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SIGX1094 is a first-in-class, clinical-stage **dual FAK/SRC inhibitor** developed by Signet Therapeutics using proprietary organoid disease modeling and AI-driven drug design. It is the world's first targeted therapy candidate for diffuse gastric cancer (DGC), an aggressive malignancy with no approved targeted treatments, and has demonstrated preclinical efficacy both as monotherapy and in combination regimens for DGC and other metastatic solid tumors such as ovarian cancer, triple-negative breast cancer, and pancreatic cancer. SIGX1094 works by simultaneously inhibiting Focal Adhesion Kinase (FAK) and SRC kinase, key components that form a complex driving critical downstream signaling involved in cancer progression and metastasis. This dual inhibition strategy overcomes compensatory resistance mechanisms observed with single-target agents. SIGX1094 received FDA Fast Track and Orphan Drug Designation in late 2024 and entered Phase I clinical trials in China in early 2025. The drug was discovered and optimized in collaboration with XtalPi, leveraging AI, quantum physics, and robotics for molecular design and screening, and validated using Signet’s patient-derived organoid models[1][2][3][4][6][8][10].
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