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Your Position: Casa > Licensing > BYZ202202

A2aR/A2bR Antagonist

BLA Filing
  • Project profile
    Project name: A2aR/A2bR Antagonist
    Indications: Advanced/metastatic solid tumors or hematological malignancies
    Research phase: IND approved (FDA)
    Cooperation demands: License-out (Ex-China) or co-development
  • Highlights

    1. Clear MoA- Restores T Cell Function through Inhibition on Adenosine Signaling Pathway

    Clear MOA

    (1) The asset treatment results in decrease of pCREB, a downstream PD marker of adenosine signaling.

    (2) The asset antagonizes the immunosuppressive effects by NECA (adenosine analogue) and results in rescue of IL-2 and TNF-α secretion from CD4+ T cells and CD8+ T cells, which suggests the recovery of anti-tumor effects of T cells.

    2. Shows Significant Monotherapy Activity

    (1) The asset shows anti-tumor effects in a dose-dependent manner in the mouse MC38-hPD-L1 colorectal tumor model.

    (2) The asset shows better anti-tumor activity than AB928 at the same dose.

    (3) The asset reduces Treg infiltrated in tumors.

    Clear MOA

    3. Significant Synergy with Tecentriq (PD-L1 mAb) &Keytruda (PD-1mAb)

    (1) The asset has comparable anti-tumor effects with Tecentriq & Keytruda (PD-L1 mAb) in the mouse MC38-hPD-L1 colorectal tumor model/ humanized HCC827 NSCLC model.

    (2) Combo of the asset and Tecentriq & Keytruda shows significant synergy.

    Clear MOA

    4. Non-clinical TOX Studies were observed

    (1) In the pivotal 4-week repeated dose toxicity with a 4-week recovery period in SD rats and beagle dogs, animals in this asset treated group were well tolerated, and a good safety margin (3.6 vs. NOAEL in dogs, 25.9 vs. HNSTD in rats) was achieved.

    (2) The IC50 of hERG current was >40 μM.

    (3) Showed low risk for the cardiovascular, respiratory and central nervous system in safety-pharmacology studies.

    (4) No genotoxicity was noted in the chromosomal aberration test in Chinese hamster lung fibroblasts.

    (5) No genotoxic effect on CD-1 mice bone marrow cells was observed in mice bone marrow micronucleus study.

  • Project Introduction

    1. Asset type: A2aR/A2bR Antagonist

    2. Indication: Advanced/metastatic solid tumors or hematological malignancies

    3. Research phase: IND approved (FDA)

    4. Administration route oral Tablets(5 mg/25 mg/75 mg)

    5. Cooperation demands: License-out (Ex-China) or co-development

    6. Research progress:

    (1) Project Advantages: The fourth A2aR/A2bR inhibitor worldwide, with the characteristics of high activity, high selectivity and low toxicity.
    (2) Patent Strategy: The core patents are expected to be filed in major countries in October 2022. (CN, PCT, US, EP, JP, CA, AU, FR, SG etc.)

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