AB928 is a potent and selective dual antagonist of the adenosine receptors known as A2aR and A2bR. Adenosine is a powerful immunosuppressive substance produced inside tumors as a result of rapid cancer cell turnover and, in some cases, in connection with certain anti-tumor interventions, such as chemotherapy and radiation.

The A2aR and A2bR receptors are expressed on the surface of immune cells (such as T cells, NK cells, dendritic cells and macrophages) and mediate the immunosuppressive effects of adenosine. AB928, a small-molecule drug that will be administered to patients orally, is the only drug currently in development that is able to block both of these adenosine receptors. AB928 is currently being evaluated in a Phase 1/1b program in combination with our anti-PD-1 antibody (AB122) and with chemotherapy.

AB928 Clinical Trials Currently Enrolling

Trial Summary

A Phase 1/1b, open-label, dose-escalation, and dose-expansion study to evaluate the safety, tolerability, pharmacokinetic (PK), pharmacodynamic (PD), and clinical activity of AB928 in combination with mFOLFOX in participants with advanced metastatic gastroesophageal Cancer (GEC) or colorectal cancer (CRC)

Trial Identifier

Trial Summary

A Phase 1/1b, open-label, dose-escalation, and dose-expansion study to evaluate the safety, tolerability, pharmacokinetic, pharmacodynamic, and clinical activity of AB928 in combination with pegylated liposomal doxorubicin (PLD) in participants with advanced metastatic triple-negative breast cancer or ovarian cancer

Trial Identifier

Trial Summary

A Phase 1, open-label, dose-escalation study to evaluate the safety, tolerability, PK, PD and clinical activity of AB928 in combination with AB122 in participants with advanced malignancies

Trial Identifier

For questions about our clinical trials, please contact ClinicalTrialInquiry@arcusbio.com.

Publications and Abstracts

November 29, 2018

The Dual A2aR/A2bR Antagonist AB928 Reverses Adenosine-Mediated Immune Suppression and Inhibits Tumor Growth in vivo. DiRenzo D, Piovesan D, Narasappa N, Lim WH, Ashok D, Park A, Jeffrey JL, Leleti MR, Tan JBL, Seitz L, Young SW, Powers JP, Walters MJ. American Association for Cancer Research; Tumor Immunology and Immunotherapy, Miami Beach, FL.; poster No. A10.

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November 7—November 11, 2018

Development of biomarkers to assess adenosine generation & activity in support of clinical trials conducted with the adenosine receptor antagonist AB928. DiRenzo D, Ashok D, Anderson AE, Udyavar A, Tan JBL, Zhang K, Jeffrey JL, Seitz L, Leleti MR, Young SW, Powers JP, Walters MJ. Society for Immunotherapy of Cancer Annual Meeting, Washington, D.C.; poster No. P35; abstract No. 10513.

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November 7—November 11, 2018

Selection of optimized drug candidates, dosing regimen, pharmacodynamic endpoints, tumor types, and biomarkers for translating inhibition of the adenosine pathway into effective anti-tumor activity. Jaen J, Powers J, Schindler U, Seitz L, Tan J, Walters M, and Young S. Society for Immunotherapy of Cancer Annual Meeting, Washington, D.C.;poster No. P668; abstract No. 10724.

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November 7—November 11, 2018

A phase 1/1b study to evaluate the safety and tolerability of AB928, a novel dual adenosine receptor antagonist, in combination with chemotherapy in patients with breast or gynecologic malignancies. De Souza, Lee CK, Sjoquist K, Pan S, Idan A, Rieger A, Berry W, Jin L, Seitz L, Ashok D, Walters MJ, Piovesan D, Tan JBL, Lee SJ, Park A, DiRenzo D, Karakunnel J. Society for Immunotherapy of Cancer Annual Meeting, Washington, D.C.; poster No. P320; abstract No. 10688.

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November 7—November 11, 2018

A phase 1/1b study to evaluate the safety and tolerability of AB928, a novel dual adenosine receptor antagonist, in combination with chemotherapy in patients with gastrointestinal malignancies. De Souza, Lee CK, Sjoquist K, Pan S, Idan A, Rieger A, Berry W, Jin L, Seitz L, Ashok D, Walters MJ, Piovesan D, Tan JBL, Lee SJ, Park A, DiRenzo D, Karakunnel J. Society for Immunotherapy of Cancer Annual Meeting, Washington, D.C.; poster No. P321; abstract no. 10700.

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November 7—November 11, 2018

A phase 1/1b study to evaluate the safety and tolerability of AB928, a novel dual adenosine receptor antagonist, in combination with carboplatin/pemetrexed and pembrolizumab in lung cancer patients. De Souza, Lee CK, Sjoquist K, Pan S, Idan A, Rieger A, Berry W, Jin L, Seitz L, Ashok D, Walters MJ, Piovesan D, Tan JBL, Lee SJ, Park A, DiRenzo D, Karakunnel J. Society for Immunotherapy of Cancer Annual Meeting, Washington, D.C.; poster No. P322; abstract No. 10706.

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November 7—November 11, 2018

A phase 1 study to evaluate the safety and tolerability of AB928, a novel dual adenosine receptor antagonist, with AB122, a programmed cell death-1 inhibitor, in patients with advanced malignancies. Seitz L, Rieger A, Berry W, Jin L, Ashok D, Walters MJ, Piovesan D, Tan JBL, Lee S, Park A, DiRenzo D, Karakunnel J Society for Immunotherapy of Cancer Annual Meeting, Washington, D.C.; poster No. P323; abstract No. 10711.

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October 19-October 23, 2018

Final results of the Phase 1 study in healthy volunteers of AB928, a dual antagonist of the A2aR and A2bR adenosine receptors being studied as an activator of anti-tumor immune response. Seitz L, Ashok D, Leleti M, Powers J, Rosen B, Miles D, Sharif E, Jin L, Park A, Young S, Rieger A, Schindler U, Karakunnel J, Walters MJ. European Society of Medical Oncology 2018 Congress, Munich, Germany; abstract No1880P.

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September 30-October 3, 2018

AB928, a dual antagonist of the A2aR and A2bR adenosine receptors, relieves adenosine-mediated immune suppression. DiRenzo D, Piovesan D, Tan JBL, Miles DH, Leleti MR, Park T, Soriano F, Handlos B, Jeffrey J, Sharif E, Rosen B, Schindler U, Powers JP, Walters MJ. CRI-CIMT-EATI-AACR International Cancer Immunotherapy Conference: Translating Science into Survival; New York, New York; abstract No. A162.

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April 14-18, 2018

Pharmacokinetic-Pharmacodynamic relationship for AB928, a dual antagonist of the A2aR and A2bR adenosine receptors. Seitz L, Ashok D, Leleti M, Powers J, Rosen B, Miles D, Sharif E, Jin L, Park A, Young S, Soriano F, Rieger A, Karakunnel J, Walters MJ. Annual Meeting of the American Association of Cancer Research; Chicago, Illinois; abstract No. 3769.

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April 14-18, 2018

Combining adenosine receptor inhibition with AB928 and chemotherapy results in greater immune activation and tumor control. Walters MJ, Piovesan D, Tan JBL, DiRenzo D, Yin F, Miles D, Leleti M, Park T, Soriano F, Sharif E, Schindler U and Powers JP. Annual Meeting of the American Association of Cancer Research; Chicago, Illinois; abstract No. 5556.

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March 23-27, 2018

Adenosinergic Axis Provides an Anchor in Multiple Anti-tumor Combination Strategies. Tan JBL, Becker A, Piovesan D, Yin FF, Soriano F, Leleti M, Jeffrey J, Miles D, Powers JP, Schindler U, Walters MJ. Keystone Symposia on Molecular and Cell Biology: Cancer Immunotherapy: Combinations, Montreal, Canada; Abstract No. 3031.

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