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    DRUG CLASS:

    IRAK-4 inhibitor

    Related drugs:
    17d
    A Study of AZD2962, an IRAK4 Inhibitor (IRAK4 [a Body Protein] Blocker), in Participants With Haematologic Neoplasms (Blood Cancers) (clinicaltrials.gov)
    P1, N=72, Recruiting, AstraZeneca | Not yet recruiting --> Recruiting | Phase classification: P1/2 --> P1 | Initiation date: Jul 2025 --> Nov 2025
    Enrollment open • Phase classification • Trial initiation date
    2ms
    A Randomised, Double-Blind, Placebo-Controlled, First-in-Human Study of the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Single and Multiple Ascending Doses of ZE46 0134 in Healthy Volunteers (ACTRN12623000871640)
    P1, N=104, Completed, Lomond Therapeutics AU Pty Ltd | Recruiting --> Completed
    Trial completion • First-in-human
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    itraconazole
    2ms
    Disruption of fibroblast MYD88 signaling promotes antitumor immunity in pancreatic ductal adenocarcinoma. (PubMed, Cell Rep)
    Using an innovative collagen gel implantation model, we demonstrate that loss of MYD88 in CAFs enhances T cell infiltration and suppresses tumor growth. Combining MYD88 inhibition with immune checkpoint blockade significantly reduces tumor size and enhances antitumor immune responses, underscoring its potential as a therapeutic target in PDAC.
    Journal
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    MYD88 (MYD88 Innate Immune Signal Transduction Adaptor)
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    emavusertib (CA-4948)
    3ms
    Generation of a potent & selective series of IRAK4 inhibitors based on a structure based, hybridization approach. (PubMed, Bioorg Med Chem)
    In this article, we describe the development of a highly potent and selective IRAK4 lead compound 5e, starting from Astellas AS2444697 (1a). The work includes identification of the pyrazole-pyridine substituent in compound 1g, binding towards the gatekeeper region of IRAK4, followed by a structure-guided scaffold hybridization that led to 5a. Subsequent optimization of substituents of the indazole scaffold yielded 5e, which exhibits a 10-fold improvement in IRAK4 cell potency and higher off-target selectivity compared to AS244697 (1a).
    Journal
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    IRAK4 (Interleukin 1 Receptor Associated Kinase 4)
    3ms
    HPB-092 for the Treatment of Relapsed and Refractory Acute Myeloid Leukemia (clinicaltrials.gov)
    P1, N=60, Not yet recruiting, Hangzhou Polymed Biopharmaceuticals, Inc.
    New P1 trial • IO biomarker
    |
    HPB-092
    4ms
    CA-4948 in Combination With Cisplatin, Gemcitabine, and Durvalumab in Patients With Untreated Advanced or Metastatic Biliary Tract Cancer (clinicaltrials.gov)
    P1, N=48, Not yet recruiting, Washington University School of Medicine
    New P1 trial
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    cisplatin • Imfinzi (durvalumab) • gemcitabine • emavusertib (CA-4948)
    4ms
    Pharmacokinetic Study of MY004567 Tablets in Patients with Moderate to Severe Active Rheumatoid Arthritis (ChiCTR2500103914)
    P1, N=10, Recruiting, The First Hospital of Jilin University; The First Hospital of Jilin University
    New P1 trial
    |
    CRP (C-reactive protein)
    4ms
    PRESTO: A Study to Investigate the Effect of AZD6793 in Participants With Moderate to Very Severe Chronic Obstructive Pulmonary Disease (clinicaltrials.gov)
    P2, N=1160, Recruiting, AstraZeneca
    New P2 trial
    4ms
    CTN-03208-1: Study of Single and Multiple Ascending Doses of ZE46-0134 in Healthy Volunteers (clinicaltrials.gov)
    P1, N=112, Active, not recruiting, Eilean Therapeutics | N=64 --> 112 | Recruiting --> Active, not recruiting | Trial completion date: Nov 2024 --> Oct 2025 | Trial primary completion date: Oct 2024 --> Jun 2025
    Enrollment closed • Enrollment change • Trial completion date • Trial primary completion date
    |
    itraconazole
    4ms
    Dose Escalation and Expansion Study to Evaluate the Safety, PK, PD and Efficacy of ZE46-0134 in Adults With FLT3 Mutated Relapsed or Refractory Acute Myeloid Leukemia (clinicaltrials.gov)
    P1, N=60, Recruiting, Eilean Therapeutics | Not yet recruiting --> Recruiting | Trial primary completion date: Sep 2025 --> Jan 2026
    Enrollment open • Trial primary completion date
    5ms
    A Study of AZD2962, an IRAK4 Inhibitor (IRAK4 [a Body Protein] Blocker), in Participants With Haematologic Neoplasms (Blood Cancers) (clinicaltrials.gov)
    P1/2, N=72, Not yet recruiting, AstraZeneca
    New P1/2 trial
    5ms
    Meeting Report From the 2024 Symposium on IRAK4 in Cancer: Highlights and Clinical Updates. (PubMed, Clin Lymphoma Myeloma Leuk)
    Clinical data from the targeted small-molecule IRAK4 inhibitor emavusertib (CA-4948) were presented, including data from the TakeAim Leukemia and TakeAim Lymphoma trials of emavusertib in myeloid and lymphoid malignancies, respectively, and preliminary data from trials of emavusertib in multiple solid tumors. The meeting closed with expert discussion of the emerging profile of IRAK4 inhibition in cancers and the potential for IRAK4 inhibition to improve outcomes across both solid and liquid tumors.
    Review • Journal
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    IRAK4 (Interleukin 1 Receptor Associated Kinase 4)
    |
    emavusertib (CA-4948)