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    DRUG CLASS:

    IRAK-4 degrader

    Related drugs:
    9d
    Safety, PK/PD, and Clinical Activity of KT-413 in Adult Patients with Relapsed or Refractory B-cell NHL (clinicaltrials.gov)
    P1, N=7, Completed, Kymera Therapeutics, Inc. | Suspended --> Completed | N=80 --> 7
    Trial completion • Enrollment change
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    KT-413
    22d
    Unveiling Biomarkers in Head and Neck Squamous Cell Carcinoma through Bioinformatics: The Role of SPP1 and KRT78. (PubMed, Int J Mol Sci)
    This study analyzed gene expression profiles from three datasets (GSE6791, GSE29330, and GSE58911) to identify differentially expressed genes (DEGs) in HNSCC...Remarkably, the expression levels of these hub genes correlated with tumor grade, clinical cancer stage, and poor prognosis in HNSCC. Our findings hold significant clinical potential for early diagnosis and the development of novel therapeutic targets for patients with HNSCC.
    Journal
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    SPP1 (Secreted Phosphoprotein 1)
    29d
    A Single and Multiple Ascending Dose Trial of LT-002-158 in Healthy Adult Volunteers (clinicaltrials.gov)
    P1, N=82, Recruiting, Shanghai Leadingtac Pharmaceutical Co., Ltd. | Not yet recruiting --> Recruiting
    Enrollment open
    1m
    Analysis of Human Papillomavirus-Associated Cervical Cancer Differentially Expressed Genes and Identification of Prognostic Factors using Integrated Bioinformatics Approaches. (PubMed, Adv Biomed Res)
    Two gene expression profiles of GSE9750 and GSE6791, which included cervical cancer HPV-positive and -negative samples, were evaluated using the R limma package with established cut-off criteria of P value < 0.05 and | fold change| ≥ 1...In fact, the current study has the potential to give a distinct viewpoint on the molecular pathways linked to cervical cancer. Considering the potential importance of the hub genes, we recommend conducting in-depth wet lab research to determine their impact on the biological mechanisms of cervical cancer.
    Journal
    |
    CDC45 (Cell Division Cycle 45)
    2ms
    ADVANTA: Phase 2 Study of SAR444656 in Adult Participants With Moderate to Severe Atopic Dermatitis (clinicaltrials.gov)
    P2, N=200, Recruiting, Sanofi | N=115 --> 200 | Trial completion date: Feb 2025 --> Aug 2026 | Trial primary completion date: Jan 2025 --> Jul 2026
    Enrollment change • Trial completion date • Trial primary completion date
    2ms
    ZEN: A Phase 2 Study to Evaluate the Efficacy and Safety of SAR444656 Compared With Placebo in Adult Participants With Moderate to Severe Hidradenitis Suppurativa (clinicaltrials.gov)
    P2, N=156, Recruiting, Sanofi | N=99 --> 156 | Trial completion date: Mar 2025 --> Jul 2026 | Trial primary completion date: Feb 2025 --> Jun 2026
    Enrollment change • Trial completion date • Trial primary completion date
    4ms
    Discovery of KT-474─a Potent, Selective, and Orally Bioavailable IRAK4 Degrader for the Treatment of Autoimmune Diseases. (PubMed, J Med Chem)
    This molecule successfully completed phase I studies in healthy adult volunteers and patients with atopic dermatitis or hidradenitis suppurativa. Phase II clinical trials in both of these indications have been initiated.
    Journal
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    IL1R1 (Interleukin 1 receptor, type I) • IRAK4 (Interleukin 1 Receptor Associated Kinase 4)
    6ms
    Discovery of KT-413, a Targeted Protein Degrader of IRAK4 and IMiD Substrates Targeting MYD88 Mutant Diffuse Large B-Cell Lymphoma. (PubMed, J Med Chem)
    KT-413 achieves concurrent degradation of these proteins by functioning as both a heterobifunctional degrader and a molecular glue. Based on the demonstrated activity and safety of KT-413 in preclinical studies, a phase 1 clinical trial in B-cell lymphomas, including MYD88 mutant ABC DLBCL, is currently underway.
    Journal
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    MYD88 (MYD88 Innate Immune Signal Transduction Adaptor) • IKZF1 (IKAROS Family Zinc Finger 1) • IRAK4 (Interleukin 1 Receptor Associated Kinase 4)
    |
    KT-413
    6ms
    Unveiling the role of HACE1 in cervical cancer: implications for human papillomavirus infection and prognosis. (PubMed, Transl Cancer Res)
    From The Cancer Genome Atlas Cervical Squamous Cell Carcinoma and Endocervical Adenocarcinoma (TCGA-CESC) and Gene Expression Omnibus (GEO, GSE6791) datasets, we obtained RNA-Seq profiles and associated clinical information...Our study reveals that HACE1 upregulation is associated with cervical cancer, particularly in HPV-positive patients. HACE1 emerges as an independent prognostic factor, linked to unfavorable outcomes.
    Journal
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    UBR5 (Ubiquitin Protein Ligase E3 Component N-Recognin 5)
    6ms
    A Single and Multiple Ascending Dose Trial of LT-002-158 in Healthy Adult Volunteers (clinicaltrials.gov)
    P1, N=82, Not yet recruiting, Shanghai Leadingtac Pharmaceutical Co., Ltd. | Initiation date: Jan 2024 --> Jun 2024
    Trial initiation date
    11ms
    ADVANTA: Phase 2 Study of SAR444656 in Adult Participants With Moderate to Severe Atopic Dermatitis (clinicaltrials.gov)
    P2, N=115, Recruiting, Sanofi | Trial completion date: May 2026 --> Feb 2025 | Trial primary completion date: Apr 2026 --> Jan 2025
    Trial completion date • Trial primary completion date
    11ms
    ZEN: A Phase 2 Study to Evaluate the Efficacy and Safety of SAR444656 Compared With Placebo in Adult Participants With Moderate to Severe Hidradenitis Suppurativa (clinicaltrials.gov)
    P2, N=99, Recruiting, Sanofi | Trial completion date: Sep 2026 --> Mar 2025 | Trial primary completion date: Aug 2026 --> Feb 2025
    Trial completion date • Trial primary completion date
    11ms
    ZEN: A Phase 2 Study to Evaluate the Efficacy and Safety of SAR444656 Compared With Placebo in Adult Participants With Moderate to Severe Hidradenitis Suppurativa (clinicaltrials.gov)
    P2, N=99, Recruiting, Sanofi | Trial completion date: Mar 2025 --> Sep 2026 | Trial primary completion date: Feb 2025 --> Aug 2026
    Trial completion date • Trial primary completion date
    11ms
    ADVANTA: Phase 2 Study of SAR444656 in Adult Participants With Moderate to Severe Atopic Dermatitis (clinicaltrials.gov)
    P2, N=115, Recruiting, Sanofi | Trial completion date: Feb 2025 --> May 2026 | Trial primary completion date: Jan 2025 --> Apr 2026
    Trial completion date • Trial primary completion date
    12ms
    Safety, PK/PD, and Clinical Activity of KT-413 in Adult Patients With Relapsed or Refractory B-cell NHL (clinicaltrials.gov)
    P1, N=80, Suspended, Kymera Therapeutics, Inc.
    Trial completion date • Trial primary completion date
    |
    KT-413
    1year
    ZEN: A Phase 2 Study to Evaluate the Efficacy and Safety of SAR444656 Compared With Placebo in Adult Participants With Moderate to Severe Hidradenitis Suppurativa (clinicaltrials.gov)
    P2, N=99, Recruiting, Sanofi | Not yet recruiting --> Recruiting
    Enrollment open
    1year
    ADVANTA: Phase 2 Study of SAR444656 in Adult Participants With Moderate to Severe Atopic Dermatitis (clinicaltrials.gov)
    P2, N=115, Recruiting, Sanofi | Not yet recruiting --> Recruiting
    Enrollment open
    1year
    Safety, PK/PD, and Clinical Activity of KT-413 in Adult Patients With Relapsed or Refractory B-cell NHL (clinicaltrials.gov)
    P1, N=80, Suspended, Kymera Therapeutics, Inc. | Recruiting --> Suspended
    Trial suspension
    |
    KT-413
    over1year
    PHASE 1 TRIAL OF KT-413, A DEGRADER OF IRAK4 AND IMID SUBSTRATES, IN ADULT PATIENTS WITH RELAPSED OR REFRACTORY B-CELL NON-HODGKIN’S LYMPHOMAS (ICML 2023)
    Initial clinical data with KT-413 demonstrate degradation of IRAK4 and Ikaros/Aiolos in PBMC and tumor. It is anticipated that higher doses will achieve the predicted degradation profile in tumors that may confer clinical benefit in MYD88-mutant patients. Dose escalation is ongoing, and analyses from additional patients will be presented at the meeting.
    Clinical • P1 data
    |
    MYD88 (MYD88 Innate Immune Signal Transduction Adaptor) • IKZF1 (IKAROS Family Zinc Finger 1) • IRF4 (Interferon regulatory factor 4) • IRAK4 (Interleukin 1 Receptor Associated Kinase 4)
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    MYD88 mutation • MYD88 wild-type
    |
    KT-413
    2years
    Phase 1 Study of KT-413, a Targeted Protein Degrader of IRAK4 and IMiD Substrates, in Adult Patients with Relapsed or Refractory B-Cell Non-Hodgkin Lymphoma (ASH 2022)
    Furthermore, based on new genetic classifications, co-mutations in MYD88 and CD79 (C5 and MCD subgroups) are associated with an inferior survival after standard R-CHOP. Enrollment in the Phase 1a portion of the KT413-DL-101 study is ongoing. NCT05233033.
    Clinical • P1 data • IO biomarker
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    MYD88 (MYD88 Innate Immune Signal Transduction Adaptor) • IKZF1 (IKAROS Family Zinc Finger 1) • IRF4 (Interferon regulatory factor 4) • IL1R1 (Interleukin 1 receptor, type I) • IRAK4 (Interleukin 1 Receptor Associated Kinase 4)
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    MYD88 mutation • MYD88 mutation + CD79B mutation • MYD88 wild-type
    |
    Rituxan (rituximab) • KT-413
    2years
    Precision Targeting of MYD88 Mutant DLBCL Using the Novel Combination of Irakimids and BCL2 Inhibition (ASH 2022)
    Background: Based on new genetic classifications, co-mutations in MYD88 and CD79B (C5 and MCD subgroups) are associated with an inferior survival after standard R-CHOP. Preclinical studies highlight the potential of IRAKIMiDs as a therapeutic approach for the treatment of MYD88MT DLBCL. KTX-582 demonstrates preferential activity in MYD88MT ABC-DLBCL. Single agent venetoclax demonstrated varying potency in ABC-DLBCL cell lines, irrespective of MYD88 mutational status.
    IO biomarker
    |
    BCL2 (B-cell CLL/lymphoma 2) • MYD88 (MYD88 Innate Immune Signal Transduction Adaptor) • IKZF1 (IKAROS Family Zinc Finger 1) • CD79B (CD79b Molecule) • IRAK4 (Interleukin 1 Receptor Associated Kinase 4)
    |
    MYD88 mutation • BCL2 expression • CD79B mutation • MYD88 mutation + CD79B mutation • MYD88 wild-type
    |
    Venclexta (venetoclax) • Rituxan (rituximab) • KT-413 • KTX-582