Mirati Therapeutics announced the U.S. Food and Drug Administration (FDA) has cleared the company's investigational new drug (IND) application for MRTX849, a small molecule inhibitor of KRAS G12C. Mirati is developing MRTX849 for the treatment of cancers driven by KRAS G12C mutations.

"KRAS mutations, like the G12C mutation, are recognized as drivers of multiple tumor types, including non-small cell lung cancer and colorectal cancers. Efforts over the last 25 years to develop drugs to inhibit mutant KRAS have been largely unsuccessful," said James Christensen, Ph.D., Chief Scientific Officer, Mirati Therapeutics. "MRTX849 represents the culmination of significant scientific effort by our research team to design a potent and highly selective inhibitor of KRAS G12C. We believe that this scientific breakthrough has the potential to result in meaningful and lasting clinical benefit for patients with G12C mutation-positive cancers. We look forward to working with patients and physicians to evaluate the potential of MRTX849."

FDA clearance of the IND enables Mirati to initiate its planned Phase 1/2 clinical trial in patients with advanced solid tumors that harbor KRAS G12C mutations. The Phase 1 dose escalation phase of the trial will assess the safety, tolerability, pharmacokinetics and preliminary anti-tumor activity of MRTX849 in patients with molecularly-identified KRAS G12C-positive cancers. A dose expansion phase is planned to follow the selection of a recommended Phase 2 dose. Mirati expects the first patient to be enrolled in the trial by January 2019.

MRTX849 is an orally-available small molecule that potently and selectively inhibits a form of KRAS which harbors a substitution mutation (G12C). KRAS G12C mutations are present in approximately 14% of NSCLC adenocarcinoma patients and 5% of colorectal cancer patients. 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. MTRX849 has demonstrated broad-spectrum tumor regression in a large cohort of KRAS G12C-positive pre-clinical in-vivo human tumor models. MRTX849 demonstrated complete regression of tumors in a subset of models at well-tolerated dose levels. Early proof-of-concept clinical data is anticipated in 2019.

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