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AB801 is an orally bioavailable small molecule inhibitor of the receptor tyrosine kinase AXL. It is being developed by Arcus Biosciences for the treatment of various cancers, including renal cell carcinoma, STK11-mutant non-small cell lung cancer, colorectal carcinoma, breast cancer, ovarian cancer, head and neck squamous cell carcinoma, and bladder carcinoma. By inhibiting AXL signaling—a pathway associated with poor prognosis and therapeutic resistance in tumors—AB801 aims to overcome resistance to standard-of-care therapies and modulate the immunosuppressive tumor microenvironment. Preclinical data indicate that AB801 has excellent potency and selectivity for AXL over other kinases as well as favorable pharmacokinetic properties such as moderate clearance, long half-life, good oral bioavailability in humans, and a good safety profile.
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