On May 7, 2019 Syros Pharmaceuticals (NASDAQ: SYRS), a leader in the development of medicines that control the expression of genes, reported the online publication of a new manuscript, Discovery and Characterization of SY-1365, a Selective, Covalent Inhibitor of CDK7, in the American Association for Cancer Research (AACR) (Free AACR Whitepaper)’s (AACR) (Free AACR Whitepaper) journal, Cancer Research (Press release, Syros Pharmaceuticals, MAY 7, 2019, View Source [SID1234535853]). SY-1365, a first-in-class selective cyclin-dependent kinase 7 (CDK7) inhibitor, is currently being investigated in a Phase 1 clinical trial as a single agent and in combination with standard-of-care therapies in multiple ovarian and breast cancer patient populations that lack effective treatment options. This publication highlights the discovery, mechanism of action and promise of SY-1365 as a new targeted approach for a range of difficult-to-treat cancers.
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"SY-1365 represents a potentially transformative targeted approach for a number of cancers that have eluded treatment with existing approaches," said Eric R. Olson, Ph.D., Syros’ Chief Scientific Officer. "While CDK7 has long been a target of interest, it was historically difficult-to-drug. This new publication profiles our work in discovering SY-1365, which we believe to be the most advanced selective CDK7 inhibitor in clinical development, and the substantial anti-tumor activity seen in preclinical models that supported its advancement into the clinic. We are excited by the promise of CDK7 inhibition and the potential benefit SY-1365 may bring to patients who are in dire need of better therapies."
Syros is currently conducting a Phase 1 clinical trial assessing the safety and efficacy of SY-1365 as a single agent and in combination with standard-of-care therapies in multiple ovarian and breast cancer patient populations. The trial includes cohorts evaluating SY-1365 as a single agent in patients with relapsed ovarian clear cell cancer and in high-grade serous ovarian cancer (HGSOC) patients who have had three or more prior lines of therapy; in combination with carboplatin in HGSOC patients who have had one or more prior lines of therapy; in combination with fulvestrant in metastatic hormone receptor-positive breast cancer patients who are resistant to treatment with a CDK4/6 inhibitor; and as a single agent in patients with solid tumors of any histology accessible for biopsy. Additional details about the trial can be found using the identifier NCT03134638 at www.clinicaltrials.gov.
CDK7 plays a key role in the transcription of genes and in cell cycle regulation, and inhibiting CDK7 disrupts two important processes that cancer cells use to survive: 1) expression of cancer-promoting genes; and 2) uncontrolled cell cycle progression. SY-1365 has shown anti-tumor activity in preclinical models of a range of solid tumors and blood cancers, including cancers that have become resistant to treatment with existing therapies or where existing options have failed to provide meaningful benefit to patients. Further, data suggests that SY-1365 works to inhibit the growth of cell lines representing many different cancer types at nanomolar concentrations, decreases MCL1 protein levels, and demonstrates activity among cancer cells with low BCL-XL expression.
Building on its leadership in CDK7 inhibition, Syros is advancing SY-5609, a highly selective and potent oral CDK7 inhibitor, toward clinical development. In preclinical studies, SY-5609 has demonstrated substantial anti-tumor activity, including inducing complete regressions in cell line-derived xenograft models of breast and ovarian cancers. The company plans to complete investigational new drug application (IND)-enabling studies by the end of 2019 to support the initiation of a Phase 1 oncology trial in early 2020.