Rigel's R788 Demonstrates Significant Improvement in Rheumatoid Arthritis in Phase 2 Clin...(100mg 150mg ...),Health

po BID N=47 po BID N=46 po BID N=49 po BID N=47

Completed Study at

Reduced Dose (N) 1 0 5 13

Dropouts (N): 11 6 6 8

Withdrew Consent 6 3 2 1

Adverse Event 2 1 3 6

Other 3 2 1 1

Neutropenia (N)

Requiring dose reduction 0 0 5 10

ALT > 3XULN (N) 2 0 0 3

Diarrhea (N)

(severity moderate

or greater) 0 3 2 10

Upper GI side effects (N)

(gastritis, nausea,

dyspepsia) (severity

moderate or greater) 2 1 2 12

Hypertension (N)

(severity moderate

or greater) 0 0 2 0

Note: At 12 weeks. All patients were on stable doses of methotrexate

throughout the clinical trial period and extension.

Study Design

The clinical trial was a multi-center, randomized, double blind, placebo controlled, ascending dose study involving 189 patients in three approximately equal size cohorts receiving 50, 100, or 150 mg po bid. Within each cohort, patients were assigned on a 3:1 basis to R788 or placebo. The clinical trial was conducted over a 12-week treatment period in patients who had RA for at least 12 months. These patients had active disease despite receiving adequate stable doses of methotrexate over the preceding 6 months. All of the patients continued to receive their same stable dose of methotrexate throughout the clinical trial period and extension. Efficacy assessments for each participant were based on the American College of Rheumatology crit
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