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MTX-531 is an experimental small molecule from MEKanistic Therapeutics, in phase 1 trials for head and neck squamous cell carcinoma, endometrial cancer and HER2-negative metastatic breast cancer and other cancers.
MTX-531 is a small molecule (oral) from MEKanistic Therapeutics. A computationally designed small molecule that inhibits both EGFR and PI3K; the company says PPAR-gamma agonist activity reduces the hyperglycaemia expected from PI3K inhibition. Its furthest stage is phase 1, for head and neck squamous cell carcinoma, endometrial cancer, HER2-negative metastatic breast cancer and RAS and BRAF wild-type metastatic colorectal cancer. ClinicalTrials.gov registers it in one study linked below. Phase 1 NCT07874880 not yet recruiting (registry, first posted 15 Oct 2026). Whether it works in people has not been established unless a trial below reports it.
A computationally designed small molecule that inhibits both EGFR and PI3K; the company says PPAR-gamma agonist activity reduces the hyperglycaemia expected from PI3K inhibition. Connects to EGFR.
1.MTX-531 slips into a pocket on EGFR.
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Query for this drug: (TITLE:"MTX-531" OR ABSTRACT:"MTX-531") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about MTX-531, not a curated reading list.
Shares MEKanistic Therapeutics, EGFR and the tag pipeline.
Shares Endometrial cancer, Breast cancer (all types), Metastatic cancer (cancer that has spread), Colorectal cancer and the tag pipeline.
Shares Endometrial cancer, Metastatic cancer (cancer that has spread), Colorectal cancer and the tag pipeline.
Shares Endometrial cancer, Breast cancer (all types), Metastatic cancer (cancer that has spread) and the tag pipeline.
Shares EGFR, Metastatic cancer (cancer that has spread) and the tag pipeline.
Shares EGFR, Metastatic cancer (cancer that has spread) and the tag pipeline.
Shares Endometrial cancer, Metastatic cancer (cancer that has spread), Colorectal cancer and the tag pipeline.
Shares EGFR, Metastatic cancer (cancer that has spread) and the tag pipeline.
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