Arresting cancer resistance
Developing a novel category of precision medicines that offer targeted and long-lasting benefits for cancer patients.
Pipeline
Harnessing the potential of well-established biological targets, our portfolio of rationally designed small molecules arrest the pathways exploited by PI3KCA mutant cancers to elude and resist existing treatment modalities.
Science
Background
PIK3CA is one of the most frequently mutated genes across a spectrum of solid cancers including head and neck, lung, breast, and gastrointestinal malignancies.
Cancer cells often develop resistance mechanisms to evade the effects of PI3K inhibitors. This can occur through mutations in the PI3K pathway or activation of alternative signaling pathways, rendering these inhibitors ineffective over time.
Despite these challenges, continuous refinement of drug design and the deepening understanding of the underlying biology of PI3K signaling are poised to unlock the full therapeutic potential of these medicines.
MTX-531
Introducing MTX-531, a first-in-class small molecule dual inhibitor of PI3K and its crucial adaptive resistance pathway, EGFR, marking a new frontier in precision medicine. Read more about the science and the preclinical results in a recent Nature Cancer publication.
New Hope for Cancer Patients
Inhibiting EGFR mitigates the necessity to escalate PI3K dosages, thereby reducing exposure to toxicity and broadening the therapeutic index. This not only enhances activity but also yields more durable anti-tumor results.
MTX-531
TOXICITY /
Enhanced safety margin.
The first pan-PI3K inhibitor known to circumvent hyperglycemia induction.COMBINATIONS /
Potentiates the efficacy of established treatments.
Exhibits significant synergy with RAS pathway inhibitors, radiation therapy, and immunotherapyIMPACT /
Applicable across multiple cancer indications.
Complete regressions have been observed in multiple preclinical models. Early clinical trials will encompass a diverse range of PIK3CA and KRAS mutant cancers.PARTNERS /
Selected for NCI’s NExT program.
MEKanistic is partnering with the NCI to accelerate the development of this promising cancer therapy towards the clinic.
“Preclinical data supports MTX-531’s anti-tumor activity and the ability to arrest the paradoxical resistance that has limited other KRAS inhibitors. This bodes well for MTX-531 as a single agent therapy and also in combination with other cancer therapies currently on trial and in the clinic.”
— Dr. Patricia LoRusso,
Leading Phase 1 investigator and Professor of Medicine and Associate Director for Innovative Medicine at Yale Cancer Center, and President-Elect of American Association for Cancer Research
Addressing a wide range of cancer indications.
Head and neck
Breast
Lung
Gastrointestinal
Contact us
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