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    DRUG CLASS:

    Adenosine A2B receptor antagonist

    Related drugs:
    1m
    A Phase 2 Study to Evaluate the Triplet Combination of Pemetrexed Plus AB928 (Etrumadenant) + AB122 (Zimberelimab) in Patients With Previously Treated Advanced or Metastatic MTAP Deficient Urothelial Carcinoma (clinicaltrials.gov)
    P2, N=10, Active, not recruiting, M.D. Anderson Cancer Center | Recruiting --> Active, not recruiting | N=20 --> 10
    Enrollment closed • Enrollment change
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    MTAP (Methylthioadenosine Phosphorylase) • IL17A (Interleukin 17A)
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    pemetrexed • Yutuo (zimberelimab) • etrumadenant (AB928)
    1m
    Enhanced antitumor efficacy of combined targeting of adenosine A2B receptor and PD-1 is mediated via multiple effects on different cell populations within tumor microenvironment. (PubMed, Cancer Immunol Immunother)
    Our findings suggest that inhibition of adenosine activity by blocking the A2B receptor reduces TGFβ signaling and enhances the efficacy of ICI therapy in NSCLC.
    Journal • PD(L)-1 Biomarker • IO biomarker
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    PD-1 (Programmed cell death 1) • GZMB (Granzyme B)
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    PBF-1129
    2ms
    PBF-1129 and Nivolumab for the Treatment of Recurrent or Metastatic Non-Small Cell Lung Cancer (clinicaltrials.gov)
    P1, N=30, Recruiting, Dwight Owen | Trial completion date: Dec 2025 --> Dec 2026 | Trial primary completion date: Dec 2025 --> Dec 2026
    Trial completion date • Trial primary completion date
    |
    PD-L1 (Programmed death ligand 1) • ALK (Anaplastic lymphoma kinase)
    |
    Opdivo (nivolumab) • PBF-1129
    4ms
    ADO-5030 in Bronchoconstriction Challenge, Phase 1b (clinicaltrials.gov)
    P1, N=36, Not yet recruiting, Adovate
    New P1 trial
    4ms
    Reversing adenosine-mediated immunosuppression in triple-negative breast cancer by synergistic chemo-immunotherapy via stimuli-responsive nanomedicines. (PubMed, EBioMedicine)
    Co-delivery of an ICD inducer (EPI) and an adenosine receptor antagonist (AB928) is realised in a stimuli-responsive nanomedicine to address immunosuppression induced by adenosine, thereby enhancing ICD effects and synergistically reprogramming the immunosuppressive tumor microenvironment.
    Journal • IO biomarker
    |
    ADORA2A (Adenosine A2a Receptor)
    |
    epirubicin • etrumadenant (AB928)
    4ms
    Phase 1 dose escalation trial of the selective adenosine A2B antagonist PBF-1129 in patients with metastatic non-small cell lung cancer. (PubMed, Invest New Drugs)
    The reduction of PD-1 expression on CD4⁺ T cells and decreased myeloid-derived suppressor cells were also associated with better outcomes. These findings suggest PBF-1129 is safe and modulates the systemic immune parameters, warranting further evaluation in combination with immune checkpoint blockade.
    P1 data • Journal • PD(L)-1 Biomarker • IO biomarker
    |
    CD8 (cluster of differentiation 8) • PD-1 (Programmed cell death 1) • CD4 (CD4 Molecule)
    |
    PBF-1129
    5ms
    Safety and Efficacy of Zimberelimab (AB122) in Combination With Domvanalimab (AB154) and Etrumadenant (AB928) in Patients With Previously Treated Non-Small Cell Lung Cancer (clinicaltrials.gov)
    P2, N=30, Active, not recruiting, Washington University School of Medicine | Trial completion date: Dec 2029 --> Jun 2030 | Trial primary completion date: Oct 2025 --> Apr 2026
    Trial completion date • Trial primary completion date
    |
    PD-L1 (Programmed death ligand 1)
    |
    PD-L1 expression
    |
    PD-L1 IHC 22C3 pharmDx
    |
    Yutuo (zimberelimab) • domvanalimab (AB154) • etrumadenant (AB928)
    6ms
    Discovery of Novel Triple A1/A2A/A2B Adenosine Receptor Antagonists for Cancer Immunotherapy. (PubMed, J Med Chem)
    Compound 14a also effectively restored T cell proliferation suppressed by 5'-N-ethylcarboxamidoadenosine (NECA) and exhibited superior T cell-mediated cytotoxicity in coculture systems with A1R- and PD-L1-expressed cancer cells compared with ciforadenant (A2AR antagonist) and etrumadenant (A2AR/A2BR dual antagonist). Moreover, the combination of compound 14a with avelumab, an anti-PD-L1 antibody, resulted in enhanced infiltration of effector T cells and significantly increased the CD8+/Treg ratio in the CT26 syngeneic mouse model, substantially inhibiting tumor growth. Therefore, compound 14a is a promising candidate for multitargeted immunomodulation in cancer immunotherapy.
    Journal
    |
    CD8 (cluster of differentiation 8)
    |
    PD-L1 expression
    |
    Bavencio (avelumab) • etrumadenant (AB928) • ciforadenant (CPI-444)
    6ms
    ARC-9: An Open Label Study Evaluating the Efficacy and Safety of Etrumadenant (AB928) Based Treatment Combinations in Participants With Metastatic Colorectal Cancer. (clinicaltrials.gov)
    P1/2, N=227, Completed, Arcus Biosciences, Inc. | Active, not recruiting --> Completed | Trial completion date: Mar 2026 --> Sep 2025
    Trial completion • Trial completion date
    |
    Avastin (bevacizumab) • 5-fluorouracil • Stivarga (regorafenib) • Yutuo (zimberelimab) • leucovorin calcium • etrumadenant (AB928) • quemliclustat (AB680)
    7ms
    A Phase 2 Study to Evaluate the Triplet Combination of Pemetrexed Plus AB928 (Etrumadenant) + AB122 (Zimberelimab) in Patients With Previously Treated Advanced or Metastatic MTAP Deficient Urothelial Carcinoma (clinicaltrials.gov)
    P2, N=20, Recruiting, M.D. Anderson Cancer Center | Trial completion date: Sep 2025 --> Sep 2027 | Trial primary completion date: Sep 2025 --> Sep 2027
    Trial completion date • Trial primary completion date
    |
    MTAP (Methylthioadenosine Phosphorylase) • IL17A (Interleukin 17A)
    |
    pemetrexed • Yutuo (zimberelimab) • etrumadenant (AB928)
    7ms
    PANTHER: A Phase I-II Study to Test the Safety and Efficacy of PD1 (AB122) and Adenosine Receptor (AB928) Antagonists With Chemotherapy After Short-Course Radiation for Rectal Cancer. (clinicaltrials.gov)
    P2, N=43, Recruiting, Weill Medical College of Cornell University | Trial primary completion date: Dec 2025 --> Dec 2026
    Trial primary completion date
    |
    5-fluorouracil • Yutuo (zimberelimab) • leucovorin calcium • etrumadenant (AB928)
    7ms
    ARC-7: Study to Evaluate Monotherapy and Combination Immunotherapies in Participants With PD-L1 Positive Non-small Cell Lung Cancer (clinicaltrials.gov)
    P2, N=151, Completed, Arcus Biosciences, Inc. | Active, not recruiting --> Completed
    Trial completion
    |
    PD-L1 (Programmed death ligand 1)
    |
    PD-L1 expression • PD-L1 overexpression
    |
    Yutuo (zimberelimab) • domvanalimab (AB154) • etrumadenant (AB928)