June 26, 2024 - First-in-Class Suppressor of the TLR Pathway (Oral, Small Molecule IRAK4 Kinase Inhibitor) Innate immune responses orchestrated through Toll-like receptors or certain interleukin receptors are important mediators of the body’s initial defense against foreign antigens, while their dysregulation ...

Emavusertib (CA-4948) is a selective, potent and orally active IRAK4/FLT3 inhibitor. Emavusertib has an IC50 of 57 nM for IRAK4 in a FRET kinase assay. Emavusertib shows anti-tumor activity. - Mechanism of Action & Protocol.

Small molecule potent IRAK4 inhibitors from a novel bicyclic heterocycle class were designed and synthesized based on hits identified from Aurigene’s compound library. The advanced lead compound, CA-4948, demonstrated good cellular activity in ...

7016 Background: CA-4948 is a novel oral inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4) and FLT3. IRAK4 is critical in triggering inflammation, oncogenesis, and survival of cancer cells. Genetic mutations in the splicing factors SF3B1 and U2AF1 drive overexpression of a highly ...

National Cancer Institute at the National Institutes of Health

February 20, 2020 - Study record managers: refer to the Data Element Definitions if submitting registration or results information

January 17, 2022 - CA-4948 S-Isomer is the S-Isomer of CA-4948. CA-4948 is a potent and orally bioavailable inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK... Quality confirmed by NMR & HPLC. See customer reviews, validations & product citations.

ASCO’s publications—including the Society’s flagship publication, the Journal of Clinical Oncology—serve readers as the most credible, authoritative, peer-reviewed resources for significant clinical oncology research that informs the delivery of high-quality patient care across the ...

November 28, 2023 - Disclosures. Winer:Abbvie: Consultancy; Curis Inc: Consultancy. Verma:Prelude: Research Funding; Stelexis: Current equity holder in private company, Honoraria,

An ongoing challenge in cancer is the management of primary and metastatic brain malignancies. This is partly due to restrictions of the blood-brain barrier and their unique microenvironment. These challenges are most evident in cancers such as lymphoma ...

November 28, 2023 - Christian Grommes, Han Tun, Allison ... Grzegorz S. Nowakowski; Takeaim Lymphoma: An Open-Label, Dose Escalation and Expansion Trial of Emavusertib (CA-4948) in Combination with Ibrutinib in Patients with Relapsed or Refractory Hematologic Malignancies....

May 23, 2023 - Bently Doonan, MD, discusses how CA-4948 can penetrate the blood-brain barrier and interact with the tumor microenvironment, and how this approach may open doors for patients with melanoma who have brain metastases.

January 7, 2022 - CA-4948 monotherapy was found to have preliminary activity with acceptable safety and tolerability in patients with relapsed or refractory acute myeloid leukemia or high-risk myelodysplastic syndromes, according to updated data from an ongoing phase 1/2 trial.

November 5, 2020 - IntroductionCA-4948 is a novel oral small molecule inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4). IRAK4 is part of the Myddosome signalin

May 1, 2023 - We propose interleukin-1 receptor-associated kinase-4 (IRAK-4) as a potential target across these diseases and describe the activity and mechanism of oral IRAK-4 inhibitor CA-4948.Experimental Design:. Human primary central nervous system lymphoma (PCNSL) and melanoma brain metastases (MBM) ...

December 7, 2020 - CA-4948-101 is a phase I trial dose escalation trial with a 3 + 3 design. Seven dosing cohorts were assessed including 50 and 100 mg daily (QD), and 50, 100, 200, 300, or 400 mg twice daily (BID) continuous oral monotherapy in 21-day cycles. Objectives included safety and tolerance (primary), ...

Small molecule potent IRAK4 inhibitors from a novel bicyclic heterocycle class were designed and synthesized based on hits identified from Aurigene's compound library. The advanced lead compound, CA-4948, demonstrated good cellular activity in ABC DLBCL and AML cell lines. Inhibition of TLR ...

March 11, 2024 - The updated results of an ongoing phase 1/2 study indicated that CA-4948 achieved promising responses and a tolerable safety profile in patients with relapsed/refractory acute myeloid leukemia and myelodysplastic syndromes.

June 11, 2021 - Dentzer added, "We are especially pleased with the outcomes seen to date for patients with spliceosome or FLT3 mutations. All three patients with a spliceosome mutation achieved an objective response. The FLT3 patient also achieved an objective response and, after two cycles of CA-4948, the ...

February 20, 2020 - Study record managers: refer to the Data Element Definitions if submitting registration or results information