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    DRUG CLASS:

    AHR inhibitor

    Related drugs:
    Associations

    News

    Trials
    11d
    Baseline AHR expression shapes immune response to pharmacological modulation in PBMCs from pancreatic cancer patients. (PubMed, Front Immunol)
    Peripheral blood mononuclear cells (PBMCs) from patients with PDAC and healthy donors were isolated and treated ex vivo with two AHR agonists (Carbidopa and Tapinarof) and one antagonist (BAY 2416964). Baseline AHR expression critically shapes the immune response to pharmacological modulation in PBMCs from PDAC patients. These findings suggest that AHR profiling may serve as a clinically relevant biomarker for stratifying patients and guiding personalized immunotherapy approaches for PDAC.
    Journal • PD(L)-1 Biomarker • IO biomarker
    |
    PD-L1 (Programmed death ligand 1) • PD-1 (Programmed cell death 1) • IL10 (Interleukin 10) • AHR (Aryl hydrocarbon receptor)
    |
    carbidopa • ilantimod (BAY 2416964)
    10ms
    A Study to Learn How Safe the Study Drug BAY 2416964 (AhR Inhibitor) in Combination With the Treatment Pembrolizumab is, How This Combination Affects the Body, the Maximum Amount That Can be Given, How it Moves Into, Through and Out of the Body and Its Action Against Advanced Solid Cancers in Adults (clinicaltrials.gov)
    P1, N=47, Terminated, Bayer | Trial completion date: Dec 2025 --> Jan 2025 | Active, not recruiting --> Terminated; Last patient ongoing on treatment ended the study on 20th January 2025. Hence, the end of study was reached as defined in the protocol.
    Trial completion date • Trial termination
    |
    Keytruda (pembrolizumab) • ilantimod (BAY 2416964)
    1year
    A Study to Learn How Safe the Study Drug BAY 2416964 (AhR Inhibitor) in Combination With the Treatment Pembrolizumab is, How This Combination Affects the Body, the Maximum Amount That Can be Given, How it Moves Into, Through and Out of the Body and Its Action Against Advanced Solid Cancers in Adults (clinicaltrials.gov)
    P1, N=47, Active, not recruiting, Bayer | Trial completion date: Mar 2025 --> Dec 2025 | Trial primary completion date: Mar 2025 --> Jun 2024
    Trial completion date • Trial primary completion date • Combination therapy • Metastases
    |
    Keytruda (pembrolizumab) • ilantimod (BAY 2416964)
    1year
    Long-term exposure to BAY2416964 reduces proliferation, migration and recapitulates transcriptional changes induced by AHR loss in PyMT-induced mammary tumor cells. (PubMed, Front Oncol)
    No differentially expressed genes (DEGs) were identified in wildtype cells exposed to 1 μM BAY2416964 for 24 h; however, 46.4% of DEGs overlapped between AhrKO and LT-BAY cells including gene regulated cell proliferation. Our data reveal long-term pharmacological inhibition of AHR by BAY2416964 closely resembles AHR loss in a mouse model of breast cancer.
    Journal • Tumor cell
    |
    CYP1A1 (Cytochrome P450 Family 1 Subfamily A Member 1) • CYP1B1 (Cytochrome P450 Family 1 Subfamily B Member 1)
    |
    ilantimod (BAY 2416964)
    almost2years
    Oral AHR Antagonist in Combination With Nivolumab in Patients With PD-1 Resistant Metastatic or Recurrent Head and Neck Cancer (clinicaltrials.gov)
    P1, N=0, Withdrawn, Ikena Oncology | Phase classification: P1b --> P1 | N=54 --> 0 | Trial completion date: Jul 2025 --> Apr 2023 | Not yet recruiting --> Withdrawn | Trial primary completion date: Jul 2024 --> Apr 2023
    Phase classification • Enrollment change • Trial completion date • Trial withdrawal • Trial primary completion date • Combination therapy • Metastases
    |
    PD-L1 (Programmed death ligand 1)
    |
    PD-L1 expression
    |
    Opdivo (nivolumab) • IK-175
    almost2years
    A Study to Learn How Safe the Study Drug BAY 2416964 (AhR Inhibitor) in Combination With the Treatment Pembrolizumab is, How This Combination Affects the Body, the Maximum Amount That Can be Given, How it Moves Into, Through and Out of the Body and Its Action Against Advanced Solid Cancers in Adults (clinicaltrials.gov)
    P1, N=47, Active, not recruiting, Bayer | Trial completion date: Dec 2025 --> Mar 2025 | Trial primary completion date: Dec 2025 --> Mar 2025
    Trial completion date • Trial primary completion date • Combination therapy • Metastases
    |
    Keytruda (pembrolizumab) • ilantimod (BAY 2416964)
    almost2years
    A First-in-Humans Dose Finding Study for an Aryl Hydrocarbon Receptor Inhibitor (AhRi) in Patients With Advanced Cancer (clinicaltrials.gov)
    P1, N=78, Completed, Bayer | Active, not recruiting --> Completed
    Trial completion • Metastases
    |
    ilantimod (BAY 2416964)
    almost2years
    A Study to Learn How Safe the Study Drug BAY 2416964 (AhR Inhibitor) in Combination With the Treatment Pembrolizumab is, How This Combination Affects the Body, the Maximum Amount That Can be Given, How it Moves Into, Through and Out of the Body and Its Action Against Advanced Solid Cancers in Adults (clinicaltrials.gov)
    P1, N=47, Active, not recruiting, Bayer | Recruiting --> Active, not recruiting | N=164 --> 47
    Enrollment closed • Enrollment change • Combination therapy • Metastases
    |
    Keytruda (pembrolizumab) • ilantimod (BAY 2416964)
    almost2years
    The Garlic Compound, Diallyl Trisulfide, Attenuates Benzo[a]Pyrene-Induced Precancerous Effect through Its Antioxidant Effect, AhR Inhibition, and Increased DNA Repair in Human Breast Epithelial Cells. (PubMed, Nutrients)
    At the same time, it increased DNA POLβ protein expression, which indicates increased DNA repair, thus causing a chemopreventive effect. These results provide evidence for the chemopreventive effects of DATS in breast cancer prevention.
    Journal
    |
    AHR (Aryl hydrocarbon receptor) • CYP1A1 (Cytochrome P450 Family 1 Subfamily A Member 1)
    |
    HIF1A expression • AHR expression
    almost2years
    A First-in-Humans Dose Finding Study for an Aryl Hydrocarbon Receptor Inhibitor (AhRi) in Patients With Advanced Cancer (clinicaltrials.gov)
    P1, N=78, Active, not recruiting, Bayer | Trial completion date: Apr 2025 --> Jan 2024
    Trial completion date • Metastases
    |
    ilantimod (BAY 2416964)
    2years
    Targeting the aryl hydrocarbon receptor (AhR) with BAY 2416964: a selective small molecule inhibitor for cancer immunotherapy. (PubMed, J Immunother Cancer)
    These findings identify AhR inhibition as a novel therapeutic approach to overcome immune resistance in various types of cancers.
    Journal • IO biomarker
    |
    AHR (Aryl hydrocarbon receptor) • TDO2 (Tryptophan 2,3-Dioxygenase)
    |
    AHR expression
    |
    ilantimod (BAY 2416964)
    2years
    A Study to Learn How Safe the Study Drug BAY 2416964 (AhR Inhibitor) in Combination With the Treatment Pembrolizumab is, How This Combination Affects the Body, the Maximum Amount That Can be Given, How it Moves Into, Through and Out of the Body and Its Action Against Advanced Solid Cancers in Adults (clinicaltrials.gov)
    P1, N=164, Recruiting, Bayer | Phase classification: P1b --> P1
    Phase classification • Combination therapy • Metastases
    |
    Keytruda (pembrolizumab) • ilantimod (BAY 2416964)