A Phase 1b/2 dose escalation and dose expansion study of OP-1250, an oral complete estrogen receptor antagonist (CERAN)/selective estrogen receptor degrader (SERD), in combination with the CDK4/6 inhibitor palbociclib in patients with advanced and/or metastatic estrogen receptor (ER)-positive, HER2-negative breast cancer (OP-1250-002; NCT05266105)
Poster: 2022 San Antonio Breast Cancer Symposium. #P3-07-15
Combination of complete estrogen receptor antagonist, OP-1250, and CDK4/6 inhibitors enhances tumor suppression and inhibition of cell cycle-related gene expression
Poster: 2022 San Antonio Breast Cancer Symposium. #P2-24-07
Preliminary Phase 1/2 results from OP-1250-001, a study of OP-1250, an oral CERAN/SERD, in patients with advanced and/or metastatic estrogen receptor (ER)-positive, HER2-negative breast cancer (NCT04505826)
Poster: 34th EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics 2022 #101/PB091
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
Poster: American Association for Cancer Research Annual Meeting 2022
OP-1250 Prevents Tumor Spread in a Model of Metastatic Mutant ERα+ Breast Cancer
Poster: American Association for Cancer Research Annual Meeting 2022
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
Poster: 2021 San Antonio Breast Cancer Symposium. #P1-17-12
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
Poster: 2021 San Antonio Breast Cancer Symposium. #P5-08-07
A Phase 1/2 Dose Escalation and Expansion Study of OP-1250 in Adults with Advanced and/or Metastatic Hormone Receptor-positive (HR+), HER2-negative (HER2-) Breast Cancer
Poster: 2021 AACR-NCI-EORTC Virtual International Conference
Complete Estrogen Receptor (ER) Antagonism As An Optimal Approach for ER-Positive Breast Cancer Drug Development
Poster: 2021 JCA-AACR Precision Cancer Medicine International Conference [Virtual].
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
Late-breaking poster: American Association for Cancer Research Annual Meeting 2021 [Virtual]. #LB-122
The Complete Estrogen Receptor Antagonist OP-1250 Shrinks Tumors in Xenograft Models and Has Favorable Preclinical Pharmacokinetic Attributes
Poster: 2020 San Antonio Breast Cancer Symposium [Virtual]. #PS-18-16
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)
Poster: 2020 San Antonio Breast Cancer Symposium [Virtual]. #OT-09-10
Development of OP-1250, an oral Complete Estrogen Receptor Antagonist (CERAN) that shrinks ER-positive breast tumors in xenograft models
Hodges-Gallagher L, Sun R, Myles DC, Harmon CL, Kushner PJ | Poster: San Antonio Breast Cancer Symposium, December 10-14, 2019. #P5-05-02
OP-1250, a Complete Estrogen Receptor Antagonist (CERAN) that penetrates the brain and prevents lethality from intracranial xenograft tumors expressing mutant ESR1
Hodges-Gallagher L, Sun R, Myles DC, et al. | Poster: American Association for Cancer Research Annual Meeting 2020 [Virtual]. #4376
Specific stereochemistry of OP-1074 disrupts estrogen receptor alpha helix 12 and confers pure antiestrogenic activity
Fanning SW, Hodges-Gallagher L, Myles DC, et al. | Nature Communications. 2018;9:2368.
OP-1250: a potent orally available complete antagonist of estrogen receptor-mediated signaling that shrinks wild type and mutant breast tumors.
Hodges-Gallagher L, Sun R, Myles DC, Harmon CL, Kushner PJ, Poster: ENA 2020: EORTC-NCI-ACCR: 32nd Symposium [Virtual]