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Curis, Inc
curis.com › home › pipeline › emavusertib (ca-4948)
Emavusertib (CA-4948) - Curis, Inc
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 ...
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Medchemexpress
medchemexpress.com › ca-4948-1.html
Emavusertib (CA-4948) | IRAK4 Inhibitor | MedChemExpress
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.
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NCBI
ncbi.nlm.nih.gov › pmc › articles › PMC7734642
Discovery of CA-4948, an Orally Bioavailable IRAK4 Inhibitor for Treatment of Hematologic Malignancies - PMC
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 ...
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Ascopubs
ascopubs.org › doi › 10.1200 › JCO.2022.40.16_suppl.7016
Phase 1/2a study of the IRAK4 inhibitor CA-4948 as monotherapy or in combination with azacitidine or venetoclax in patients with relapsed/refractory (R/R) acute myeloid leukemia or lyelodysplastic syndrome. | Journal of Clinical Oncology
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 ...
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Clinicaltrials
clinicaltrials.gov › study › NCT03328078
ClinicalTrials.gov
February 20, 2020 - Study record managers: refer to the Data Element Definitions if submitting registration or results information
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Selleckchem
selleckchem.com › products › ca-4948.html
Emavusertib (CA-4948) | ≥99%(HPLC) | Selleck | IRAK inhibitor
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.
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Ascopubs
ascopubs.org › doi › 10.1200 › JCO.2022.40.16_suppl.7575
Open-label, dose-escalation, and expansion trial of CA ...
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 ...
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NCBI
ncbi.nlm.nih.gov › pmc › articles › PMC10150246
Oral IRAK-4 Inhibitor CA-4948 Is Blood-Brain Barrier Penetrant and Has Single-Agent Activity against CNS Lymphoma and Melanoma Brain Metastases - PMC
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 ...
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Ashpublications
ashpublications.org › blood › article › 142 › Supplement 1 › 4497 › 500877 › Takeaim-Lymphoma-An-Open-Label-Dose-Escalation-and
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 | Blood | American Society of Hematology
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....
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OncLive
onclive.com › view › irak-4-inhibitor-ca-4948-may-enhance-immunotherapeutic-outcomes-in-melanoma-with-brain-metastases
IRAK-4 Inhibitor CA-4948 May Enhance Immunotherapeutic Outcomes in Melanoma With Brain Metastases
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.
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OncLive
onclive.com › view › ca-4948-shows-early-activity-tolerability-in-relapsed-refractory-aml-and-high-risk-mds
CA-4948 Shows Early Activity, Tolerability in Relapsed/Refractory AML and High-Risk MDS
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.
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Aacrjournals
aacrjournals.org › clincancerres › article › doi › 10.1158 › 1078-0432.CCR-22-1682 › 718809 › Oral-IRAK-4-Inhibitor-CA-4948-Is-Blood-Brain
Oral IRAK-4 Inhibitor CA-4948 Is Blood-Brain Barrier ...
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) ...
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Confex
ash.confex.com › ash › 2020 › webprogram › Paper140857.html
Paper: Safety, Pharmacokinetics and Activity of CA-4948, an IRAK4 Inhibitor, for Treatment of Patients with Relapsed or Refractory Hematologic Malignancies: Results from the Phase 1 Study
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), ...
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PubMed
pubmed.ncbi.nlm.nih.gov › 33335659
Discovery of CA-4948, an Orally Bioavailable IRAK4 Inhibitor for Treatment of Hematologic Malignancies - PubMed
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 ...
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Cancer Network
cancernetwork.com › view › ca-4948-garners-positive-early-results-in-relapsed-refractory-aml-and-mds
CA-4948 Garners Positive Early Results in Relapsed/Refractory AML and MDS
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.
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Prnewswire
prnewswire.com › news-releases › curis-announces-positive-updated-data-from-ongoing-phase-12-study-of-ca-4948-monotherapy-in-patients-with-relapsed-or-refractory-acute-myeloid-leukemia-and-myelodysplastic-syndromes-301310659.html
Curis Announces Positive Updated Data from Ongoing Phase 1/2 Study of CA-4948 Monotherapy in Patients with Relapsed or 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 ...
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Clinicaltrials
clinicaltrials.gov › study › NCT04278768
Dose Escalation/ Expansion Trial of CA-4948 as ...
February 20, 2020 - Study record managers: refer to the Data Element Definitions if submitting registration or results information