• OP-1250 is a complete ER antagonist (CERAN) and selective ER degrader (SERD), which blocks both the AF1 and AF2 transcriptional activation domains of the ER3 (Figure 1). OP …
FDA Fast Tracks OP-1250 for HR+, HER2- Metastatic ... - Targeted …
2022年7月21日 · OP-1250 is a novel, oral complete estrogen receptor (ER) antagonist and selective ER degrader (SERD). In a preclinical study, it was shown that OP-1250 antagonizes …
Breast cancer therapies with paradigm-shifting potential. - Olema
Our lead investigational drug, palazestrant (OP-1250), is a novel oral compound developed to completely antagonize the estrogen receptor (ER) and block the ER-mediated cancer cell …
OP-1250: A potent orally available complete antagonist of …
Here we describe the preclinical development of OP-1250, a complete ER antagonist with good oral bioavailability and favorable pharmacokinetics, a combination that may particularly benefit …
HER2阴性转移性乳腺癌新疗法：OP-1250获快速通道指定 - 知乎
美国食品和药物管理局 (FDA)于近日授予新型抗癌药OP-1250快速通道指定，用于治疗HER2阴性的 转移性乳腺癌 (mBC)患者，港安健康国际指出补充，这些患者在接受1个或多个线的内分泌 …
•OP-1250 is a once-daily oral small molecule complete estrogen receptor antagonist (CERAN) and selective estrogen receptor degrader (SERD) that has displayed preclinical efficacy in a …
202P A phase Ib/II study of OP-1250, an oral complete ... - ESMO …
OP-1250 is small molecule CERAN/SERD that binds to and completely blocks transcriptional activity of wild-type and mutant ER. OP-1250 was well tolerated in a phase I/II monotherapy …
OP-1250获FDA的快速通道指定用于ER+/HER2-转移性乳腺癌患者…
2022年10月31日 · OP-1250是一款兼具完全雌激素受体拮抗剂 (CERAN)和选择性雌激素受体降解剂 (SERD)活性的口服小分子药物，能有效且完全地抑制ER (AF1和AF2转录激活域)的活性， …
A phase 1b/2 dose escalation and expansion study of OP-1250 in ...
2023年5月31日 · OP-1250 is a small molecule oral complete estrogen receptor antagonist (CERAN) and selective estrogen receptor degrader (SERD) that binds the ligand binding …
382MO Updated results from the phase I/II study of OP-1250, an …
OP-1250 is a small molecule CERAN/SERD with antitumor activity in breast cancer (BC) xenograft models, including ESR1/PIK3CA mutations and brain metastasis. OP-1250 was …