carcinoma xenograft
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2022 ◽  
pp. 174753
Author(s):  
Surachai Maijaroen ◽  
Sompong Klaynongsruang ◽  
Somrudee Reabroi ◽  
Arthit Chairoungdua ◽  
Sittiruk Roytrakul ◽  
...  

Pharmaceutics ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 598
Author(s):  
Yuchen Wang ◽  
Xiao Liu ◽  
Xiaowen Zou ◽  
Shuting Wang ◽  
Lijun Luo ◽  
...  

IMMH-010 is an ester prodrug of YPD-29B, a potent programmed cell death ligand 1 (PD-L1) inhibitor. The metabolism of IMMH-010 was investigated and compared in various species. Four metabolites of IMMH-010 were identified, and the major metabolite was the parent compound, YPD-29B, which was mainly catalyzed by carboxylesterase 1 (CES1). We observed IMMH-010 metabolism in the plasma of various species. IMMH-010 was rapidly metabolized to YPD-29B in rat and mouse plasma, whereas it remained stable in human and monkey plasma. In the liver S9 fractions of human, monkey, dog, and rat, IMMH-010 was quickly transformed to YPD-29B with no obvious differences among species. In addition, the transformation ratio of IMMH-010 to YPD-29B was low in rat and human intestines, which indicated that the intestine was not an important site for IMMH-010 hydrolysis. Moreover, we demonstrated the remarkable antitumor efficacy of IMMH-010 in B16F10 melanoma and MC38 colon carcinoma xenograft mouse models. We also compared the pharmacokinetic profiles of IMMH-010 in rodents and primates. After oral administration of IMMH-010, the general exposure of active metabolite YPD-29B was slightly lower in primates than in rodents, suggesting that data should be extrapolated cautiously from rodents to humans.


Author(s):  
Thi-Thu Nguyen ◽  
Anh-Son Ho ◽  
Thi-Khanh-Giang Nguyen ◽  
Thi-Ngoc Nguyen ◽  
Van-Cuong Bui ◽  
...  

2021 ◽  
Vol 38 (3) ◽  
Author(s):  
Baofu Zhang ◽  
Huizhong Li ◽  
Wenbin Liu ◽  
Hui Tian ◽  
Liantao Li ◽  
...  

2020 ◽  
Vol 223 ◽  
pp. 33-43
Author(s):  
Yuwei Wu ◽  
Jinyu Wang ◽  
Xiaodong Zheng ◽  
Yongyan Chen ◽  
Mei Huang ◽  
...  

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