A Study to Determine the Safety and Efficacy of LX3305 in Subjects With Active Rheumatoid Arthritis

Lexicon Pharmaceuticals

Status and phase: Completed; Phase 1

Conditions: Rheumatoid Arthritis

Treatments: Drug: 200 mg LX3305 QD; Drug: 150 mg LX3305 QD; Drug: 500 mg LX3305 QD; Drug: 50 mg LX3305 QD; Drug: 300 mg LX3305 QD; Drug: 400 mg LX3305 QD; Drug: 250 mg LX3305 QD; Drug: 100 mg LX3305 QD; Drug: 250 mg LX3305 BID; Drug: Placebo

Study type: Interventional

Funder types: Industry

Identifiers

NCT01417052

LX3305.106 (Other Identifier)

LX3305.1-106-RA

Details and patient eligibility

About

The primary objective of this study is to determine the safety of LX3305 in a dose escalation compared with placebo over 12 weeks in subjects with active rheumatoid arthritis (RA).

Enrollment: 10 patients

Sex: All

Ages: 18 to 75 years old

Volunteers: No Healthy Volunteers

Inclusion criteria

• Adult subjects, aged 18 to 75 years
• Active rheumatoid arthritis (RA), class I to III (defined by the American College of Rheumatology), diagnosed at least 3 months prior to Screening
• Minimum of 4 swollen joints (at Screening and Day 1), minimum of 4 tender joints (at Screening and Day 1), and serum C-reactive protein (CRP) level >1.2x the upper limit of normal and/or elevated erythrocyte sedimentation rate (ESR)
• If receiving methotrexate (7.5 mg to 25 mg/week), subject must have been treated for at least 6 weeks prior to Screening and currently receiving a stable dose of methotrexate (MTX) with a stable route of administration, and have no plans to change MTX dose during the study
• Ability to give written informed consent

Exclusion criteria

• Women who are pregnant or nursing
• RA diagnosis prior to 16 years of age (juvenile RA)
• Intra-articular and/or parenteral corticosteroids within 4 weeks of study Day 1
• Receipt of live vaccine within 4 weeks prior to Day 1
• Major surgical procedure within 8 weeks prior to Day 1
• Blood donation within 4 weeks prior to Day 1
• Any systemic inflammatory condition
• History of bleeding diathesis
• History of medically significant opportunistic infection
• History of drug or alcohol abuse within 3 years prior to Day 1
• History of cancer within 5 years prior to Day 1
• Presence of hepatic or biliary disease
• History of tuberculosis
• History of human immunodeficiency virus (HIV)
• Any clinically significant laboratory test results, in the opinion of the investigator
• Use of any investigational agent or participation in an investigative trial within 30 days of Day 1
• Concurrent use of any biologic agent for the treatment of RA or concomitant disease modifying antirheumatoid drugs (other than MTX, hydroxychloroquine, leflunomide, and sulfasalazine - at stables doses for 8 weeks)

Trial design

Primary purpose: Treatment

Allocation: Randomized

Interventional model: Single Group Assignment

Masking: Quadruple Blind

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10 participants in 10 patient groups, including a placebo group

50 mg LX3305 QD

Experimental group

Treatment:

Drug: 50 mg LX3305 QD

100 mg LX3305 QD

Experimental group

Treatment:

Drug: 100 mg LX3305 QD

150 mg LX3305 QD

Experimental group

Treatment:

Drug: 150 mg LX3305 QD

200 mg LX3305 QD

Experimental group

Treatment:

Drug: 200 mg LX3305 QD

250 mg LX3305 QD

Experimental group

Treatment:

Drug: 250 mg LX3305 QD

300 mg LX3305 QD

Experimental group

Treatment:

Drug: 300 mg LX3305 QD

400 mg LX3305 QD

Experimental group

Treatment:

Drug: 400 mg LX3305 QD

250 mg LX3305 BID

Experimental group

Treatment:

Drug: 250 mg LX3305 BID

500 mg LX3305 QD

Experimental group

Treatment:

Drug: 500 mg LX3305 QD

Placebo

Placebo Comparator group

Treatment:

Drug: Placebo