Syros Pharmaceuticals’ investigational compound SY-1365 showed potent anticancer activity in cell and animal models of ovarian cancer, giving the company momentum to move toward the Phase 1 trial it plans later this year.
SY-1365 was also active against breast cancer and lung cancer, Syros said at the American Association of Cancer Research (AACR) 2017 Annual Meeting in Washington. Its presentation was titled “SY-1365, a potent and selective CDK7 inhibitor, exhibits promising anti-tumor activity in multiple preclinical models of aggressive solid tumors.”
The treatment targets cancer by blocking a molecule known as CDK7, for cyclin-dependent kinase 7, Many cancers’ growth and survival are dependent on the activation of specific genes, and SY-1365 interferes with gene activation, which scientists call transcription.
Syros is also developing drugs to target CDK12 and CDK13, which belong to the same family of proteins as CDK7.
“SY-1365, our first-in-class selective CDK7 inhibitor, as well as our CDK12 and CDK13 inhibitor program, highlight the power of our gene control platform to selectively target transcription and potentially treat diseases that have been underserved by other genomic-based approaches,” Nancy Simonian, MD, chief executive officer of Syros, said in a press release.
“These new data show SY-1365 reduces proliferation and induces apoptosis [programmed cell death] in cancer cells in several difficult-to-treat tumors. The results build on earlier data demonstrating that SY-1365 preferentially kills cancer cells over non-cancerous cells and lowers the expression of disease-driving transcription factors,” she added.
Syros has tested SY-1365 in many lab-grown cancer cells. The compound has also proved effective in animals injected with either lab-grown cancer cells or cells derived from patients.
In addition, the drug works well with anticancer agents that block the expression of the BCL-2 protein, researchers said.
All CDK factors impact gene transcription. Syros’ results suggest that different protein family members can block the activity of specific sets of genes, making it possible to adapt the treatment to various tumor types. Ovarian cancer is among those that respond to CDK12 and CDK13 blockers as well as CDK7.
“Our CDK12 and CDK13 inhibitor program further highlights the potential of our platform to produce drug candidates that target the transcription of unique sets of genes linked to specific tumors,” Simonian said.
Syros said its plans for the Phase 1 clinical trial of SY-1365 are on schedule.