[PDF][PDF] ARV-110: An oral androgen receptor PROTAC degrader for prostate cancer

T Neklesa, LB Snyder, RR Willard… - J. Clin …, 2019 - s3.us-east-1.amazonaws.com
… Conclusions: In summary, we report preclinical data on an orally bioavailable AR PROTAC
degrader, ARV-110, that demonstrates efficacy in multiple prostate cancer models. ARV-110 …

[PDF][PDF] ARV-330: Androgen receptor PROTAC degrader for prostate cancer

TK Neklesa, M Jin, AP Crew, AK Rossi… - J. Clin …, 2016 - s3.us-east-1.amazonaws.com
… of tumor growth. In summary, the AR PROTAC ARV-330 removes AR from prostate cancer
… efficacious therapy for patients with prostate cancer for whom current therapies have failed. …

PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer

K Raina, J Lu, Y Qian, M Altieri… - Proceedings of the …, 2016 - National Acad Sciences
… , the disease often progresses to castration-resistant prostate cancer (CRPC), which is still
… molecule pan-BET degrader based on proteolysis-targeting chimera (PROTAC) technology, …

[PDF][PDF] An oral androgen receptor PROTAC degrader for prostate cancer

TK Neklesa, LB Snyder, M Bookbinder, X Chen… - J. Clin. Oncol, 2017 - arvinas.com
… data on an orally bioavailable AR PROTAC degrader ARV-110 that demonstrates efficacy
in enzalutamideresistant prostate cancer. PROTAC: PROteolysis TArgeting Chimera …

Discovery of ARD-2585 as an exceptionally potent and orally active PROTAC degrader of androgen receptor for the treatment of advanced prostate cancer

W Xiang, L Zhao, X Han, C Qin, B Miao… - Journal of medicinal …, 2021 - ACS Publications
… In order to induce AR degradation most effectively, a PROTAC AR degrader needs to
form a … restriction of the linker in an AR PROTAC degrader may lead to a more stable and …

Phase 1/2 study of ARV-110, an androgen receptor (AR) PROTAC degrader, in metastatic castration-resistant prostate cancer (mCRPC).

X Gao, HA Burris III, J Vuky, R Dreicer, AO Sartor… - 2022 - ascopubs.org
… oral PROteolysis TArgeting Chimera (PROTAC) protein degrader that selectively targets AR…
, 2) AR L702H mutation or AR-V7 (variants not degraded by ARV-110 in nonclinical studies), …

Discovery of ARD-69 as a highly potent proteolysis targeting chimera (PROTAC) degrader of androgen receptor (AR) for the treatment of prostate cancer

X Han, C Wang, C Qin, W Xiang… - Journal of medicinal …, 2019 - ACS Publications
PROTAC degraders of androgen receptor (AR), as exemplified by compound 34 (ARD-69).
ARD-69 induces degradation of AR protein in AR-positive prostate cancer … + prostate cancer

[HTML][HTML] Treatment of prostate cancers and kennedy's disease by PROTAC-androgen receptor degradation

RB Kargbo - ACS Medicinal Chemistry Letters, 2019 - ACS Publications
… a disease condition such as prostate cancer and Kennedy’s Disease. The first targeted protein
degrader (Arv-110, an orally bioavailable small molecule AR PROTAC) has been cleared …

… I study of ARV-110, an androgen receptor (AR) PROTAC degrader in patients (pts) with metastatic castrate-resistant prostate cancer (mCRPC) following enzalutamide …

DP Petrylak, X Gao, NJ Vogelzang, MH Garfield… - 2020 - ascopubs.org
… Background: Proteolysis Targeting Chimera (PROTAC) … PROTAC that specifically degrades
AR ≥ 95% and achieves anti-tumor activity in ENZ-naïve and -resistant prostate cancer

[PDF][PDF] Discovery of ARV-110, a first in class androgen receptor degrading PROTAC for the treatment of men with metastatic castration resistant prostate cancer

LB Snyder, TK Neklesa, X Chen, H Dong… - Cancer …, 2021 - s3.us-east-1.amazonaws.com
This presentation contains forward-looking statements within the meaning of The Private
Securities Litigation Reform Act of 1995 that involve substantial risks and uncertainties, …