|View printer-friendly version|
|Rigel's R788 Significantly Improves Rheumatoid Arthritis in Phase 2b Clinical Trial|
Expected and Manageable Safety Profile Demonstrated in TASKi2
Rigel will host a conference call today at
"These are impressive results," said
Efficacy Results Treatment N of Pts ACR 20 ACR 50 ACR 70 DAS28<2.6 Placebo 153 53 (35%) 29 (19%) 16 (10%) 9 (6%) 150 mg qd 152 87 (57%) 49 (32%) 21 (14%) 26 (17%) p<0.001 p=0.007 p=0.34 p=0.003 100 mg bid 152 101 (66%) 65 (43%) 43 (28%) 41 (27%) p<0.001 p<0.001 p<0.001 <0.001 p values compared to placebo Note: At 6 months. All patients were on stable doses of methotrexate throughout the clinical trial. * The results presented are based on an intention to treat analysis that includes all randomized patients, regardless of how long treatment lasted. Any patient who dropped out of the study for any reason, or for whom month 6 data were unavailable, was considered a treatment failure (ACR non-responder). Disease Activity Scores are based on a 28 joint count and CRP or an ESR at week 24 (depending on which was the qualifying biomarker).
The most common clinically meaningful drug-related adverse events noted in TASKi2 were diarrhea and hypertension. Dose reduction options were pre-specified in the trial protocol and in cases where doses were reduced, patients generally completed the clinical trial with minimal safety issues. The most common adverse events in the trial overall were related to infections, though these were generally evenly distributed among the placebo and active dose groups.
The mean increase in blood pressure from baseline at 6 months, using a last observation carry forward methodology, was less than 0.5 mmHg for the 150 mg qd dose group and approximately 1 mmHg for the 100 mg bid dose group. Approximately 18% and 23% of patients in the 150 mg qd and the 100 mg bid dose groups, respectively, had blood pressure medication adjusted or in some cases initiated during the course of the study, compared with 7% of the placebo patients. The blood pressure was successfully reduced in these patients, and their blood pressure was generally well controlled throughout the trial. The blood pressure medications were standard doses of common blood pressure medications such as ACE inhibitors or diuretics.
"R788 continues to perform with strong efficacy and good tolerability in the groups of patients with RA who have failed to respond to methotrexate," said Elliott Grossbard, M.D., chief medical officer for Rigel. "We now have a much better understanding of R788's safety profile and believe that the observed side effects may be effectively managed," he added.
Safety Results Tables (N) Placebo (153) 150 mg qd (152) 100 mg bid (152) Dose Reductions N % N % N % # Had a Dose Reduction 6 4% 21 14% 21 14% Neutropenia (ANC <1500) 1 1% 6 4% 1 1% Diarrhea, nausea, vomiting, dizziness 1 1% 5 3% 9 6% Increase in Blood Pressure 2 1% 4 3% 6 4% ALT or Alkphos Elevation 2 1% 6 4% 5 3% Treatment Emergent Adverse Events N % N % N % Diarrhea 5 3% 18 12% 29 19% Hypertension 7 5% 18 12% 21 14% Infections 42 27% 37 24% 53 35% Mean Blood Pressure (Systolic/Diastolic in mmHg) mmHg mmHg mmHg Baseline 125/76 125/77 125/77 At Month 6 123/76 125/77 125/78 Change from Baseline to Month 6 (LOCF) -1.8/+0.4 +0.2/+0.3 +0.6/+1.4 Mean Systolic BP if had Adjustment or Initiation of BP Medication (mmHg) # Had BP Meds Adjusted/Initiated 11 (7%) 27 (18%) 35 (23%) BP Measurement Pre-Adjustment/Initiation 139 149 153 At Month 6 136 128 138 Mean Change -4 -20 -16
TASKi2 was a 6 month, multi-center, randomized, double blind, placebo
controlled, parallel dose clinical trial involving 457 RA patients in the
U.S., Latin America and
Efficacy assessments for each participant were based on the
R788 and RA
RA is a progressive, painful and potentially debilitating disease, that affects more than 2 million people in the U.S. It is a chronic inflammatory disease that puts the body's immune system into overdrive where it ultimately causes inflammation in the joints and destroys soft tissues, cartilage and bone. Rigel's R788 is a novel, orally available syk kinase inhibitor designed to interrupt the cellular signaling at the trigger point of inflammation, thereby stopping the progression of the disease.
Conference Call and Webcast Information
Rigel will host a conference call to discuss the R788 TASKi2 Phase 2b
clinical trial of R788 in rheumatoid arthritis, the Company's plans for
further development and related matters today,
About Rigel (www.Rigel.com)
Rigel is a clinical-stage drug development company that discovers and develops novel, small molecule drugs for the treatment of inflammatory/autoimmune diseases and metabolic diseases. Our pioneering research focuses on intracellular signaling pathways and related targets that are critical to disease mechanisms. Rigel's productivity has resulted in strategic collaborations with large pharmaceutical partners to develop and market our product candidates. Rigel has product development programs in inflammatory/autoimmune diseases such as rheumatoid arthritis, thrombocytopenia and asthma, as well as in cancer.
This press release contains "forward-looking" statements, including
statements related to the potential efficacy and commercial potential of R788
and Rigel's plans to pursue further clinical development thereof and a
corporate partnership. Any statements contained in this press release that
are not statements of historical fact may be deemed to be forward-looking
statements. Words such as "believe," "plan" and similar expressions are
intended to identify these forward-looking statements. There are a number of
important factors that could cause Rigel's results to differ materially from
those indicated by these forward-looking statements, including risks
associated with entering into a corporate partnership agreement and reliance
on a corporate partner, the timing and success of clinical trials and the
commercialization of product candidates, potential problems that may arise in
the clinical testing and approval process and Rigel's need for additional
capital, as well as other risks detailed from time to time in Rigel's SEC
reports, including its Form 10-Q for the quarter ended