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    DRUG CLASS:

    Adenosine A2B receptor antagonist

    Related drugs:
    1d
    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
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    CD8 (cluster of differentiation 8) • PD-1 (Programmed cell death 1) • CD4 (CD4 Molecule)
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    PBF-1129
    29d
    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
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    PD-L1 (Programmed death ligand 1)
    |
    PD-L1 expression
    |
    PD-L1 IHC 22C3 pharmDx
    |
    Yutuo (zimberelimab) • domvanalimab (AB154) • etrumadenant (AB928)
    1m
    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
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    Bavencio (avelumab) • etrumadenant (AB928) • ciforadenant (CPI-444)
    2ms
    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
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    Avastin (bevacizumab) • 5-fluorouracil • Stivarga (regorafenib) • Yutuo (zimberelimab) • leucovorin calcium • etrumadenant (AB928) • quemliclustat (AB680)
    3ms
    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)
    3ms
    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)
    3ms
    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)
    4ms
    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, Active, not recruiting, Arcus Biosciences, Inc. | Trial completion date: Aug 2025 --> Mar 2026 | Trial primary completion date: Jul 2025 --> Oct 2025
    Trial completion date • Trial primary completion date
    |
    Avastin (bevacizumab) • 5-fluorouracil • Stivarga (regorafenib) • Yutuo (zimberelimab) • leucovorin calcium • etrumadenant (AB928) • quemliclustat (AB680)
    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 primary completion date: Jul 2025 --> Oct 2025 | Trial completion date: Sep 2029 --> Dec 2029
    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)
    7ms
    A Study of Etrumadenant and Zimberelimab in People With Dedifferentiated Liposarcoma (clinicaltrials.gov)
    P2, N=16, Active, not recruiting, Memorial Sloan Kettering Cancer Center | Recruiting --> Active, not recruiting | N=25 --> 16
    Enrollment closed • Enrollment change
    |
    Yutuo (zimberelimab) • etrumadenant (AB928)
    7ms
    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: Apr 2029 --> Sep 2029 | Trial primary completion date: Jan 2025 --> Jul 2025
    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)
    8ms
    ADPORT-601: TT-10 (PORT-6) and TT-4 (PORT-7) as Single Agents and in Combination in Subjects With Advanced Selected Solid Tumors (clinicaltrials.gov)
    P1/2, N=90, Recruiting, Portage Biotech | Active, not recruiting --> Recruiting | Trial completion date: Aug 2025 --> Dec 2027 | Trial primary completion date: May 2025 --> Jun 2026
    Enrollment open • Trial completion date • Trial primary completion date
    |
    PORT-6 • PORT-7