Decreasing Expression of Oncogenic Transcription Factors
SY-1365 is a first-in-class potent and selective inhibitor of the cyclin-dependent kinase 7 (CDK7) that is in a Phase 1 clinical trial in patients with advanced solid tumors, including cancers such as triple negative breast, small cell lung and ovarian cancers that are dependent on unusually high expression of transcription factors for their growth and survival.
SY-1365 has shown significant anti-proliferative and pro-apoptotic activity in multiple preclinical models of difficult-to-treat solid tumors, including triple negative breast, small cell lung and ovarian cancers. SY-1365 has induced anti-tumor activity in both cell line-derived xenograft and patient-derived xenograft models of triple negative breast cancer, including significant regressions at a twice weekly dosing regimen consistent with the initial regimen being used in the Phase 1 clinical trial. In preclinical models, SY-1365 has also been shown to preferentially kill cancer cells over non-cancerous cells and can lower the expression of oncogenic transcription factors, including MYC.
Upon establishing the appropriate dose in the ongoing Phase 1 trial, we plan to expand development of SY-1365 into acute leukemia, including acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL).