Syros’ SY-5609 Shows Promising Activity in OC Models, Supports Planned Phase 1 Trial, Results Show

Syros’ SY-5609 Shows Promising Activity in OC Models, Supports Planned Phase 1 Trial, Results Show
Syros Pharmaceuticals' investigational oral inhibitor, SY-5609, can lead to a sustained inhibition of cancer growth in animal models of ovarian cancer and other solid tumors, preclinical data showed. The findings support the initiation of a Phase 1 trial testing the compound early next year, investigators said. Researchers from Syros presented the findings in a poster titled "Preclinical evaluation of PK, PD, and anti-tumor activity of the oral, non-covalent, potent and highly selective CDK7 inhibitor, SY-5609, provides rationale for clinical development in multiple solid tumor indications." The poster was presented at the AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics, held Oct. 26-30 in Boston. SY-5609 is a small molecule that serves as an oral inhibitor of cyclin-dependent kinase (CDK) 7. CDKs regulate transcription, which is the process by which DNA is transformed into RNA, leading to gene expression. Therefore, they are potential therapeutic targets for cancers that have to activate or silence specific gene pathways to survive. The preclinical experiments evaluated the effect of different doses of SY-5609, given daily to immunosuppressed mice implanted with cancer tissue extracted from patients — a research model called xenograft. Results showed that SY-5609 inhibited tumor growth in a dose-dependent manner. The study also found that a significant reduction in tumor size was achieved at doses as low as one-fifth of the maximum tolerated dose in xenografts of ovarian and breast cancer. The therapy was tested on 12 models of difficult-to-treat solid tumors, including triple-negative breast cancer, small lung cell carcinoma, and high-grade serous ovarian cancer. All of the models responded to the treatment. Add
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