Entospletinib Dimesylate

Syk (Spleen Tyrosine Kinase) is a crucial enzyme found in the human body that plays a significant role in immune cell signaling. It is primarily expressed in cells of the hematopoietic system, such as B cells, T cells, and mast cells. Syk acts as a key mediator in various immune responses, including B cell receptor signaling, Fc receptor signaling, and integrin signaling. By initiating downstream signaling cascades, Syk regulates immune cell activation, differentiation, and cytokine production. Due to its pivotal role in immune cell function, Syk has emerged as a potential therapeutic target for various immune-related disorders, including autoimmune diseases and certain cancers. The analysis of the current competitive landscape and future development of target Syk reveals that Rigel Pharmaceuticals, Inc., Novartis AG, HUTCHMED (China) Ltd., and TopiVert Ltd. are among the companies growing fastest under this target. These companies have made significant progress in the R&D of drugs targeting Syk, with drugs in the Approved and Phase 3 stages. Drugs targeting Syk have been approved for various indications, covering a wide range of diseases and conditions. Small molecule drugs are progressing most rapidly, indicating their potential as therapeutic options. The development of drugs targeting Syk is taking place in various countries/locations, with the United States, European Union, and China being prominent players. Further research and development are needed to fully explore the potential of drugs targeting Syk and address the inactive drugs in the pipeline. How do they work?Syk inhibitors are a type of medication that target and inhibit the activity of the spleen tyrosine kinase (Syk) enzyme. From a biomedical perspective, Syk is an enzyme involved in signaling pathways within immune cells, particularly B cells and mast cells. It plays a crucial role in the activation of these cells and the release of inflammatory mediators. Syk inhibitors work by binding to the Syk enzyme and blocking its activity. By inhibiting Syk, these medications can help regulate immune responses and reduce inflammation. They are primarily used in the treatment of certain autoimmune diseases, such as rheumatoid arthritis and immune thrombocytopenic purpura. These inhibitors are considered targeted therapies as they specifically target the Syk enzyme, minimizing potential side effects on other cellular processes. They can be administered orally or intravenously, depending on the specific medication. Syk inhibitors have shown promising results in clinical trials and are an active area of research in the field of biomedicine. List of Syk InhibitorsThe currently marketed Syk inhibitors include: Fostamatinib DisodiumMidostaurinSovleplenibIMG-016TOP-1630CerdulatinibEntospletinib DimesylateGusacitinibIC-265IC-270For more information, please click on the image below. What are Syk inhibitors used for?Syk inhibitors are primarily used in the treatment of certain autoimmune diseases, such as rheumatoid arthritis and immune thrombocytopenic purpura. For more information, please click on the image below to log in and search. How to obtain the latest development progress of Syk inhibitors?In the Synapse database, you can keep abreast of the latest research and development advances of Syk inhibitors anywhere and anytime, daily or weekly, through the "Set Alert" function. Click on the image below to embark on a brand new journey of drug discovery!

Lanraplenib is one of Kronos’ two clinical-stage assets. After a mid-stage flop, Kronos Bio is discontinuing a cancer trial for lanraplenib and seeking a partner to continue development of the SYK inhibitor—the second acute myeloid leukemia (AML) candidate to disappoint the biotech. The announcement, which was made last night after market close, sent the biotech’s stock spiraling 13%, from $1.47 per share yesterday to $1.27 as of 10:40 a.m. ET today. The pipeline update follows a review of phase 1b data from Kronos’ phase 1b/2 trial assessing lanraplenib in combo with Xospata among 24 patients with FLT3-mutated relapsed/refractory AML. The patients were split up across four groups, receiving 20 mg to 90 mg of lanraplenib in combination with 120 mg of Xospata. No complete responses (CRs) or CRs with partial hematologic recovery (CRh) were observed and several patients discontinued treatment early on, according to Kronos. The company has now chosen not to proceed with the phase 2 part of the trial but does want to continue development of lanraplenib with a partner. “Patients in our study were older, more heavily pre-treated, and frailer than the relapsed/refractory patients in earlier studies. Many patients experienced non-drug related infectious disease complications leading to discontinuation during the first two months of treatment without achieving the count recovery needed to achieve a CR or CRh,” Jorge DiMartino, M.D., Ph.D., chief medical officer and executive vice president of clinical development at Kronos, said in a Dec. 18 release. “Given the changes in the treatment landscape for relapsed/refractory FLT3-mutated AML, it would be challenging to demonstrate the clinical benefit of adding lanraplenib to gilteritinib in this population.” This summer, the FDA approved Daiichi Sankyo’s quizartinib (marketed as Vanflyta), the first FLT3 inhibitor approved across three phases of the common blood cancer. Lanraplenib is one of Kronos’ two clinical-stage assets. Attention will now turn to KB-0742, the company’s first internally discovered molecule. In November, the biotech shared positive preliminary phase 1/2 trial data for the solid tumor candidate and announced efforts to streamline operations that included a 19% workforce reduction.   Besides KB-0742, Kronos has a partnership with Roche’s Genentech for several undisclosed discovery programs. Inked in January, the Genentech partnership is crucial for Kronos, coming right after the biotech kicked a late-stage AML asset called entospletinib to the curb. The Roche unit jumped in to save the day for the struggling biotech with a $20 million upfront payment plus milestones that could top $177 million for the first program and $100 million for the first licensed product. Now, after another AML disappointment, Kronos has revealed a new development candidate, dubbed KB-9558. The preclinical asset is designed to modulate the IRF4 transcription regulatory network—a key driver in multiple myeloma. KB-9558 is Kronos’ second internally created product and is currently in IND-enabling studies, which are expected to be completed in the fourth quarter of next year. “Existing therapies for this disease, including CAR-T and bispecific antibody therapies, are not curative, and there is substantial need for new therapies,” said Norbert Bischofberger, Ph.D., Kronos Bio president and CEO. “Preclinical data indicate that treatment of multiple myeloma cells with KB-9558 leads to a rapid and potent down-regulation of IRF4, and we believe our product candidate has the potential to be an innovative treatment for patients with this incurable disease.”