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The details are as follows: Session Title: Acquired and inherited platelet disorders Oral Presentation: "Treatment of Primary Adult Chronic Immune Thrombocytopenia (CITP) with Fostamatinib, an Oral SYK Inhibitor: Results of Two Randomized, Placebo-Controlled Phase 3 Studies" Date: Saturday, June 24, 2017 Time: 12:30 - 12:45pm CEST Location: IFEMA - Feria de Madrid: Avda. del Partenón, 5, 28042 Madrid, Spain, Room N101 Final Abstract Code: S435 The recently accepted NDA is supported by data from the Phase 3 clinical program for fostamatinib in ITP, which was comprised of three studies, two randomized placebo-controlled studies (Studies 047 and 048) and an open-label extension study (Study 049). Together with an initial proof of concept study, the NDA included 163 ITP patients. Across all indications, fostamatinib has been evaluated in over 4,600 subjects.  Data from all studies, including preclinical evaluation and drug manufacturing data, were included in the NDA submission. In patients with ITP, the immune system attacks and destroys the body's own blood platelets, which play an active role in blood clotting and healing.  Common symptoms of ITP are excessive bruising and bleeding.  People suffering with chronic ITP may live with increased risk of severe bleeding events that can result in serious medical complication, or even death.  Current therapies for ITP include steroids, blood platelet production boosters (TPO-RAs) and splenectomy. However, not all patients are adequately treated with existing therapies. As a result, there remains a significant medical need for additional treatment options for patients with ITP. TAVALISSE™ is an oral investigational drug candidate designed to inhibit SYK kinase, a key signaling member in the immune process that leads to platelet destruction in ITP. Unlike other therapies that modulate the immune system in different ways or stimulate platelet production, fostamatinib may address an underlying autoimmune cause of ITP by impeding platelet destruction. (www.rigel.com)  Rigel Pharmaceuticals, Inc. is a biotechnology company dedicated to discovering, developing and providing novel small molecule drugs that significantly improve the lives of patients with immune and hematological disorders, cancer and rare diseases.  Rigel's pioneering research focuses on signaling pathways that are critical to disease mechanisms. The company's current clinical programs include clinical trials of fostamatinib, an oral spleen tyrosine kinase (SYK) inhibitor, in a number of indications. Rigel has submitted an NDA to the FDA for fostamatinib in patients with chronic or persistent immune thrombocytopenia (ITP). In addition, Rigel has product candidates in development with partners BerGenBio AS, Daiichi Sankyo and Aclaris Therapeutics. This release contains forward-looking statements relating to, among other things, the timing of a response from the FDA to our NDA submission.  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 "will," "may," "expect," and similar expressions are intended to identify these forward-looking statements. These forward-looking statements are based on Rigel's current expectations and inherently involve significant risks and uncertainties. Actual results and the timing of events could differ materially from those anticipated in such forward looking statements as a result of these risks and uncertainties, which include, without limitation, the FDA may interpret Rigel's findings differently, which could result in the FDA not approving any submitted NDA; the availability of resources to develop Rigel's product candidates; Rigel's need for additional capital in the future to sufficiently fund Rigel's operations and research; as well as other risks detailed from time to time in Rigel's reports filed with the Securities and Exchange Commission, including its Quarterly Report on Form 10-Q for the period ended March 31, 2017. Rigel does not undertake any obligation to update forward-looking statements and expressly disclaims any obligation or undertaking to release publicly any updates or revisions to any forward-looking statements contained herein. To view the original version on PR Newswire, visit:http://www.prnewswire.com/news-releases/rigel-announces-oral-presentation-of-tavalisse-fostamatinib-disodium-phase-3-clinical-data-at-the-european-hematology-association-22nd-annual-congress-300478623.html


The NDA submission is supported by data from the Phase 3 clinical program for fostamatinib in ITP, which was comprised of three studies, two randomized placebo-controlled studies (Studies 047 and 048), and an open-label extension study (Study 049). Together with an initial proof of concept study, the NDA included 163 ITP patients. Across all indications, fostamatinib has been evaluated in over 4,600 subjects.  Data from all studies, including preclinical evaluation and drug manufacturing data, were included in the NDA submission. In patients with ITP, the immune system attacks and destroys the body's own blood platelets, which play an active role in blood clotting and healing.  Common symptoms of ITP are excessive bruising and bleeding.  People suffering with chronic ITP may live with increased risk of severe bleeding events that can result in serious medical complication, or even death.  Currently approved therapies for ITP include steroids, blood platelet production boosters (TPO-RAs) and splenectomy. However, not all patients derive a benefit from existing therapies. As a result, there remains a significant medical need for additional treatment options for patients with ITP. TAVALISSE™ is an oral investigational drug candidate designed to inhibit SYK kinase, a key signaling member in the immune process that leads to platelet destruction in ITP.  Unlike other therapies that modulate the immune system in different ways or stimulate platelet production, fostamatinib may address an underlying autoimmune cause of ITP by impeding platelet destruction. (www.rigel.com)  Rigel Pharmaceuticals, Inc. is a biotechnology company dedicated to discovering, developing and providing novel small molecule drugs that significantly improve the lives of patients with immune and hematological disorders, cancer and rare diseases.  Rigel's pioneering research focuses on signaling pathways that are critical to disease mechanisms. The company's current clinical programs include clinical trials of fostamatinib, an oral spleen tyrosine kinase (SYK) inhibitor, in a number of indications. Rigel has submitted an NDA to the FDA for fostamatinib in patients with chronic or persistent immune thrombocytopenia (ITP). In addition, Rigel has product candidates in development with partners BerGenBio AS, Daiichi Sankyo and Aclaris Therapeutics. This release contains forward-looking statements relating to, among other things, the timing of a response from the FDA to our NDA submission and Rigel's belief that fostamatinib may be an attractive alternative for patients with ITP.  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 "if," "planned," "will," "may," "expect," and similar expressions are intended to identify these forward-looking statements. These forward-looking statements are based on Rigel's current expectations and inherently involve significant risks and uncertainties. Actual results and the timing of events could differ materially from those anticipated in such forward looking statements as a result of these risks and uncertainties, which include, without limitation, the FDA may interpret Rigel's findings differently, which could result in the FDA not approving any submitted NDA; the availability of resources to develop Rigel's product candidates; Rigel's need for additional capital in the future to sufficiently fund Rigel's operations and research; the uncertain timing of completion of and the success of clinical studies; market competition, risks associated with and Rigel's dependence on Rigel's corporate partnerships; risks related to changes in estimated cash position based on the completion of financial closing procedures and the audit of Rigel's financial statements; as well as other risks detailed from time to time in Rigel's reports filed with the Securities and Exchange Commission, including its Quarterly Report on Form 10-Q for the quarter ended March 31, 2017. Rigel does not undertake any obligation to update forward-looking statements and expressly disclaims any obligation or undertaking to release publicly any updates or revisions to any forward-looking statements contained herein. To view the original version on PR Newswire, visit:http://www.prnewswire.com/news-releases/fda-accepts-rigels-new-drug-application-for-tavalisse-fostamatinib-disodium-for-the-treatment-of-chronic-itp-300475653.html


Genovese M.C.,Stanford University | Kavanaugh A.,University of California at San Diego | Weinblatt M.E.,Harvard University | Peterfy C.,Spire science | And 5 more authors.
Arthritis and Rheumatism | Year: 2011

Objective To assess the efficacy and safety of R788 (fostamatinib disodium), an inhibitor of spleen tyrosine kinase (Syk), in patients with active rheumatoid arthritis (RA) that did not respond to biologic therapies. Methods. A total of 219 patients with active RA in whom treatment with biologic agents had failed were enrolled in a 3-month multicenter, randomized, double-blind, placebo-controlled trial of R788. The primary end point was the percentage of patients who met the American College of Rheumatology 20% improvement criteria (achieved an ACR20 response) at month 3. Secondary end points included changes in inflammation and damage, as assessed by magnetic resonance imaging (MRI), and changes in the Disease Activity Score. Results. The ACR20 response in the R788 100 mg twice daily group was 38%, versus 37% in the placebo group, at month 3. No significant differences were achieved in the ACR20, ACR50, or ACR70 response levels at 3 months. There were differences between the groups from baseline to month 3 in the secondary end points C-reactive protein (CRP) level and synovitis score on MRI. There were baseline differences in steroid use, prior biologic use, and synovitis score on MRI between the R788 group and the placebo group that may have affected the outcomes. A high placebo response rate was seen in this trial, and exploratory analysis suggested that this may in part have been driven by patients who entered the trial with an elevated erythrocyte sedimentation rate but normal CRP level. Conclusion. Our findings indicate that there were no differences in the primary end point between the R788 and placebo groups. Differences were observed between the R788 and placebo groups in secondary end points, particularly in those patients who entered the study with an elevated CRP level. © 2011 by the American College of Rheumatology.


Duncton M.A.J.,Evotec | Duncton M.A.J.,Rigel Inc
MedChemComm | Year: 2011

The addition of a radical to a heteroaromatic base is commonly referred to as a Minsici reaction. Such reactions constitute a broad-set of selective CH-functionalization processes. This review describes some of the major applications of Minisci reactions and related processes to medicinal or biological chemistry, and highlights some potential developments within this area. © 2011 The Royal Society of Chemistry.


trans-2-(Trifluoromethyl)cyclopropylboronic acid N-methyliminodiacetic acid (MIDA) ester 5 was synthesized as a pure diastereomer from vinylboronic acid MIDA ester and (trifluoromethyl)diazomethane in a single step. An X-ray study confirmed the trans-stereochemistry around the cyclopropyl ring. Use of 5 in Suzuki reactions, with a variety of aryl or heteroaryl coupling partners, provided trans-2-(trifluoromethyl)cyclopropyl products in moderate to excellent yields (17-90%). © 2013 American Chemical Society.


Weinblatt M.E.,Harvard University | Kavanaugh A.,University of California at San Diego | Genovese M.C.,Stanford University | Musser T.K.,Rigel Inc | And 2 more authors.
New England Journal of Medicine | Year: 2010

BACKGROUND: Spleen tyrosine kinase (Syk) is an important modulator of immune signaling. The objective of this phase 2 study was to evaluate the efficacy and safety of R788, an oral inhibitor of Syk, in patients with active rheumatoid arthritis despite methotrexate therapy. METHODS: We enrolled 457 patients who had active rheumatoid arthritis despite long-term methotrexate therapy in a 6-month, double-blind, placebo-controlled trial. The primary outcome was the American College of Rheumatology (ACR) 20 response (which indicates at least a 20% reduction in the number of both tender and swollen joints and improvement in at least three of five other criteria) at month 6. RESULTS: R788, at a dose of 100 mg twice daily and at a dose of 150 mg once daily, was significantly superior to placebo at month 6 (ACR 20 response rates of 67% and 57%, respectively, vs. 35%; P<0.001 for the comparison of both doses with placebo). It was also significantly superior with respect to ACR 50, which indicates at least a 50% improvement (43% and 32% vs. 19%; P<0.001 for the comparison of the 100-mg dose with placebo, P = 0.007 for the comparison of the 150-mg dose with placebo) and ACR 70 (28% and 14% vs. 10%; P<0.001 for the comparison of the 100-mg dose with placebo, P = 0.34 for the comparison of the 150-mg dose with placebo). A clinically significant effect was noted by the end of the first week of treatment. Adverse effects included diarrhea (in 19% of subjects taking the 100-mg dose of R788 vs. 3% of those taking placebo), upper respiratory infections (14% vs. 7%), and neutropenia (6% vs. 1%). R788 was associated with an increase in systolic blood pressure of approximately 3 mm Hg between baseline and month 1, as compared with a decrease of 2 mm Hg with placebo; 23% of the patients taking R788 vs. 7% of the patients receiving placebo required the initiation of or a change in antihypertensive therapy. CONCLUSIONS: In this phase 2 study, a Syk inhibitor reduced disease activity in patients with rheumatoid arthritis; adverse events included diarrhea, hypertension, and neutropenia. Additional studies will be needed to further assess the safety and efficacy of Syk-inhibition therapy in patients with rheumatoid arthritis. Copyright © 2010 Massachusetts Medical Society. All rights reserved.


This invention is directed to compounds of formula (I): where n, m, Y, R^(1), R^(2), R^(3), R^(4 )and R^(5 )are disclosed herein, as isolated stereoisomers or mixtures thereof, or pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising the compounds of formula (I); and methods of using the compounds and the pharmaceutical compositions in treating diseases or conditions associated with JAK2 activity.


News Article | November 1, 2016
Site: www.prnewswire.com

SOUTH SAN FRANCISCO, Calif., Nov. 1, 2016 /PRNewswire/ -- Rigel Pharmaceuticals, Inc. (Nasdaq:RIGL) today reported financial results for the third quarter and nine months ended September 30, 2016. During the third quarter of 2016, Rigel accomplished a number of noteworthy milestones, m...


News Article | November 10, 2016
Site: www.prnewswire.com

SOUTH SAN FRANCISCO, Calif., Nov. 10, 2016 /PRNewswire/ -- Rigel Pharmaceuticals, Inc. (Nasdaq: RIGL) today announced that Raul Rodriguez, the company's president and chief executive officer, is scheduled to present a company overview at the Jefferies 2016 London Healthcare Conference on...

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