ARV-471 demonstrates promising anti-tumor activity in late line patients † 7 patients out of 21 are excluded from graph due to no measurable disease at baseline (n=4), discontinuation of treatment w ithout post-treatment target lesion measurements (n=2), and discontinuation after 2 doses due to noncompliance (n=1).-

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The antigen PSA was effectively down-regulated in patients using ARV-110, and the down-regulation was more than 50% in 4 patients. This range is also of great significance for patients who have received multi-line therapy. ARV-471, an estrogen receptor (ER) alpha PROTAC™ protein degrader, is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular ARV-471 demonstrated improved potency and anti-tumor activity both as a monotherapy and in combination with a CDK4/6 inhibitor, compared to current standard of care treatment regimens. We believe that ARV-471 has the potential to be the first oral protein degrader for the treatment of patients with metastatic ER-positive/HER2-negative ARV-471: an ER-targeting protein degrader for breast cancer. Arvinas is developing ARV-471, an oral estrogen receptor (ER)-targeting PROTAC® protein degrader for the potential treatment of patients with locally advanced or metastatic ER positive / HER2 negative breast cancer. 1 dag sedan · Arvinas' ARV-110 and ARV-471 are PROTAC molecules that respectively target the degradation of androgen receptor (AR) and estrogen receptor (ER). The previously announced preliminary clinical trial results showed that ARV-471 had the potential to be a best-in-class estrogen receptor degrading agent.

Arv 471

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ARV-471 degrades ERamutants ARV-471 is a potent ERadegrader SABCS, Dec 4-8, 2018 MCF7 / estradiol Summary • Orally-bioavailable ARV-471 demonstrates single-digit nanomolar ERadegradation potency in wild-type and variant ERa-expressing cell lines • ARV-471 displays no agonist activity in rodent uterine tissue

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Arv 471

ARV-471 is an investigational orally bioavailable PROTAC® protein degrader designed to specifically target and degrade the estrogen receptor (ER) for the treatment of patients with locally advanced or metastatic ER+/HER2- breast cancer.

Arv 471

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Arv 471

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ARV-471 degrades ERamutants ARV-471 is a potent ERadegrader SABCS, Dec 4-8, 2018 MCF7 / estradiol Summary • Orally-bioavailable ARV-471 demonstrates single-digit nanomolar ERadegradation potency in wild-type and variant ERa-expressing cell lines • ARV-471 displays no agonist activity in rodent uterine tissue ARV-110 and ARV471 are two PROTAC molecules developed based on Arvinas’ proprietary technology platform-PROTAC (Proteolysis-Targeted Chimera) protein degradation agent. ARV-110 is the world’s first oral bioavailable PRAOTC small molecule drug that has entered clinical trials in the field of protein degradation targeted chimeras.

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2018-12-08 · ARV-471 inhibited growth of tamoxifen-resistant and ERa gene (ESR1) mutant tumors while also reducing tumor ERa levels. ARV-471 displayed no ER agonist activity. About Arvinas ARV-471 Degraded Estrogen Receptor and Provided Improved Anti-Tumor Activity When Compared to SOC, Both as a Monotherapy and in Combination.


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