A Phase 2, Multi-Center, Randomized, Double-Blind, Placebo-Controlled, Parallel Group Study of Two Doses of Inhaled R940343 in Patients With Mild to Moderate Allergic Asthma

The purpose of this study is to determine the safety, efficacy and tolerability of R940343 in the treatment of mild to moderate asthma.

Start Date01 Jul 2012

Sponsor / Collaborator

Rigel Pharmaceuticals, Inc.

100 Clinical Results associated with R-343

100 Translational Medicine associated with R-343

100 Patents (Medical) associated with R-343

Literatures (Medical) associated with R-343

04 Mar 2022·Expert Opinion on Investigational DrugsQ2 · MEDICINE

Investigational spleen tyrosine kinase (SYK) inhibitors for the treatment of autoimmune diseases

Q2 · MEDICINE

Review

Author: Yu, Qinghong ; Ding, Changhai ; Tang, Su’an

INTRODUCTIONAutoimmune diseases (ADs) are disorders induced by multiple inflammatory mediators, in which immune system attacks healthy tissues and triggers tissue injury. Targeted regulation of the activity of kinases that influence inflammation is one of the major therapies for ADs. Recently, investigational spleen tyrosine kinase (SYK) inhibitors have shown encouraging results in the AD therapy.AREAS COVEREDThis article provides a background on autoimmune diseases and provides an update on investigational SYK inhibitors. This literature review was conducted by searching publications about investigational SYK inhibitors in the treatment of ADs from experimental to clinical studies. The search terms used were SYK inhibitors, R406, fostamatinib (R788), P505-15 (PRT062607), entospletinib (GS-9973), R112, lanraplenib (GS-9876), cerdulatinib, R343, BAY-61-3606, GSK compound 143 (GSK143), R211, SKI-G-618, SKI-O-85, ER-27319, YM193306, RO9021 in conjunction with autoimmune disease using electronic databases including PubMed, EMBASE, MEDLINE and Google Scholar.EXPERT OPINIONSYK inhibitors are promising drugs with unique advantages and acceptable tolerability and safety for the treatment of ADs. However, the difficulties in developing highly selective SYK inhibitors and the unknown effects are challenges. Long-term and real-world data are essential to determine the risk-benefit ratio and true role of SYK inhibitors in the therapy of ADs.

01 Jul 2012·Expert Opinion on Investigational DrugsQ2 · MEDICINE

Tyrosine kinase inhibitors as potential drugs for B-cell lymphoid malignancies and autoimmune disorders

Q2 · MEDICINE

Review

Author: Robak, Ewa ; Robak, Tadeusz

INTRODUCTIONIn the last few years, several tyrosine kinase inhibitors (TKIs) have been synthesized and become available for preclinical studies and clinical trials. This article summarizes recent achievements in the mechanism of action, pharmacological properties, and clinical activity and toxicity, as well as the emerging role of TKIs in lymphoid malignancies, allergic diseases, and autoimmune disorders.AREAS COVEREDA literature review was conducted of the MEDLINE database PubMed for articles in English. Publications from 2000 through January 2012 were scrutinized. The search terms used were Bruton's tyrosine kinase (Btk) inhibitors, PCI-32765, GDC-0834, LFM-A13, AVL-101, AVL-292, spleen tyrosine kinase (Syk) inhibitors, R343, R406, R112, R788, fostamatinib, BAY-61-3606, C-61, piceatannol, Lyn, imatinib, nilotinib, bafetinib, dasatinib, GDC-0834, PP2, SU6656 in conjunction with lymphoid malignancy, NHL, CLL, autoimmune disease, allergic disease, asthma, and rheumatoid arthritis. Conference proceedings from the previous 5 years of the American Society of Hematology, European Hematology Association, American Society of Clinical Oncology, and ACR/ARHP Annual Scientific Meetings were searched manually. Additional relevant publications were obtained by reviewing the references from the chosen articles.EXPERT OPINIONThe use of TKIs, especially inhibitors of Btk, Syk, and Lyn, is a promising new strategy for targeted treatment of B-cell lymphoid malignancies, autoimmune disorders and allergic diseases. However, definitive data from ongoing and future clinical trials will aid in better defining the status of TKIs in the treatment of these disorders.

01 Oct 2009·Expert Opinion on Therapeutic PatentsQ2 · MEDICINE

A novel Syk kinase inhibitor suitable for inhalation: R-343(?) – WO-2009031011

Q2 · MEDICINE

Article

Author: Norman, Peter

The subject of this application is N(4)-[(2,2-difluoro-4H-benzo[1,4]oxazin-3-one)-6-yl]-5-fluoro-N(2)-[3-(methylaminocarbonylmethyleneoxy)phenyl]-2,4-pyrimidinediamine xinafoate salt, as well as inhalant formulations of the salt and a process for the preparation of the salt. This salt is probably R-343, a Syk kinase inhibitor being developed under license by Pfizer, an inhaled formulation of which is in Phase I development for the treatment of asthma.

100 Deals associated with R-343

R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Allergic asthma	Preclinical	US	Rigel Pharmaceuticals, Inc.	01 Jul 2012
Allergic asthma	Preclinical	CA	Rigel Pharmaceuticals, Inc.	01 Jul 2012

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01591044 (SITAR, CTgov)	Phase 2	Allergic asthma	301	R940343 2mg (R940343 2mg, 2 Puffs Bid)	ofwywnkihu(noowfxaihf) = kaqgnlfull lsbzgkruvj (dsodctgpeo, osubjdkdjf - cmfrtbvjaj) View more	-	29 Sep 2016
				Placebo (Placebo)	ofwywnkihu(noowfxaihf) = cgnjcbstlf lsbzgkruvj (dsodctgpeo, zirbvvvvoa - cbxfhxelyf) View more

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