Phase I/II trial of enzalutamide and mifepristone, a glucocorticoid receptor antagonist, for metastatic castration-resistant prostate cancer
AV Serritella, D Shevrin, EI Heath, JL Wade… - Clinical Cancer …, 2022 - AACR
… a phase I/II open label trial (NCT:02012296) of study of enzalutamide combined with mifepristone
to … on disease progression with dual AR and GR antagonism. The study started with a …
to … on disease progression with dual AR and GR antagonism. The study started with a …
A Phase I Trial of Enzalutamide Plus Selective Glucocorticoid Receptor Modulator Relacorilant in Patients with Metastatic Castration-Resistant Prostate Cancer
KB Desai, AV Serritella, WM Stadler, PH O'Donnell… - Clinical Cancer …, 2024 - AACR
… a phase I/II trial to determine whether continuous GR pathway inhibition with mifepristone
was … In our phase I/II mifepristone + enzalutamide trial, enzalutamide 120 mg/d in combination …
was … In our phase I/II mifepristone + enzalutamide trial, enzalutamide 120 mg/d in combination …
The dual androgen receptor and glucocorticoid receptor antagonist CB-03-10 as potential treatment for tumors that have acquired GR-mediated resistance to AR …
C Rosette, FJ Agan, N Rosette, A Mazzetti, L Moro… - Molecular Cancer …, 2020 - AACR
… trials (NCT03674814, NCT03437941). However, the initial result of a phase I/II trial with
combined mifepristone and enzalutamide in … A possible explanation is that mifepristone's GR …
combined mifepristone and enzalutamide in … A possible explanation is that mifepristone's GR …
Rational drug design for androgen receptor and glucocorticoids receptor dual antagonist
M Wu, Y Xie, X Cui, C Huang, R Zhang, Y He… - European Journal of …, 2019 - Elsevier
… The second-generation antiandrogen enzalutamide (ENZa) … of Z19 or positive control
mifepristone (Mif) for 24 h. Dual-… Mif is ongoing (NCT02012296, Phase I/II), and the detail data …
mifepristone (Mif) for 24 h. Dual-… Mif is ongoing (NCT02012296, Phase I/II), and the detail data …
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633)
X Du, J Eksterowicz, H Zhou, Y Rew… - Journal of Medicinal …, 2019 - ACS Publications
… of mifepristone (1) led to the discovery of novel mifepristone … on progesterone receptor (PR)
and androgen receptor (AR) … For example, the combinations of 1 with enzalutamide and nab-…
and androgen receptor (AR) … For example, the combinations of 1 with enzalutamide and nab-…
Synthesis of hydrocortisone esters targeting androgen and glucocorticoid receptors in prostate cancer in vitro
… Recently, the initial outcome of a phase I/II trial combining enzalutamide and mifepristone
in metastatic CRPC (NCT02012296) was published. The combination was safe and tolerable, …
in metastatic CRPC (NCT02012296) was published. The combination was safe and tolerable, …
[HTML][HTML] Second generation androgen receptor antagonists and challenges in prostate cancer treatment
Y Chen, Q Zhou, W Hankey, X Fang, F Yuan - Cell Death & Disease, 2022 - nature.com
… of the principal mechanisms of resistance to AR antagonists [23, 24, 41], a phase I/II clinical
trial for enzalutamide and the GR antagonist mifepristone in mCRPC (NCT02012296) has …
trial for enzalutamide and the GR antagonist mifepristone in mCRPC (NCT02012296) has …
[HTML][HTML] Androgen receptor signaling in prostate cancer and therapeutic strategies
… with enzalutamide in mCRPC in a phase I/II trial [66]. … Glucocorticoid receptor (GR) activation:
Enzalutamide resistance has … combined with mifepristone, a GR antagonist, in patients with …
Enzalutamide resistance has … combined with mifepristone, a GR antagonist, in patients with …
[HTML][HTML] Monitoring Glucocorticoid Receptor in Plasma-derived Extracellular Vesicles as a Marker of Resistance to Androgen Receptor Signaling Inhibition in Prostate …
… enzalutamide (ENZA) and mifepristone were purchased from MedChem Express LLC. …
In concordance with our findings, a randomized phase I/II trial of ENZA and mifepristone …
In concordance with our findings, a randomized phase I/II trial of ENZA and mifepristone …
Design and Synthesis of Dual-Target Inhibitors Targeting Androgen Receptors and Glucocorticoid Receptors to Overcome Antiandrogen Resistance in Castration …
C Li, X Han, Q Yan, Y Ji, R Zhang, D Yuan… - Journal of Medicinal …, 2024 - ACS Publications
… A clinical trial of the combination of mifepristone (Mif) and ENZa for the treatment of CRPC
… as current clinically used AR antagonists like enzalutamide, apalutamide, and darolutamide …
… as current clinically used AR antagonists like enzalutamide, apalutamide, and darolutamide …