Combination AZD5363 with enzalutamide significantly delays enzalutamide-resistant prostate cancer in preclinical models

P Toren, S Kim, T Cordonnier, C Crafter, BR Davies… - European urology, 2015 - Elsevier
Abstract The phosphatidylinositol-4, 5-bisphosphate 3-kinase/Akt (PI3K/Akt) pathway is a
key pathway activated in castrate-resistant prostate cancer (CRPC). This preclinical study …

Synergistic Targeting of PI3K/AKT Pathway and Androgen Receptor Axis Significantly Delays Castration-Resistant Prostate Cancer Progression In Vivo

C Thomas, F Lamoureux, C Crafter, BR Davies… - Molecular cancer …, 2013 - AACR
The progression to castration-resistant prostate cancer (CRPC) correlates with gain-of-
function of the androgen receptor (AR) and activation of AKT. However, as single agents, AR …

Enzalutamide, an androgen receptor signaling inhibitor, induces tumor regression in a mouse model of castration‐resistant prostate cancer

J Guerrero, IE Alfaro, F Gómez, AA Protter… - The …, 2013 - Wiley Online Library
BACKGROUND Enzalutamide (formerly MDV3100 and available commercially as Xtandi®),
a novel androgen receptor (AR) signaling inhibitor, blocks the growth of castration‐resistant …

[HTML][HTML] Combined AKT and MEK pathway blockade in pre-clinical models of enzalutamide-resistant prostate cancer

P Toren, S Kim, F Johnson, A Zoubeidi - PLoS One, 2016 - journals.plos.org
Despite recent improvements in patient outcomes using newer androgen receptor (AR)
pathway inhibitors, treatment resistance in castrate resistant prostate cancer (CRPC) …

Targeting the androgen receptor confers in vivo cross-resistance between enzalutamide and docetaxel, but not cabazitaxel, in castration-resistant prostate cancer

RJ Van Soest, ES de Morrée, CF Kweldam… - European urology, 2015 - Elsevier
Abstract Treatment options for metastatic castration-resistant prostate cancer (CRPC) have
evolved with the established benefit of the novel androgen receptor (AR)-targeted agents …

Enzalutamide: Development from bench to bedside

RM Bambury, HI Scher - Urologic Oncology: Seminars and Original …, 2015 - Elsevier
Prostate tissue, whether benign or malignant, is heavily dependent on androgen receptor
(AR) signaling for growth and proliferation. Androgen deprivation therapy has been standard …

AZD3514: A Small Molecule That Modulates Androgen Receptor Signaling and Function In Vitro and In Vivo

SA Loddick, SJ Ross, AG Thomason… - Molecular cancer …, 2013 - AACR
Continued androgen receptor (AR) expression and signaling is a key driver in castration-
resistant prostate cancer (CRPC) after classical androgen ablation therapies have failed …

[HTML][HTML] Reciprocal feedback inhibition of the androgen receptor and PI3K as a novel therapy for castrate-sensitive and-resistant prostate cancer

W Qi, C Morales, LS Cooke, B Johnson, B Somer… - Oncotarget, 2015 - ncbi.nlm.nih.gov
Gain-of-function of the androgen receptor (AR) and activation of PI3K/AKT/mTOR pathway
have been demonstrated to correlate with progression to castration-resistant prostate cancer …

Intracrine androgens and AKR1C3 activation confer resistance to enzalutamide in prostate cancer

C Liu, W Lou, Y Zhu, JC Yang, N Nadiminty… - Cancer research, 2015 - AACR
The introduction of enzalutamide and abiraterone has led to improvement in the treatment of
metastatic castration-resistant prostate cancer. However, acquired resistance to …

ASC-J9® suppresses castration resistant prostate cancer progression via degrading the enzalutamide-induced androgen receptor mutant AR-F876L

R Wang, W Lin, C Lin, L Li, Y Sun, C Chang - Cancer letters, 2016 - Elsevier
Androgen deprivation therapy (ADT) with the newly developed powerful anti-androgen
enzalutamide (Enz, also known as MDV3100) has promising therapeutic effects to suppress …