Precision Run-on Sequencing (PRO-Seq) Analysis of a Treatment Time Course in ER+ Breast Cancer Cell Lines Profiles the Transcriptional Changes Underlying Response to Complete Estrogen Receptor Antagonist (CERAN) OP-1250
Preliminary Data From a Phase 1/2, Multicenter, Dose Escalation Study of OP-1250, an Oral CERAN/SERD, in Patients With Advanced and/or Metastatic Estrogen Receptor (ER)-Positive, HER2-Negative Breast Cancer
The Complete Estrogen Receptor Antagonist OP-1250 Can Combine with HER2 Inhibition to Inhibit Estrogen Receptor-driven Cellular Proliferation and Shrink Xenograft Tumors in ER+/HER2+ Breast Cancer Models
The complete estrogen receptor antagonist (CERAN) OP-1250 shrinks ER+ breast cancer tumors expressing the ESR1-Y537S mutant estrogen receptor in an intracranial xenograft model of brain metastases
A Phase I/II Open-label, First-in-Human, Multicenter, Dose Escalation and Dose Expansion Study of OP-1250 monotherapy in adult subjects with locally advanced, recurrent, and metastatic Hormone Receptor (HR)-positive, HER2-negative breast cancer (NCT04505826)
Specific stereochemistry of OP-1074 disrupts estrogen receptor alpha helix 12 and confers pure antiestrogenic activity
“[The] findings inform future design efforts, providing a framework for structure based design for breast cancer drugs with superior antagonist and pharmacological properties."