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    DRUG CLASS:

    Adenosine A2B receptor antagonist

    Related drugs:
    1m
    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 completion date: Dec 2027 --> Dec 2030
    Trial completion date
    |
    5-fluorouracil • Yutuo (zimberelimab) • leucovorin calcium • etrumadenant (AB928)
    2ms
    ARC-6: Adenosine Receptor Antagonist Combination Therapy for Metastatic Castrate Resistant Prostate Cancer (clinicaltrials.gov)
    P1/2, N=173, Completed, Arcus Biosciences, Inc. | Active, not recruiting --> Completed
    Trial completion • Combination therapy • Metastases
    |
    docetaxel • Xtandi (enzalutamide capsule) • Yutuo (zimberelimab) • Trodelvy (sacituzumab govitecan-hziy) • etrumadenant (AB928) • quemliclustat (AB680)
    3ms
    Dual A2A/ A2B adenosine receptor antagonist M1069 counteracts immuno-suppressive mechanisms of adenosine and reduces tumor growth in vivo. (PubMed, Mol Cancer Ther)
    In vivo, M1069 decreased tumor growth as a monotherapy and enhanced anti-tumor activity of bintrafusp alfa (BA) or cisplatin in syngeneic adenosinehi/CD73hi 4T1 breast tumor model, but not in the CD73 knockout (KO) 4T1 tumor model or in adenosinelow/CD73low MC38 murine colon carcinoma model. In summary, our dual A2A/A2B AR antagonist M1069 may counteract immune-suppressive mechanisms of high concentrations of adenosine in vitro and in vivo and enhance the anti-tumor activity of other agents, including BA and cisplatin.
    Preclinical • Journal
    |
    CD73 (5'-Nucleotidase Ecto) • IL2 (Interleukin 2) • CXCL5 (Chemokine (C-X-C motif) ligand 5) • CXCL1 (Chemokine (C-X-C motif) ligand 1)
    |
    cisplatin • bintrafusp alfa (M7824) • M1069
    3ms
    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: Jul 2024 --> Oct 2024 | Trial primary completion date: Jul 2024 --> Oct 2024
    Trial completion date • Trial primary completion date • Metastases
    |
    Avastin (bevacizumab) • 5-fluorouracil • Stivarga (regorafenib) • Yutuo (zimberelimab) • leucovorin calcium • etrumadenant (AB928) • quemliclustat (AB680)
    3ms
    ARC-4: A Study to Evaluate Immunotherapy Combinations in Participants With Lung Cancer (clinicaltrials.gov)
    P1, N=77, Active, not recruiting, Arcus Biosciences, Inc. | Trial completion date: Aug 2024 --> Nov 2024 | Trial primary completion date: Aug 2024 --> Nov 2024
    Trial completion date • Trial primary completion date
    |
    EGFR (Epidermal growth factor receptor)
    |
    Keytruda (pembrolizumab) • carboplatin • pemetrexed • Yutuo (zimberelimab) • etrumadenant (AB928)
    6ms
    CURATE: TT-702 in Patients With Advanced Solid Tumours. (clinicaltrials.gov)
    P1/2, N=188, Recruiting, Cancer Research UK | N=114 --> 188 | Trial completion date: Sep 2025 --> Jun 2027 | Trial primary completion date: Sep 2025 --> Jun 2027
    Enrollment change • Trial completion date • Trial primary completion date • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor) • MSI (Microsatellite instability) • MLH1 (MutL homolog 1) • MSH6 (MutS homolog 6) • MSH2 (MutS Homolog 2)
    |
    HER-2 positive • HR positive • MSI-H/dMMR • HER-2 negative • ER negative
    |
    Nubeqa (darolutamide) • TT-702
    6ms
    SBRT-AMICO: Adenosine Signaling Modulation and Immune Checkpoint Inhibition With Hormone Sensitive Oligometastatic Prostate Cancer (clinicaltrials.gov)
    P2, N=23, Recruiting, Catherine Spina | Trial primary completion date: Apr 2024 --> Dec 2025
    Trial primary completion date • Checkpoint inhibition • Metastases
    |
    Yutuo (zimberelimab) • etrumadenant (AB928) • quemliclustat (AB680)
    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; Recruiting --> Active, not recruiting
    Combination therapy • Enrollment closed
    |
    PD-L1 (Programmed death ligand 1)
    |
    PD-L1 expression
    |
    PD-L1 IHC 22C3 pharmDx
    |
    Yutuo (zimberelimab) • domvanalimab (AB154) • etrumadenant (AB928)
    8ms
    PBF-1129 and Nivolumab for the Treatment of Recurrent or Metastatic Non-Small Cell Lung Cancer (clinicaltrials.gov)
    P1, N=30, Recruiting, Dwight Owen | Suspended --> Recruiting
    Enrollment open • Metastases
    |
    PD-L1 (Programmed death ligand 1) • ALK (Anaplastic lymphoma kinase) • STK11 (Serine/threonine kinase 11)
    |
    Opdivo (nivolumab) • PBF-1129
    8ms
    INCB106385 Alone or in Combination With Immunotherapy in Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=54, Completed, Incyte Corporation | Active, not recruiting --> Completed
    Trial completion • Combination therapy • Metastases
    |
    CD8 (cluster of differentiation 8)
    |
    Zynyz (retifanlimab-dlwr) • INCB106385
    9ms
    PBF-1129 and Nivolumab for the Treatment of Recurrent or Metastatic Non-Small Cell Lung Cancer (clinicaltrials.gov)
    P1, N=30, Suspended, Dwight Owen | Recruiting --> Suspended
    Trial suspension • Metastases
    |
    PD-L1 (Programmed death ligand 1) • ALK (Anaplastic lymphoma kinase) • STK11 (Serine/threonine kinase 11)
    |
    Opdivo (nivolumab) • PBF-1129
    9ms
    PBF-1129 in Patients With NSCLC (clinicaltrials.gov)
    P1, N=18, Active, not recruiting, Palobiofarma SL | Trial completion date: Dec 2023 --> Aug 2024 | Trial primary completion date: Oct 2023 --> May 2024
    Trial completion date • Trial primary completion date • Metastases
    |
    EGFR (Epidermal growth factor receptor) • ALK (Anaplastic lymphoma kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
    |
    ALK mutation • ROS1 mutation
    |
    PBF-1129
    9ms
    ARC-6: Adenosine Receptor Antagonist Combination Therapy for Metastatic Castrate Resistant Prostate Cancer (clinicaltrials.gov)
    P1/2, N=173, Active, not recruiting, Arcus Biosciences, Inc. | Phase classification: P1b/2 --> P1/2 | Trial completion date: Apr 2024 --> Aug 2024 | Trial primary completion date: Apr 2024 --> Aug 2024
    Phase classification • Trial completion date • Trial primary completion date • Combination therapy • Metastases
    |
    docetaxel • Xtandi (enzalutamide capsule) • Yutuo (zimberelimab) • Trodelvy (sacituzumab govitecan-hziy) • etrumadenant (AB928) • quemliclustat (AB680)
    9ms
    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. | Phase classification: P1b/2 --> P1/2 | Trial completion date: Jan 2024 --> Jul 2024 | Trial primary completion date: Jan 2024 --> Jul 2024
    Phase classification • Trial completion date • Trial primary completion date • Metastases
    |
    Avastin (bevacizumab) • 5-fluorouracil • Stivarga (regorafenib) • Yutuo (zimberelimab) • leucovorin calcium • etrumadenant (AB928) • quemliclustat (AB680)
    10ms
    A Phase 1 Study of YZJ-5053 Tablets in Participants With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=157, Recruiting, Shanghai Haiyan Pharmaceutical Technology Co., Ltd.
    New P1 trial • Metastases
    1year
    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, Active, not recruiting, Arcus Biosciences, Inc. | Trial completion date: Feb 2024 --> Feb 2025 | Trial primary completion date: Feb 2024 --> Feb 2025
    Trial completion date • Trial primary completion date • Combination therapy
    |
    PD-L1 (Programmed death ligand 1)
    |
    PD-L1 expression • PD-L1 overexpression
    |
    Yutuo (zimberelimab) • domvanalimab (AB154) • etrumadenant (AB928)
    1year
    PANTHEoN: A Study of Concurrent Chemoradiation in Combination With or Without PD1 Inhibitor AB122 Adenosine 2a Receptor / Adenosine 2b Receptor Inhibitor AB928 Therapies in Locally Advanced Head and Neck Cancers (clinicaltrials.gov)
    P1, N=0, Withdrawn, Jennifer Choe | N=24 --> 0 | Not yet recruiting --> Withdrawn
    Enrollment change • Trial withdrawal • Combination therapy • IO biomarker • Metastases
    |
    cisplatin • Yutuo (zimberelimab) • etrumadenant (AB928)
    1year
    An Open Label Study Evaluating the Efficacy and Safety of Etrumadenant (AB928) Based Treatment Combinations in Participants With Metastatic Colorectal Cancer. (clinicaltrials.gov)
    P1b/2, N=227, Active, not recruiting, Arcus Biosciences, Inc. | Trial primary completion date: Sep 2023 --> Jan 2024
    Trial primary completion date • Metastases
    |
    Avastin (bevacizumab) • 5-fluorouracil • Stivarga (regorafenib) • Yutuo (zimberelimab) • leucovorin calcium • etrumadenant (AB928) • quemliclustat (AB680)
    1year
    Phase 2 Study to evaluate the triplet combination of pemetrexed plus etrumadenant and zimberelimab in patients with previously treated advanced or MTAP-deficient metastatic urothelial carcinoma (mUC) (SITC 2023)
    Exploratory objective is to evaluate progression-free and overall survival. Interim analysis for futility and safety occurs in cohorts of 5 patients and is performed based on Bayesian sequential methods.
    Clinical • P2 data • PD(L)-1 Biomarker • IO biomarker • Metastases
    |
    CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • MTAP (Methylthioadenosine Phosphorylase) • CDKN2B (Cyclin Dependent Kinase Inhibitor 2B)
    |
    PD-L1 expression
    |
    pemetrexed • Yutuo (zimberelimab) • etrumadenant (AB928)
    over1year
    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 | Not yet recruiting --> Recruiting
    Enrollment open • Metastases
    |
    MTAP (Methylthioadenosine Phosphorylase) • IL17A (Interleukin 17A)
    |
    pemetrexed • Yutuo (zimberelimab) • etrumadenant (AB928)
    over1year
    ARC-4: A Study to Evaluate Immunotherapy Combinations in Participants With Lung Cancer (clinicaltrials.gov)
    P1, N=77, Active, not recruiting, Arcus Biosciences, Inc. | Trial completion date: Jul 2023 --> Aug 2024 | Trial primary completion date: Jul 2023 --> Aug 2024
    Trial completion date • Trial primary completion date
    |
    EGFR (Epidermal growth factor receptor)
    |
    EGFR mutation
    |
    Keytruda (pembrolizumab) • carboplatin • pemetrexed • Yutuo (zimberelimab) • etrumadenant (AB928)
    over1year
    SBRT-AMICO: Adenosine Signaling Modulation and Immune Checkpoint Inhibition With Hormone Sensitive Oligometastatic Prostate Cancer (clinicaltrials.gov)
    P2, N=23, Recruiting, Catherine Spina | Not yet recruiting --> Recruiting
    Enrollment open • Checkpoint inhibition • Metastases
    |
    Yutuo (zimberelimab) • etrumadenant (AB928) • quemliclustat (AB680)
    over1year
    Development of [Lu]Lu-LNC1003 for radioligand therapy of prostate cancer with a moderate level of PSMA expression. (PubMed, Eur J Nucl Med Mol Imaging)
    In this study, [Lu]Lu-LNC1003 was successfully synthesized with high radiochemical purity and stability. High binding affinity and PSMA targeting specificity were identified in vitro and in vivo. With greatly enhanced tumor uptake and retention, [Lu]Lu-LNC1003 has the potential to improve therapeutic efficacy using significantly lower dosages and less cycles of Lu that promises clinical translation to treat prostate cancer with various levels of PSMA expression.
    Journal
    |
    FOLH1 (Folate hydrolase 1)
    |
    FOLH1 expression
    |
    Pluvicto (lutetium Lu 177 vipivotide tetraxetan) • LNC-003
    over1year
    SBRT-AMICO: Adenosine Signaling Modulation and Immune Checkpoint Inhibition With Hormone Sensitive Oligometastatic Prostate Cancer (clinicaltrials.gov)
    P2, N=23, Not yet recruiting, Catherine Spina
    New P2 trial • Checkpoint inhibition • Metastases
    |
    Yutuo (zimberelimab) • etrumadenant (AB928) • quemliclustat (AB680)
    over1year
    INCB106385 Alone or in Combination With Immunotherapy in Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=54, Active, not recruiting, Incyte Corporation | Recruiting --> Active, not recruiting | N=230 --> 54
    Enrollment closed • Enrollment change • Combination therapy • IO biomarker • Metastases
    |
    CD8 (cluster of differentiation 8)
    |
    Zynyz (retifanlimab-dlwr) • INCB106385
    over1year
    A Study of Etrumadenant and Zimberelimab in People With Dedifferentiated Liposarcoma (clinicaltrials.gov)
    P2 | N=25 | Recruiting | Sponsor: Memorial Sloan Kettering Cancer Center
    Combination therapy • New P2 trial
    |
    Yutuo (zimberelimab) • etrumadenant (AB928)
    over1year
    Improving combination therapies: Targeting A2B adenosine receptor to modulate metabolic tumor microenvironment and immunosuppression. (PubMed, J Natl Cancer Inst)
    Data identify A2BAR as a valuable therapeutic target to modify metabolic and immune TME to reduce immunosuppression, enhance the efficacy of immunotherapies, and support clinical application of PBF-1129 in combination therapies.
    Journal • Combination therapy • PD(L)-1 Biomarker • IO biomarker
    |
    EGFR (Epidermal growth factor receptor) • IFNG (Interferon, gamma)
    |
    PBF-1129
    over1year
    PANTHEoN: A Study of Concurrent Chemoradiation in Combination With or Without PD1 Inhibitor AB122 Adenosine 2a Receptor / Adenosine 2b Receptor Inhibitor AB928 Therapies in Locally Advanced Head and Neck Cancers (clinicaltrials.gov)
    P1, N=24, Not yet recruiting, Jennifer Choe | Trial completion date: Apr 2025 --> Aug 2026 | Trial primary completion date: Apr 2024 --> Aug 2025
    Trial completion date • Trial primary completion date • Combination therapy • IO biomarker • Metastases
    |
    cisplatin • Yutuo (zimberelimab) • etrumadenant (AB928)
    over1year
    Updates on Abstract 397600: ARC-7: Randomized phase 2 study of domvanalimab + zimberelimab ± etrumadenant versus zimberelimab in first-line, metastatic, PD-L1-high non-small cell lung cancer (NSCLC) (ASCO 2023)
    No abstract available
    Clinical • P2 data • Metastases
    |
    PD-L1 (Programmed death ligand 1)
    |
    Yutuo (zimberelimab) • domvanalimab (AB154) • etrumadenant (AB928)
    over1year
    Adenosine Receptor A2B Antagonist Inhibits the Metastasis of Gastric Cancer Cells and Enhances the Efficacy of Cisplatin. (PubMed, Technol Cancer Res Treat)
    ADORA2B regulated the expression of EMT marker proteins in GC cells and affected GC cell metastasis. Antagonizing ADORA2B expression increased the efficacy of cisplatin treatment.
    Journal
    |
    CTNNB1 (Catenin (cadherin-associated protein), beta 1) • VIM (Vimentin) • CDH2 (Cadherin 2)
    |
    VIM expression
    |
    cisplatin
    almost2years
    PBF-1129 in Patients With NSCLC (clinicaltrials.gov)
    P1, N=18, Active, not recruiting, Palobiofarma SL | Recruiting --> Active, not recruiting | Trial completion date: Jun 2023 --> Dec 2023 | Trial primary completion date: Dec 2022 --> Oct 2023
    Enrollment closed • Trial completion date • Trial primary completion date • Metastases
    |
    EGFR (Epidermal growth factor receptor) • ALK (Anaplastic lymphoma kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
    |
    ALK mutation • ROS1 mutation
    |
    PBF-1129
    almost2years
    ARC-7: Randomized phase 2 study of domvanalimab + zimberelimab ± etrumadenant versus zimberelimab in first-line, metastatic, PD-L1-high non-small cell lung cancer (NSCLC). (ASCO Plenary Dec 2022)
    NCT04262856
    Clinical • P2 data
    |
    PD-L1 (Programmed death ligand 1)
    |
    PD-L1-H
    |
    Yutuo (zimberelimab) • domvanalimab (AB154) • etrumadenant (AB928)
    almost2years
    VELOCITY-Lung: A Study of Novel Treatment Combinations in Patients With Lung Cancer (clinicaltrials.gov)
    P2, N=335, Not yet recruiting, Gilead Sciences
    New P2 trial
    |
    EGFR (Epidermal growth factor receptor) • ALK (Anaplastic lymphoma kinase)
    |
    cisplatin • carboplatin • docetaxel • albumin-bound paclitaxel • pemetrexed • Yutuo (zimberelimab) • Trodelvy (sacituzumab govitecan-hziy) • domvanalimab (AB154) • etrumadenant (AB928)
    almost2years
    Study of SRF617 With AB928 (Etrumadenent) and AB122 (Zimberelimab) in Patients With Metastatic Castration Resistant Prostate Cancer (clinicaltrials.gov)
    P2, N=40, Active, not recruiting, Surface Oncology | Recruiting --> Active, not recruiting | Trial completion date: Nov 2023 --> Jul 2023 | Trial primary completion date: Nov 2023 --> May 2023
    Enrollment closed • Trial completion date • Trial primary completion date • Combination therapy • Metastases
    |
    CAST (Calpastatin)
    |
    Yutuo (zimberelimab) • etrumadenant (AB928) • perenostobart (SRF617)
    almost2years
    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, Not yet recruiting, M.D. Anderson Cancer Center | Initiation date: Sep 2022 --> Dec 2022
    Trial initiation date • Metastases
    |
    MTAP (Methylthioadenosine Phosphorylase) • IL17A (Interleukin 17A)
    |
    pemetrexed • Yutuo (zimberelimab) • etrumadenant (AB928)
    2years
    ARC-7: Study to Evaluate Monotherapy and Combination Immunotherapies in Participants With PD-L1 Positive Non-small Cell Lung Cancer (clinicaltrials.gov)
    P2, N=150, Active, not recruiting, Arcus Biosciences, Inc. | Recruiting --> Active, not recruiting | Trial completion date: Feb 2023 --> Feb 2024 | Trial primary completion date: Nov 2022 --> Feb 2024
    Enrollment closed • Trial completion date • Trial primary completion date • Combination therapy
    |
    PD-L1 (Programmed death ligand 1)
    |
    PD-L1 expression • PD-L1 overexpression
    |
    Yutuo (zimberelimab) • domvanalimab (AB154) • etrumadenant (AB928)
    2years
    INCB106385 Alone or in Combination With Immunotherapy in Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=230, Recruiting, Incyte Corporation | Trial completion date: Apr 2024 --> Dec 2023 | Trial primary completion date: Apr 2024 --> Dec 2023
    Trial completion date • Trial primary completion date • Combination therapy • IO biomarker • Metastases
    |
    CD8 (cluster of differentiation 8)
    |
    Zynyz (retifanlimab-dlwr) • INCB106385
    2years
    ATP-Dependent Induction of IDO1 Expression in Dendritic Cells Is Controlled through Non-Canonical NF-Kb Signaling Via P2Y11R and Leads to T Regulatory Cells Induction (ASH 2022)
    CD14+- derived DCs were cultured with ATP in presence or absence of P2X7R and P2Y11R antagonists (AZ 10606120 dihydrochloride and NF 340, respectively) and inflammasome inhibitors (Bay 11-7082 and Ac-YVAD-cmk), and then used for flow cytometry, western blot or real-time PCR analyses to evaluate DC phenotype, in particular CD73, CD39 and IDO1 expression, or release of IL-1beta as response pattern of activated inflammasome... Our data suggest that different mechanisms operate in tumor microenvironment. 1. ATP-dependent IDO1 upregulation in DCs which is induced through non-canonical NF-kB signaling by P2Y11 activation while ATP-dependent inflammasome activation via P2X7R is not involved in IDO1 regulation.
    IO biomarker
    |
    IDO1 (Indoleamine 2,3-dioxygenase 1) • CD14 (CD14 Molecule) • ENTPD1 (Ectonucleoside Triphosphate Diphosphohydrolase 1) • IL1B (Interleukin 1, beta)
    |
    IDO1 expression • CD73 expression • ENTPD1 expression
    |
    Bay11-7082
    2years
    ARC-4: A Study to Evaluate Immunotherapy Combinations in Participants With Lung Cancer (clinicaltrials.gov)
    P1, N=77, Active, not recruiting, Arcus Biosciences, Inc. | Trial completion date: Oct 2022 --> Jul 2023 | Trial primary completion date: Aug 2022 --> Jul 2023
    Trial completion date • Trial primary completion date
    |
    EGFR (Epidermal growth factor receptor)
    |
    EGFR mutation
    |
    Keytruda (pembrolizumab) • carboplatin • pemetrexed • Yutuo (zimberelimab) • etrumadenant (AB928)
    2years
    PBF-1129 and Nivolumab for the Treatment of Recurrent or Metastatic Non-Small Cell Lung Cancer (clinicaltrials.gov)
    P1, N=30, Recruiting, Dwight Owen | Not yet recruiting --> Recruiting
    Enrollment open • Metastases
    |
    PD-L1 (Programmed death ligand 1) • ALK (Anaplastic lymphoma kinase)
    |
    Opdivo (nivolumab) • PBF-1129