Wellspring Biosciences, a wholly owned subsidiary of Araxes Pharma, announced the U.S. Food and Drug Administration (FDA) has cleared an investigational new drug (IND) application for ARS-3248, a small molecule KRAS G12C inhibitor. ARS-3248 was discovered as part of an exclusive drug discovery and development agreement with Janssen Biotech, which will conduct the Phase 1 trial and have sole responsibility for clinical development.

"Although KRAS was considered an undruggable target when we initiated this program in 2012, Wellspring scientists have shown considerable progress in being the first to demonstrate that direct and covalent inhibitors can specifically induce tumor regression in mouse tumor models harboring the mutation," said Yi Liu, Ph.D., Chief Scientific Officer of Wellspring Biosciences. "ARS-3248 represents the culmination of a significant and highly productive collaboration between scientists at Wellspring and Janssen, building upon the learnings of previous tool compounds. As we continue to advance this optimized clinical candidate that holds the potential to provide meaningful benefit to patients, we look forward to supporting Janssen as they evaluate the potential of ARS-3248 in patients with KRAS G12C-positive cancers."

ARS-3248 is an investigational, orally available small molecule that is designed to potently and selectively inhibit a form of KRAS which harbors a substitution mutation (G12C). KRAS G12C mutations are present in approximately 12 percent of non-small cell lung cancer patients, as well as subsets of patients in other tumor types, such as those with colorectal and pancreatic cancers. Tumors characterized by KRAS G12C mutations are commonly associated with poor prognosis and resistance to therapy, and patients with these mutations have few treatment options. ARS-3248 will be evaluated in a Phase 1 trial of patients with molecularly identified KRAS G12C-positive advanced solid tumors.