Mirati begins dosage in MGCD265 Phase 1b clinical trial for NSCLC

Mirati Therapeutics, Inc. (NASDAQ: MRTX) today announced that the first patient with Non-Small Cell Lung Cancer (NSCLC) has been dosed in a Phase 1b clinical trial of MGCD265 in selected patients exhibiting genetic alterations of MET or Axl. In this segment of the study, one of the expansion cohorts will enroll patients with NSCLC and another will enroll patients with other solid tumors. Both cohorts will enroll only those patients that have specific MET driver mutations including MET gene point mutations, gene amplification, and MET or Axl gene rearrangements.

"In the dose escalation phase of this trial, we identified an optimal dose that achieved serum levels that we believe will result in greater than 90% inhibition of MET and Axl," said Charles M. Baum, M.D., Ph.D., president and CEO of Mirati. "We are focused on patients whose tumors harbor the specific MET and Axl genetic alterations that MGCD265 is designed to treat. By selecting and treating only those patients who carry the targeted mutations, there is strong rationale that we'll see proof of concept based on a high overall response rate in early 2015 that supports accelerated drug development."

MGCD265 is an orally bioavailable tyrosine kinase inhibitor that selectively targets MET and Axl. Genetic alterations in these targets have been implicated as drivers of tumor growth and disease progression in NSCLC, and other solid tumors. MET and Axl are also implicated as drivers of tumor progression in patients whose tumors have become resistant to EGFR inhibitors such as Tarceva, Iressa and Erbitux. Therefore, the combination of MGCD265 with EGFR inhibitors may also address acquired resistance to agents targeting EGFR.

The open-label Phase 1b study of MGCD265 is expected to enroll up to 60 patients with one cohort focused on NSCLC and another that will enroll patients with advanced solid tumors that carry genetic alterations in MET or Axl. The purpose of this trial is to evaluate the safety and efficacy of MGCD265 administered to selected patients with specific activating MET driver mutations, MET gene amplification, and MET or Axl gene rearrangements. Additional information about this clinical trial of MGCD265 is available at www.clinicaltrials.gov using identifier: NCT00697632.