Investigation of absorption, metabolism, and excretion of [ <sup>14</sup> C]pruxelutamide (GT0918), an androgen receptor antagonist in humans
Overall, all the dosed subjects completed the study, and GT0918 was found to be safe, with no grade II or above adverse events reported. A total dose of 82.81% was quantified in the urine (29.47%) and faeces (53.34%) of healthy adult male subjects after a single oral administration of 200 mg (80 μCi) GT0918 ([<sup>14</sup>C]GT0918). The metabolism of GT0918 is catalysed predominantly by CYP3A4, and an uncommon pathway of oxazole ring-opening to an aldehyde intermediate has also been proposed.
Authors
- Yuandong Zheng (ORCID: https://orcid.org/0000-0002-8325-4318)
- Xingxing Diao (ORCID: https://orcid.org/0000-0002-7672-9952)
- Dingyong Zhong (ORCID: https://orcid.org/0000-0001-5650-4767)
- Feng‐zhi Ye
- Liyan Miao (ORCID: https://orcid.org/0000-0001-8481-0630)
- Yingguo Yang (ORCID: https://orcid.org/0000-0002-1749-2799)
- Yifei He (ORCID: https://orcid.org/0000-0003-3109-839X)
- Yali Yuan (ORCID: https://orcid.org/0000-0001-7819-2338)
- Jie Chen (ORCID: https://orcid.org/0000-0003-1230-6034)
- Yifan Zhang (ORCID: https://orcid.org/0000-0002-9164-8309)
- Hua Zhang (ORCID: https://orcid.org/0000-0003-4326-7875)
- Sheng Ma
- Meiyu Wang (ORCID: https://orcid.org/0000-0003-4294-0319)
- Yao Tong (ORCID: https://orcid.org/0000-0001-6573-859X)
- Tao Hu (ORCID: https://orcid.org/0000-0001-7893-096X)
Institutions
- Chinese Academy of Sciences (CN)
- Soochow University (CN)
- Shanghai Institute of Materia Medica (CN)
- First Affiliated Hospital of Soochow University (CN)
Publication Details
- Journal
- British Journal of Clinical Pharmacology
- Published
- 2025-02-23
- DOI
- https://doi.org/10.1002/bcp.70022
- Primary Topic
- Prostate Cancer Treatment and Research
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- National Natural Science Foundation of China