Absorption, metabolism, and excretion of [C-14]YY-20394, a highly selective PI3K-Delta inhibitor in humans
文献类型：期刊论文
| 作者 | Yu, Jinghua2; Zhang, Hua1,3; Zhang, Yifan2 ; Zhan, Yan2; Ma, Sheng1,3; Hu, Tao2; Zhang, Ning2; Lou, Yangtong4; Bao, Hanying4; Xu, Zusheng4
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| 刊名 | XENOBIOTICA
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| 出版日期 | 2022-04-09 |
| 页码 | 11 |
| 关键词 | YY-20394 [C-14]YY-20394 mass balance drug metabolism pharmacokinetics |
| ISSN号 | 0049-8254 |
| DOI | 10.1080/00498254.2022.2062581 |
| 通讯作者 | Zhong, Dafang(dfzhong@simm.ac.cn) ; Miao, Liyan(miaoliyan@suda.edu.cn) ; Diao, Xingxing(xxdiao@simm.ac.cn) |
| 英文摘要 | YY-20394, a highly selective PI3K delta inhibitor, is under NDA submission for treating follicular lymphoma in China. The absorption, metabolism, and excretion of YY-20394 were evaluated in healthy Chinese male subjects following a single oral dose of 80 mg [C-14]YY-20394 (100 mu Ci). Within 264 h post-dose, 92.1% of the administered dose was recovered, with 58.1% from urine and 34.0% from faeces. YY-20394 was rapidly absorbed in humans, and the peak plasma concentrations occurred at 1.0 h. The absorbed drug fraction was at least 58.1% according to urine recovery. In addition to the parent drug, nine metabolites were identified in plasma, urine, and faeces. Unchanged YY-20394 was the predominant drug-related component in plasma (accounting for 68.4% of the total radioactivity), urine (accounting for 90.0% of the urinary radioactivity) and faeces (accounting for 41.7% of the faecal radioactivity). In humans, the major metabolic sites were the morphine ring and side chains of piperidine rings. The major metabolic pathways involved N-dealkylation, O-dealkylation, glucuronidation and acetylation. Overall, renal elimination played a significant role in the disposition of YY-20394, and the morphine ring and the side chain of the piperidine ring was the predominant metabolic sites. |
| WOS关键词 | UDP-GLUCURONOSYLTRANSFERASE ACTIVITY ; MASS-BALANCE ; PI3K INHIBITOR ; IDELALISIB |
| 资助项目 | Shanghai Yingli Pharmaceutical Co., Ltd. ; National Natural Science Foundation of China[81903701] |
| WOS研究方向 | Pharmacology & Pharmacy ; Toxicology |
| 语种 | 英语 |
| WOS记录号 | WOS:000780809200001 |
| 出版者 | TAYLOR & FRANCIS LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/299842]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Zhong, Dafang; Miao, Liyan; Diao, Xingxing |
| 作者单位 | 1.Soochow Univ, Inst Interdisciplinary Drug Res & Translat Sci, Suzhou, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China 3.Soochow Univ, Dept Pharmacol, Affiliated Hosp 1, Suzhou 215006, Peoples R China 4.Shanghai Yingli Pharmaceut Co Ltd, Shanghai, Peoples R China |
| 推荐引用方式 GB/T 7714 | Yu, Jinghua,Zhang, Hua,Zhang, Yifan,et al. Absorption, metabolism, and excretion of [C-14]YY-20394, a highly selective PI3K-Delta inhibitor in humans[J]. XENOBIOTICA,2022:11. |
| APA | Yu, Jinghua.,Zhang, Hua.,Zhang, Yifan.,Zhan, Yan.,Ma, Sheng.,...&Diao, Xingxing.(2022).Absorption, metabolism, and excretion of [C-14]YY-20394, a highly selective PI3K-Delta inhibitor in humans.XENOBIOTICA,11. |
| MLA | Yu, Jinghua,et al."Absorption, metabolism, and excretion of [C-14]YY-20394, a highly selective PI3K-Delta inhibitor in humans".XENOBIOTICA (2022):11. |
入库方式： OAI收割
来源：上海药物研究所
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