 1, 2, 3, 4, 8 and 12 hours post-dose on Day 6 and Day 7 ]
- Plasma Decay Half-Life (t1/2) for CP-690,550 [ Time Frame: 0 (pre-dose), 0.25, 0.5, 1, 2, 3, 4, 8 and 12 hours post-dose on Day 6 and Day 7 ]Plasma decay half-life is the time measured for the plasma concentration of CP-690,550 to decrease by one half.
- Apparent Oral Clearance (CL/F) for CP-690,550 [ Time Frame: 0 (pre-dose), 0.25, 0.5, 1, 2, 3, 4, 8 and 12 hours post-dose on Day 6 and Day 7 ]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 PK modeling. Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the blood.
- Time to Reach Maximum Observed Plasma Concentration (Tmax) for Methotrexate (MTX) [ Time Frame: 0 (pre-dose), 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8 ,12, 24 and 48 hours post-dose on Day 1 and Day 7 ]
- Plasma Decay Half-Life (t1/2) for Methotrexate (MTX) [ Time Frame: 0 (pre-dose), 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8 , 12, 24 and 48 hours post-dose on Day 1 and Day 7 ]Plasma decay half-life is the time measured for the plasma concentration of MTX to decrease by one half.
- Apparent Oral Clearance (CL/F) for Methotrexate (MTX) [ Time Frame: 0 (pre-dose), 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8 , 12, 24 and 48 hours post-dose on Day 1 and Day 7 ]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 PK modeling. Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the blood.
- Total Amount of Unchanged Drug Excreted in the Urine From Time Zero to 12 Hours (Ae[0-12]) for CP-690,550 [ Time Frame: 0 (pre-dose) through 12 hours post-dose on Day 6 and Day 7 ]
- Renal Clearance (CL R) for CP-690,550 [ Time Frame: 0 (pre-dose) through 24 hours post-dose on Day 6 and Day 7 ]
- Total Amount of Unchanged Drug Excreted in the Urine From Time Zero to 24 Hours (Ae[0-24]) for Methotrexate (MTX) [ Time Frame: 0 (pre-dose) through 24 hours post-dose on Day 1 and Day 7 ]
- Renal Clearance (CL R) for Methotrexate (MTX) [ Time Frame: 0 (pre-dose) through 24 hours post-dose on Day 1 and Day 7 ]

Choosing to participate in a study is an important personal decision. Talk with your doctor and family members or friends about deciding to join a study. To learn more about this study, you or your doctor may contact the study research staff using the contacts provided below. For general information, Learn About Clinical Studies.
Ages Eligible for Study: | 18 Years to 70 Years (Adult, Older Adult) |
Sexes Eligible for Study: | All |
Accepts Healthy Volunteers: | No |
Inclusion Criteria:
- Adults diagnosed with moderate to severe RA (Rheumatoid Arthritis)
- Diagnosis of RA based on the American College of Rheumatology 1987 revised criteria.
- Treatment with an oral stable weekly dose of Methotrexate (MTX) (15-25 mg/week, administered as a single dose [SD]) for a minimum of 4 doses (4 weeks)
Exclusion Criteria:
- Blood dyscrasias including confirmed: Hemoglobin <9 g/dL or Hematocrit <30%; White blood cell count <3.0 x 109/L; Absolute neutrophil count <1.2 x 109/L; Platelet count <100 x 109/L
- Evidence or history of clinically significant infections within the past 6 months (eg, those requiring hospitalization, requiring parenteral antimicrobial therapy, or those with recurrent oral or genital herpes, recurrent herpes zoster, or any infection otherwise judged by the investigator to have the potential for exacerbation by participation in the trial.
- Total bilirubin, AST (aspartate aminotransferase) or ALT (alanine aminotransferase) more than 1.2 times the upper limit of normal at the Screening visit, or a history of clinically significant elevated liver function tests (LFTs) while on current MTX dose or chronic liver disease, recent or active hepatitis.

To learn more about this study, you or your doctor may contact the study research staff using the contact information provided by the sponsor.
Please refer to this study by its ClinicalTrials.gov identifier (NCT number): NCT01745055
United States, Florida | |
Pfizer Investigational Site | |
Daytona Beach, Florida, United States, 32114 | |
Pfizer Investigational Site | |
Fort Lauderdale, Florida, United States, 33301 | |
Pfizer Investigational Site | |
Miramar, Florida, United States, 33025 | |
United States, Texas | |
Pfizer Investigational Site | |
Dallas, Texas, United States, 75247 |
Study Director: | Pfizer CT.gov Call Center | Pfizer |
Responsible Party: | Pfizer |
ClinicalTrials.gov Identifier: | NCT01745055 |
Other Study ID Numbers: |
A3921013 |
First Posted: | December 7, 2012 Key Record Dates |
Results First Posted: | December 7, 2012 |
Last Update Posted: | February 4, 2013 |
Last Verified: | January 2013 |
Pharmacokinetics oral JAK inhibitor methotrexate (MTX) rheumatoid arthritis (RA) |
Arthritis Arthritis, Rheumatoid Joint Diseases Musculoskeletal Diseases Rheumatic Diseases Connective Tissue Diseases Autoimmune Diseases Immune System Diseases Methotrexate Tofacitinib Abortifacient Agents, Nonsteroidal Abortifacient Agents Reproductive Control Agents |
Physiological Effects of Drugs Antimetabolites, Antineoplastic Antimetabolites Molecular Mechanisms of Pharmacological Action Antineoplastic Agents Dermatologic Agents Enzyme Inhibitors Folic Acid Antagonists Immunosuppressive Agents Immunologic Factors Antirheumatic Agents Nucleic Acid Synthesis Inhibitors Protein Kinase Inhibitors |