scholarly journals Metabolism and Mass Balance of the Novel Nonsteroidal Androgen Receptor Inhibitor Darolutamide in Humans

2021 ◽  
pp. DMD-AR-2020-000309
Author(s):  
Päivi Taavitsainen ◽  
Olaf Prien ◽  
Marja Kähkönen ◽  
Michael Niehues ◽  
Timo Korjamo ◽  
...  
Keyword(s):  
Androgen Receptor ◽  
Mass Balance ◽  
The Novel ◽  
Receptor Inhibitor

Clascoterone: How the Novel Androgen Receptor Inhibitor Fits Into the Acne Treatment Paradigm

2021 ◽  
pp. 106002802199205
Author(s):  
Caitlin G. Purvis ◽  
Esther A. Balogh ◽  
Steven R. Feldman
Keyword(s):  
Androgen Receptor ◽  
Treatment Outcomes ◽  
Real Life ◽  
Poor Adherence ◽  
The Novel ◽  
Treatment Paradigm ◽  
Acne Treatment ◽  
Topical Treatments ◽  
Receptor Inhibitor

Many patients with acne remain unsatisfied with results from the various topical treatments available and often do not improve, because of poor adherence. Even if topical clascoterone, a safe and effective treatment, were more potent than existing topicals, it could face the same poor adherence hurdle as existing treatments. Real-life efficacy will likely not reflect trial results because, for several reasons, adherence is better in trials than in real-life practice. Although topical clascoterone may be exciting initially for its promise to improve acne outcomes, the long-term place in therapy may be another topical option that minimally enhances patients’ treatment outcomes.

Targeting enzalutamide-resistant prostate cancer using the novel androgen receptor inhibitor ODM-201

2017 ◽  
Vol 16 (3) ◽  
pp. e1290 ◽  
Author(s):  
H. Borgmann ◽  
D. Ozistanbullu ◽  
E. Beraldi ◽  
K. Dalal ◽  
L. Fazli ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Androgen Receptor ◽  
The Novel ◽  
Receptor Inhibitor

scholarly journals MP79-04 THE PRECLINICAL CHARACTERIZATION AND DEVELOPMENT OF EPI-7386, AN N-TERMINAL DOMAIN ANDROGEN RECEPTOR INHIBITOR, FOR THE TREATMENT OF PROSTATE CANCER

2020 ◽  
Vol 203 ◽  
pp. e1216
Author(s):  
Ronan Le Moigne* ◽  
C. Adriana Banuelos ◽  
Nasrin R. Mawji ◽  
Teresa Tam ◽  
Jun Wang ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Androgen Receptor ◽  
Terminal Domain ◽  
Receptor Inhibitor

scholarly journals The novel Aryl hydrocarbon receptor inhibitor biseugenol inhibits gastric tumor growth and peritoneal dissemination

Oncotarget ◽  
2014 ◽  
Vol 5 (17) ◽  
pp. 7788-7804 ◽  
Author(s):  
De-Wei Lai ◽  
Shing-Hwa Liu ◽  
Anna Isabella Karlsson ◽  
Wen-Jane Lee ◽  
Keh-Bin Wang ◽  
...  
Keyword(s):  
Tumor Growth ◽  
Aryl Hydrocarbon Receptor ◽  
Peritoneal Dissemination ◽  
Gastric Tumor ◽  
The Novel ◽  
Aryl Hydrocarbon ◽  
Receptor Inhibitor

scholarly journals Phase I Study of Seviteronel, a Selective CYP17 Lyase and Androgen Receptor Inhibitor, in Men with Castration-Resistant Prostate Cancer

2018 ◽  
Vol 24 (21) ◽  
pp. 5225-5232 ◽  
Author(s):  
Shilpa Gupta ◽  
Luke T. Nordquist ◽  
Mark T. Fleming ◽  
William R. Berry ◽  
Jingsong Zhang ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Androgen Receptor ◽  
Phase I ◽  
Phase I Study ◽  
Castration Resistant Prostate Cancer ◽  
Castration Resistant ◽  
Receptor Inhibitor

scholarly journals Mass balance and metabolite profiling of 14C-guadecitabine in patients with advanced cancer

2019 ◽  
Vol 38 (4) ◽  
pp. 1085-1095
Author(s):  
Jeroen Roosendaal ◽  
Hilde Rosing ◽  
Luc Lucas ◽  
Abadi Gebretensae ◽  
Alwin D. R. Huitema ◽  
...  
Keyword(s):  
Mass Balance ◽  
Mononuclear Cells ◽  
Drug Product ◽  
Systemic Circulation ◽  
Target Site ◽  
The Novel ◽  
Peripheral Blood Mononuclear ◽  
Once Daily ◽  
Phosphodiester Bond ◽  
Intracellular Target

Summary Purpose The objective of this mass balance trial was to determine the excretory pathways and metabolic profile of the novel anticancer agent guadecitabine in humans after administration of a 14C-radiolabeled dose of guadecitabine. Experimental design Included patients received at least one cycle of 45 mg/m2 guadecitabine subcutaneously as once-daily doses on Days 1 to 5 of a 28-day cycle, of which the 5th (last) dose in the first cycle was spiked with 14C-radiolabeled guadecitabine. Using different mass spectrometric techniques in combination with off-line liquid scintillation counting, the exposure and excretion of 14C-guadecitabine and metabolites in the systemic circulation, excreta, and intracellular target site were established. Results Five patients were enrolled in the mass balance trial. 14C-guadecitabine radioactivity was rapidly and almost exclusively excreted in urine, with an average amount of radioactivity recovered of 90.2%. After uptake in the systemic circulation, guadecitabine was converted into ß-decitabine (active anomer), and from ß-decitabine into the presumably inactive metabolites M1-M5. All identified metabolites in plasma and urine were ß-decitabine related products, suggesting almost complete conversion via cleavage of the phosphodiester bond between ß-decitabine and deoxyguanosine prior to further elimination. ß-decitabine enters the intracellular activation pathway, leading to detectable ß-decitabine-triphosphate and DNA incorporated ß-decitabine levels in peripheral blood mononuclear cells, providing confirmation that the drug reaches its DNA target site. Conclusion The metabolic and excretory pathways of guadecitabine and its metabolites were successfully characterized after subcutaneous guadecitabine administration in cancer patients. These data support the clinical evaluation of safety and efficacy of the subcutaneous guadecitabine drug product.

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