Combining OP-3136, a KAT6 inhibitor, with endocrine therapy and CDK4/6 inhibitor enhances anti-tumor activity in ER+/HER2- breast cancer models
Combining palazestrant, a CERAN, and capivasertib, a pan-AKT inhibitor, enhances tumor suppression in ER+/HER2- breast cancer models
Combining palazestrant, a CERAN, and everolimus, an mTOR inhibitor, enhances tumor suppression in ER+/HER2- breast cancer models
OPERA-01: A randomized, open-label, phase 3 study of palazestrant (OP-1250) vs. standard-of-care treatment for ER+/HER2− advanced or metastatic breast cancer after endocrine and CDK4/6 inhibitor therapy
A phase 1b/2 study of palazestrant (OP-1250) in combination with ribociclib in patients with estrogen receptor-positive, human epidermal growth factor receptor 2-negative, advanced and/or metastatic breast cancer
Palazestrant (OP-1250), a complete estrogen receptor antagonist, inhibits wild-type and mutant ER-positive breast cancer models as monotherapy and in combination
A phase 1b/2 study of palazestrant (OP-1250) in combination with ribociclib in patients with estrogen receptor-positive, human epidermal growth factor receptor 2-negative, advanced and/or metastatic breast cancer
OPERA-01: A randomized, open-label, phase 3, study of palazestrant (OP-1250) vs standard-of-care treatment for ER+, HER2- advanced or metastatic breast cancer after endocrine and CDK4/6 inhibitor therapy
A phase 1b/2 study of palazestrant (OP-1250), an oral complete estrogen receptor antagonist (CERAN) and selective ER degrader (SERD), with palbociclib in ER-positive, HER2-negative, advanced or metastatic breast cancer patients
Results from the phase 1/2 study of OP-1250, an oral complete estrogen receptor (ER) antagonist (CERAN) and selective ER degrader (SERD) in patients (pts) with advanced or metastatic ER-positive, HER2-negative breast cancer
The discovery of potent KAT6 inhibitors that demonstrate anti-tumor activity in preclinical models of ER+ breast cancer
A phase 1b dose escalation and expansion study of OP-1250 in combination with ribociclib or alpelisib in patients with advanced and/or metastatic estrogen receptor-positive (ER+)/HER2- breast cancer
A phase 1b/2 study of OP-1250, an oral complete estrogen receptor antagonist (CERAN) and selective er degrader (SERD) with palbociclib in patients with advanced or metastatic HR+/HER2- breast cancer
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)
Combination of complete estrogen receptor antagonist, OP-1250, and CDK4/6 inhibitors enhances tumor suppression and inhibition of cell cycle-related gene expression
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)
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
OP-1250 prevents tumor spread in a model of metastatic mutant ERα+ breast cancer
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
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
Complete estrogen receptor (ER) antagonism as an optimal approach for ER-positive breast cancer drug development
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
The complete estrogen receptor antagonist OP-1250 shrinks tumors in xenograft models and has favorable preclinical pharmacokinetic attributes
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)
Development of OP-1250, an oral complete estrogen receptor antagonist (CERAN) that shrinks ER-positive breast tumors in xenograft models
OP-1250, a complete estrogen receptor antagonist (CERAN) that penetrates the brain and prevents lethality from intracranial xenograft tumors expressing mutant ESR1
Specific stereochemistry of OP-1074 disrupts estrogen receptor alpha helix 12 and confers pure antiestrogenic activity
OP-1250: a potent orally available complete antagonist of estrogen receptor-mediated signaling that shrinks wild type and mutant breast tumors.