NEW HAVEN, Conn., Feb. 17, 2022 (GLOBE NEWSWIRE) -- Arvinas, Inc. (Nasdaq: ARVN), a clinical-stage biotechnology company creating a new class of drugs based on targeted protein degradation, today announced completed Phase 1 and interim Phase 2 ARDENT data for bavdegalutamide (ARV-110), a novel PROTAC® degrader targeting the androgen receptor (AR).

ARV-110 Demonstrates Efficacy and Plasma PSA Reduction in an Enzalutamide-Insensitive PDX Model ARV-110 is showing early clinical benefit in highly refractory patients

2022年10月19日 · The first clinically evaluated PROTAC protein degrader is ARV-110, an orally bioavailable PROTAC AR degrader developed by Arvinas. On the basis of Arvinas data, ARV-110 can completely degrade AR in all tested cell lines (LNCaP, VCaP, MCF-7, among the others) with a half maximal degradation concentration (DC 50) value of <1 nM in vitro, showing ...

ARV-110是Arvinas公司开发的一种first in class每日口服1次PROTAC蛋白降解剂，选择性靶向和降解雄激素受体(AR)蛋白，拟开发用于治疗转移性去势抵抗性前列腺癌(mCRPC)。

2023年10月25日 · 近日， Arvinas 公司在欧洲肿瘤内科学会（ ESMO ）上公布其靶向雄激素受体（ AR ）的 PROTAC 蛋白降解剂 bavdegalutamide （ ARV-110 ）以及其第二代 AR 靶向 PROTAC 降解剂 ARV-766 治疗转移性去势抵抗性前列腺癌（ mCRPC ）患者的 1/2 期临床试验的积极疗效、耐受性结果。

2025年1月1日 · Arvinas, a PROTAC technology pioneer, pioneered the field of targeted protein degradation and promoted the first two PROTAC molecules into the clinical stage in 2018, with ARV-110 being the first androgen receptor degrader to enter the clinical stage for the treatment of prostate cancer, especially advanced prostate cancer and metastatic ...

2024年12月13日 · Bavdegalutamide (ARV-110) is a PROteolysis TArgeting Chimera (PROTAC®) protein degrader that recruits the cereblon-containing E3 ubiquitin ligase to direct the polyubiquitination and subsequent proteasomal degradation of AR. Bavdegalutamide selectively degrades wild-type AR and most clinically relevant mutants with low nanomolar potency.

2022年2月16日 · Conclusions: ARV-110, a novel AR protein degrader, demonstrates clinical activity in a post-NHA, heavily pretreated mCRPC pt population, with greatest PSA 50 activity and RECIST responses in pts with AR T878 and/or H875 mutations, likely representing a particularly ARV-110–sensitive population.

2020年5月23日 · ARV-110是Arvinas在蛋白降解靶向嵌合体领域的全球首个进入临床试验的口服生物可利用的PRAOTC小分子药物，选择性靶向降解雄性激素受体 （AR） 。 在2019年5月ARV-110获得FDA快速通道批准，主要用于治疗患有转移性趋势抵抗性前列腺癌 （mCRPC） 。

Arvinas研发的第二代口服AR降解剂为ARV-766，与ARV-110相比，其基因型的覆盖面更广，立体化学稳定性更优。 最新的临床试验结果表明，ARV-766让42%带有AR配体结合域（LBD）突变的患者PSA水平降低了至少50%。