scholarly journals Pharmacokinetics, Mass Balance, and Metabolism of the Novel URAT1 Inhibitor [14C]HR011303 in Humans: Metabolism is Mediated Predominantly by UDP-glucuronosyltransferase

2021 ◽  
pp. DMD-AR-2021-000581
Author(s):  
Yuandong Zheng ◽  
Hua Zhang ◽  
Mengling Liu ◽  
Guangze Li ◽  
Sheng Ma ◽  
...  
Keyword(s):  
Mass Balance ◽  
The Novel ◽  
Udp Glucuronosyltransferase

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.

1241 Mass balance study of the novel epothilone compound sagopilone in patients with advanced solid tumours

2009 ◽  
Vol 7 (2) ◽  
pp. 132-133
Author(s):  
C. Focan ◽  
F. Kreutz ◽  
N. Moeneclaey ◽  
S. Lindemann ◽  
S. Reif ◽  
...  
Keyword(s):  
Mass Balance ◽  
Solid Tumours ◽  
The Novel ◽  
Balance Study ◽  
Mass Balance Study

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

scholarly journals Human mass balance study of the novel anticancer agent ixabepilone using accelerator mass spectrometry

2007 ◽  
Vol 25 (4) ◽  
pp. 327-334 ◽  
Author(s):  
J. H. Beumer ◽  
R. C. Garner ◽  
M. B. Cohen ◽  
S. Galbraith ◽  
G. F. Duncan ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Mass Balance ◽  
Accelerator Mass Spectrometry ◽  
Anticancer Agent ◽  
The Novel ◽  
Balance Study ◽  
Mass Balance Study

The novel steroidal glycoside from the dried bulb of Allium Macrostemon Bunge inhibits platelet activation

2010 ◽  
Vol 34 (8) ◽  
pp. S33-S33
Author(s):  
Wenchao Ou ◽  
Haifeng Chen ◽  
Yun Zhong ◽  
Benrong Liu ◽  
Keji Chen
Keyword(s):  
Platelet Activation ◽  
The Novel ◽  
Steroidal Glycoside ◽  
Allium Macrostemon
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