Safety, Pharmacokinetic (PK), Pharmcodynamic (PD), and Drug-Drug Interaction of PLX3397 in Patients With Rheumatoid Arthritis Who Are Receiving Methotrexate
![]() |
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: NCT01090570 |
Recruitment Status
:
Withdrawn
First Posted
: March 22, 2010
Last Update Posted
: March 17, 2015
|
- Study Details
- Tabular View
- No Results Posted
- Disclaimer
- How to Read a Study Record
Condition or disease | Intervention/treatment | Phase |
---|---|---|
Rheumatoid Arthritis | Drug: PLX3397 | Phase 1 |
Study Type : | Interventional (Clinical Trial) |
Actual Enrollment : | 0 participants |
Allocation: | Randomized |
Intervention Model: | Parallel Assignment |
Masking: | Triple (Participant, Investigator, Outcomes Assessor) |
Primary Purpose: | Treatment |
Study Start Date : | May 2010 |
Estimated Primary Completion Date : | December 2010 |

Arm | Intervention/treatment |
---|---|
Experimental: PLX3397 25 mg |
Drug: PLX3397
Once-daily oral capsules
|
Experimental: PLX3397 50 mg |
Drug: PLX3397
Once-daily oral capsules
|
Experimental: PLX3397 100 mg |
Drug: PLX3397
Once-daily oral capsules
|
Experimental: PLX3397 200 mg |
Drug: PLX3397
Once-daily oral capsules
|
Experimental: PLX3397 300 mg |
Drug: PLX3397
Once-daily oral capsules
|
Placebo Comparator: Placebo |
Drug: PLX3397
Once-daily oral capsules
|
- To assess the drug-drug interaction of PLX3397 and Methotrexate in patients with rheumatoid arthritis [ Time Frame: 2 weeks + 2 weeks follow up ]Blood samples will be taken at multiple time points during the 2 week time frame plus a 2 week follow up time frame to study the pharmacokinetics of PLX3397 and Methotrexate in patients.
- To assess the safety and tolerability of PLX3397 when taken once daily with concomitant methotrexate administration [ Time Frame: 4 weeks ]Adverse events and safety lab tests (including a hematology panel, blood chemistry panel, coagulation and urinalysis) will be monitored throughout the study time frame.
- To assess the pharmacokinetics of PLX3397 when taken once daily for 2 weeks at either a 25, 50, 100, 200 or 300 mg dose. [ Time Frame: 2 weeks ]The pharmacokinetic profile of plasma PLX3397 will be analyzed by measurement of area under the plasma concentration-time curve (AUC0-t, AUC0-inf), peak concentration (Cmax), time to peak concentration (Tmax), half-life (t1/2), and terminal elimination rate constant (Kel).
- To assess the pharmacodynamics of PLX3397 when taken once daily for 2 weeks at either a 25, 50, 100, 200 or 300 mg dose. [ Time Frame: 4 weeks ]Measured by looking at the factors in the blood that may include, but are not limited to pro- and anti-inflammatory cytokines and mediators of the inflammatory process that may correlate with the activity of the disease and the response to PLX3397 in combination with methotrexate

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 and older (Adult, Senior) |
Sexes Eligible for Study: | All |
Accepts Healthy Volunteers: | No |
Inclusion Criteria:
- Male or female patients ≥ 18 years old with a diagnosis of rheumatoid arthritis by ACR criteria for ≥ 3 months.
- Prior to Baseline, patients must be on oral or subcutaneous methotrexate (≥ 10 mg/week and ≤ 25 mg/week) for at least 12 weeks (with a stable dose for at least 4 weeks) and folate (≥ 5 mg/week) for at least 6 weeks, and willing to continue on this regimen for the duration of the study.
- Adequate hematologic, hepatic, and renal function (absolute neutrophil count ≥ 1.5 X 109/L, Hgb > 9 g/dL, platelet count ≥ 100 X 109/L, AST/ALT WNL, albumin ≥ 3 g/dL, calculated CrCl>60 mL/min using Cockcroft-Gault formula).
- Women of child-bearing potential must have a negative pregnancy test within 7 days prior to initiation of dosing and must agree to use a double barrier method of birth control from the time of the negative pregnancy test up to 30 days after the last dose of study drug. Women of non-childbearing potential may be included if they are either surgically sterile or have been postmenopausal for ≥1 year.
- Fertile men must agree to use an acceptable method of birth control while on study drug. Acceptable methods of contraception must include either abstinence from the first dose of study drug through 4 weeks after the last dose of study drug, or use of a condom with instructions to the female partner of child-bearing potential to also be protected as above.
- Willing and able to provide written informed consent prior to any study related procedures and to comply with all study requirements.
Exclusion Criteria:
- Use of biologic response modifiers within the following periods prior to Day 1 Baseline: 4 weeks for Kineret (anakinra) and Enbrel (etanercept); 12 weeks for Remicade (infliximab), Humira (adalimumab), Simponi (golimumab), Orencia (abatacept), Actemra (tocilizumab), or Cimzia (certolizumab); 12 months for Rituxan.
- Use of Arava (leflunomide) within 12 weeks prior to Day 1 Baseline or any immunosuppressive agents other then hydroxychloroquine or sulfasalazine within 4 weeks of Day 1 Baseline.
- Investigational drug use within 4 weeks of Day 1 Baseline.
- Concomitant use of DMARDs (other than methotrexate), biological response modifiers, or known strong inducers or inhibitors of CYP3A4.
- Positive HepBsAg or HCV, or presence of clinically significant hepatic or biliary disease.
- Uncontrolled intercurrent illness.
- Refractory nausea and vomiting, malabsorption, external biliary shunt, or significant bowel resection that would preclude adequate absorption.
- QTc ≥ 450 msec at Screening.
- The presence of a medical or psychiatric condition that, in the opinion of the Principal Investigator, makes the patient inappropriate for inclusion in this study.

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): NCT01090570
United States, Alabama | |
Tuscaloosa, Alabama, United States | |
United States, Arkansas | |
Little Rock, Arkansas, United States | |
United States, California | |
San Francisco, California, United States | |
United States, Pennsylvania | |
Altoona, Pennsylvania, United States | |
United States, Texas | |
Dallas, Texas, United States |
ClinicalTrials.gov Identifier: | NCT01090570 History of Changes |
Other Study ID Numbers: |
PLX108-02 |
First Posted: | March 22, 2010 Key Record Dates |
Last Update Posted: | March 17, 2015 |
Last Verified: | March 2015 |
Additional relevant MeSH terms:
Arthritis Arthritis, Rheumatoid Joint Diseases Musculoskeletal Diseases |
Rheumatic Diseases Connective Tissue Diseases Autoimmune Diseases Immune System Diseases |