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1. Clear MoA- Restores T Cell Function through Inhibition on Adenosine Signaling Pathway
(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.
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.
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.
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.)
Explore our catalog of therapeutic antibody solutions to find the right products for you! We are dedicated to delivering solutions designed to help you drive innovation and push the boundaries of what therapeutic antibodies can be.
Organoid Toolbox is a collection of organoid solutions including ready-to-use organoids, organoid differentiation kits, and a variety of services to accelerate the progress of your drug development project.
To enable antibody characterization methodsACROBiosystems has developed a series of enzymes.such as ldeS, SpeB, EndoH, and Endo S proteases, toassist with the characterization of antibodies and theirrelated post-translational modifications (PTMs)
ACROBiosystems developed a series of GMP grade cytokines under the GMP grade quality management system. Those products are all suitable for T/NK cell generation, activation, and proliferation in cell therapy research.
50+ targets designed for CAR detection, including PE/FITC/biotin labeled proteins. The key reagents for CD19 and BCMA were FDA DMF filed which can support your IND, NDA and BLA process.
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