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A physiologically-based pharmacokinetic model adequately predicted the human pharmacokinetic profiles of ZSP1601, a novel pan-phosphodiesterase inhibitor
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Yi-fan ZHANG1, Ye XU1, Hai-jun LI2, Xiao-xin CHEN2, Song-bo XU2, Jia LIU1, Zhi-jie WANG1, Da-fang ZHONG1, *
Acta Pharmaceutica Sinica | 2021, 56(12) : 3540 - 3546
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Acta Pharmaceutica Sinica | 2021, 56(12): 3540-3546
• Original Articles •
A physiologically-based pharmacokinetic model adequately predicted the human pharmacokinetic profiles of ZSP1601, a novel pan-phosphodiesterase inhibitor
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Yi-fan ZHANG1, Ye XU1, Hai-jun LI2, Xiao-xin CHEN2, Song-bo XU2, Jia LIU1, Zhi-jie WANG1, Da-fang ZHONG1, *
Affiliations
  • 1. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
  • 2. Guangdong Raynovent Biotech Co., Ltd., Guangzhou 510663, China
Published: 2021-12-12 doi: 10.16438/j.0513-4870.2021-1024
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ZSP1601, a novel pan-phosphodiesterase inhibitor is in development for the treatment of nonalcoholic steatohepatitis. A physiologically-based pharmacokinetic (PBPK) model was developed to predict the pharmacokinetics of ZSP1601 in human. The PBPK model following intravenous and oral dose of ZSP1601 in rats and dogs was firstly built using preclinical in vitro and in vivo data. The PBPK model in human was then built based on models in animal. The in vitro-in vivo extrapolation (IVIVE) method and some allometric scaling methods were used to predict the clearance in human, respectively. The PBPK models using IVIVE and allometry of unbound CL plus the rule of exponents methods predicted the pharmacokinetics of ZSP1601 in healthy Chinese subjects successfully. The predicted parameters Cmax and AUC following single oral dose administration were within 0.5-2 folds of the observed data. The model was optimized and the final model was used to predict the pharmacokinetics of ZSP1601 in North European Caucasian, Geriatrics, Obese and Morbidly Obese, respectively. Animal studies were approved by the Animal Management and Use Committee of Suzhou AppTec Inc., and the approved No. is SZ20140916.

physiologically-based pharmacokinetic model  /  pan-phosphodiesterase inhibitor  /  nonalcoholic steatohepatitis  /  clinical pharmacokinetics
Yi-fan ZHANG, Ye XU, Hai-jun LI, Xiao-xin CHEN, Song-bo XU, Jia LIU, Zhi-jie WANG, Da-fang ZHONG. A physiologically-based pharmacokinetic model adequately predicted the human pharmacokinetic profiles of ZSP1601, a novel pan-phosphodiesterase inhibitor[J]. Acta Pharmaceutica Sinica, 2021 , 56 (12) : 3540 -3546 . DOI: 10.16438/j.0513-4870.2021-1024
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Year 2021 volume 56 Issue 12
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Article Info
doi: 10.16438/j.0513-4870.2021-1024
  • Receive Date：2021-07-09
  • Online Date：2025-12-18
  • Published：2021-12-12
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History
  • Received：2021-07-09
  • Revised：2021-10-09
Funding
Affiliations
    1. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
    2. Guangdong Raynovent Biotech Co., Ltd., Guangzhou 510663, China
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表12种不同金属材料的力学参数
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Family		 属数
Number of
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Number of
species		 占总种数比例
Percentage of
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Genus		 种数
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鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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