Keeping the Gas off AXL
Aravive has developed an AXL inhibitor with unprecedented affinity
With its development of an AXL decoy able to trap and sequester the native receptor’s ligand with femtomolar affinity, Aravive Biologics Inc. believes it has a biologic that can bypass the potency and selectivity issues of the small molecule AXL inhibitors already in the clinic for cancer. The company plans to submit an IND in 2017 for its lead candidate, Aravive-S6, in leukemia.
Last month, Aravive changed its name from Ruga Corp., and moved from Palo Alto to Houston to accept a $20 million grant from the Cancer Prevention & Research Institute of Texas (CPRIT) to help bring the compound to the clinic.
AXL is a receptor tyrosine kinase (RTK) on the surface of cells that binds the ligand GAS6 to trigger a survival response. Cancers co-opt the pathway to metastasize and become drug resistant, and overactivity is associated with poor survival.
There are no drugs on the market targeting the pathway, but at least 10 products are in preclinical or clinical development. The most advanced are small molecules, but four, including Aravive-S6, are biologics (see “Putting the Brakes on AXL”).
Table: Putting the brakes on AXL
Select AXL receptor tyrosine kinase (AXL; UFO)-targeted therapeutics in clinical and preclinical development. At least three AXL inhibitors are in clinical