Mirati Announces IND Clearance by U.S. FDA Enabling Phase 1 Initiation for First-in-Class Oral KRASG12D Selective Inhibitor, MRTX1133

Rhea-AI Summary

Mirati Therapeutics (NASDAQ: MRTX) announced FDA clearance for its Investigational New Drug (IND) application for MRTX1133, a first-in-class oral selective inhibitor targeting the KRAS^G12D mutation, affecting approximately 180,000 patients in the US and Europe. This marks the third KRAS program entering clinical development for Mirati. MRTX1133 demonstrated significant preclinical efficacy in models of pancreatic, lung, and colorectal cancers. The Phase 1/2 clinical trial is set to commence in early 2023, exploring multiple expansion cohorts. The company aims to address a significant unmet need in cancer treatment.

Positive

• FDA clearance for MRTX1133, a first-in-class oral KRAS^G12D selective inhibitor.
• Potential to address an unmet need for targeted treatment in approximately 180,000 patients with KRAS^G12D mutations.
• Demonstrated significant preclinical tumor response in pancreatic, lung, and colorectal cancer models.
• Low risk of off-target activity and favorable human half-life predicted over 50 hours.

Negative

• None.

IND demonstrates Mirati's leadership in KRAS, representing the Company's third KRAS or KRAS-signaling program to enter clinical development

SAN DIEGO, Jan. 19, 2023 /PRNewswire/ -- Mirati Therapeutics, Inc. (NASDAQ: MRTX), announced today the U.S. Food and Drug Administration (FDA) has cleared the Investigational New Drug (IND) application of MRTX1133, a potential first-in-class oral KRAS^G12D selective inhibitor for clinical evaluation. KRAS^G12D mutations impact approximately 180,000 patients in the US and Europe, representing approximately a 2.5-fold increase in prevalence compared to KRAS^G12C mutations. No targeted oncology treatment options currently exist for these patients.

MRTX1133 is a highly potent investigational inhibitor of the KRAS^G12D driver mutation and demonstrated selective and reversible inhibition of KRAS^G12D in both its active and inactive states.  In addition, MRTX1133 administration resulted in marked tumor response in preclinical KRAS^G12D mutated pancreatic cancer models as well as lung and colorectal cancer models. MRTX1133 has demonstrated favorable properties including a low risk for off-target activity and drug interactions and a predicted human half-life of greater than 50 hours.

"The clearance by the FDA to initiate clinical evaluation of MRTX1133, the third program in our KRAS franchise to enter clinical development, is illustrative of the innovative approach to drug discovery and demonstrates the best-in-class capabilities of the Mirati team. This particular mutation has been difficult to target, and we are confident in our novel oral formulation strategy, which we believe will enable near-complete target inhibition over the full dosing interval," said James Christensen, Ph.D. chief scientific officer, Mirati Therapeutics, Inc. "We are thrilled to advance MRTX1133 into clinical development and the potential to positively impact people living with KRAS^G12D-mutated cancers."

The Phase 1/2 clinical trial will launch in early 2023 with plans for multiple expansion cohorts in pancreatic, colorectal, lung and other KRAS^G12D tumor types.

About Mirati Therapeutics, Inc.

Mirati Therapeutics, Inc. is a biotechnology company whose mission is to discover, design and deliver breakthrough therapies to transform the lives of patients with cancer and their loved ones. The company is relentlessly focused on bringing forward therapies that address areas of high unmet need, including lung cancer, and advancing a pipeline of novel therapeutics targeting the genetic and immunological drivers of cancer. Unified for patients, Mirati's vision is to unlock the science behind the promise of a life beyond cancer.

For more information about Mirati, visit us at Mirati.com or follow us on Twitter, LinkedIn and Facebook. 

About MRTX1133

MRTX1133 is an investigational, highly potent, selective and reversible small molecule inhibitor of KRAS^G12D that is optimized to sustain near complete target inhibition with the potential to be both a first and best-in-class treatment option. MRTX1133 is entering Phase 1 clinical evaluation in 2023 investigating the drug's impact on KRAS^G12D-driven cancers. For more information visit Mirati.com/science.

Forward Looking Statements

This press release includes forward-looking statements regarding Mirati's business, financial guidance and the therapeutic and commercial potential of KRAZATI^TM (adagrasib), sitravatinib (TAM receptor inhibitor), MRTX1719 (MTA-cooperative PRMT5 inhibitor), MRTX0902 (SOS1 inhibitor), and MRTX1133 (selective KRASG12D inhibitor), Mirati's technologies and Mirati' other products in development. Any statement describing Mirati' goals, expectations, intentions or beliefs, financial or other projections, is a forward-looking statement and should be considered an at-risk statement. Such statements are subject to certain risks and uncertainties, including those related to the impact COVID-19 could have on our business, and including those inherent in the process of discovering, developing and commercializing medicines that are safe and effective for use as human therapeutics, and in the endeavor of building a business around such medicines.

Mirati's forward-looking statements also involve assumptions that, if they never materialize or prove correct, could cause its results to differ materially from those expressed or implied by such forward-looking statements. Although Mirati's forward-looking statements reflect the good faith judgment of its management, these statements are based only on facts and factors currently known by Mirati. As a result, you are cautioned not to rely on these forward-looking statements. These and other risks concerning Mirati's programs are described in additional detail in Mirati' annual report on Form 10-K, and most recent Form 10-Q, which are on file with the Securities and Exchange Commission and available at the SEC's Internet site (www.sec.gov). These forward-looking statements are made as of the date of this press release, and Mirati assumes no obligation to update the forward-looking statements, or to update the reasons why actual results could differ from those projected in the forward-looking statements, except as required by law.

Mirati Contacts

Investor Relations: ir@mirati.com

Media Relations: media@mirati.com

 

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SOURCE Mirati Therapeutics, Inc.

FAQ

What is MRTX1133 and its significance?

MRTX1133 is a first-in-class oral selective inhibitor targeting the KRAS^G12D mutation, which currently has no available targeted treatments.

What are the next steps for MRTX1133 after FDA clearance?

The next steps include launching a Phase 1/2 clinical trial in early 2023 with multiple expansion cohorts.

How many patients are affected by KRAS^G12D mutations?

The mutation impacts approximately 180,000 patients in the US and Europe.

What cancers will MRTX1133 target in its clinical trials?

Clinical trials for MRTX1133 will target pancreatic, colorectal, lung, and other KRAS^G12D tumor types.