Researchers at the University of Michigan Health Rogel Cancer Center have developed a new drug candidate, MTX-531, that may help overcome resistance to cancer therapies.
This promising molecule targets two key proteins involved in cancer therapy resistance, potentially offering a more effective treatment option for certain types of cancer.
The study detailing the design and preclinical evaluation of MTX-531 was published in Nature Cancer.
Led by Judith Sebolt-Leopold, Ph.D., the research team discovered that MTX-531 is a kinase inhibitor capable of selectively blocking both the epidermal growth factor receptor (EGFR) and phosphatidylinositol 3-OH kinase (PI3K).
These proteins are known to drive resistance to cancer treatments in various tumors.
“By dual targeting of EGFR and PI3K, MTX-531 shuts down the escape mechanisms that tumors use to resist treatment.
This is especially important in cancers like head and neck squamous cell carcinomas, where each of these proteins can help tumors resist the inhibition of the other,” said Sebolt-Leopold, a research professor of radiology and pharmacology at Michigan Medicine and co-leader of Rogel’s developmental therapeutics program.
The study demonstrated that in mouse models, MTX-531 led to tumor regressions in multiple head and neck cancer models and was well-tolerated by the animals.
Additionally, when combined with drugs targeting the RAS pathway, MTX-531 was highly effective against KRAS-mutated gastrointestinal tumors, including those originating in the colon or pancreas.
One of the significant advantages of MTX-531 over other PI3K inhibitors is its lack of severe side effects, such as hyperglycemia, which often leads to the discontinuation of treatment. This suggests that MTX-531 could become a less-toxic treatment option for patients.
The innovative design of MTX-531 was achieved through a computational chemistry approach led by Sebolt-Leopold and Christopher Whitehead, Ph.D., a former member of the Leopold laboratory team and now the chief operating officer of MEKanistic Therapeutics, Inc. Sebolt-Leopold and Whitehead have a long history of collaboration, dating back over 20 years when they worked together on Pfizer’s MEK inhibitor program.
Sebolt-Leopold emphasized the unique opportunity at Michigan Medicine to extend research on molecular targeted agents to a more translational level, bridging the gap between laboratory discoveries and clinical applications.
The team is currently advancing the development of MTX-531 to support clinical evaluation. Researchers are hopeful that these efforts will lead to clinical trials in patients, potentially offering a new and effective treatment for cancers resistant to current therapies.
In summary, MTX-531 represents a significant step forward in cancer research, with the potential to improve outcomes for patients facing therapy-resistant cancers.
The continued development and eventual clinical trials of this drug candidate could provide new hope for effective cancer treatments.
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