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Expression of the AXL protein is high in many patients with cancer and is associated with resistance of tumors to chemotherapy, targeted therapy and immunotherapy. AB801 is a novel inhibitor of the AXL tyrosine kinase domain, discovered using a structure-based design approach.

The potency and selectivity of AB801 were shown in pre-clinical studies to be improved over other AXL inhibitors and is able to inhibit AXL without the liabilities associated with off-target effects.

In preclinical studies, AB801 has been shown to result in tumor regression when administered in combination with standard of care therapies in colon carcinoma, non-small cell lung cancer and clear cell renal cell carcinoma models.

Arcus is evaluating AB801 alone and in combination with zimberelimab, another investigational molecule in the Arcus portfolio, and chemotherapy for the treatment of advanced solid tumors.