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Lead compound optimization strategy (9) - reducing drug clearance through structure modification
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Rui ZHANG1, 2, Jiang WANG1, 2, Hao-ran ZHU1, 2, Hong LIU1, 2, *
Acta Pharmaceutica Sinica | 2021, 56(11) : 3030 - 3046
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Acta Pharmaceutica Sinica | 2021, 56(11): 3030-3046
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Lead compound optimization strategy (9) - reducing drug clearance through structure modification
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Rui ZHANG1, 2, Jiang WANG1, 2, Hao-ran ZHU1, 2, Hong LIU1, 2, *
Affiliations
  • 1. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
  • 2. University of Chinese Academy of Sciences, Beijing 100049, China
Published: 2021-11-12 doi: 10.16438/j.0513-4870.2021-0866
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Clearance reflects the speed of extraction and elimination of drug molecules from systemic circulation. Reducing the clearance of compounds using structure modification strategy could lead to good pharmacokinetic and pharmacodynamic properties. Herein, the concept of clearance, as well as several prediction methods of in vivo clearance are introduced. The strategies of reducing drug clearance are reviewed. These methods include reducing hepatic metabolic clearance through reducing lipophilicity, blocking metabolic site, scaffold modification and increasing steric hindrance; reducing biliary or renal excretion clearance through increasing lipophilicity, reducing polar surface area and bioisosterism. In addition, the influence of spatial configuration on drug clearance is also summarized.

clearance  /  hepatic metabolism  /  excretion  /  lipophilicity  /  chiral configuration
Rui ZHANG, Jiang WANG, Hao-ran ZHU, Hong LIU. Lead compound optimization strategy (9) - reducing drug clearance through structure modification[J]. Acta Pharmaceutica Sinica, 2021 , 56 (11) : 3030 -3046 . DOI: 10.16438/j.0513-4870.2021-0866
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Year 2021 volume 56 Issue 11
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Article Info
doi: 10.16438/j.0513-4870.2021-0866
  • Receive Date：2021-06-15
  • Online Date：2025-12-18
  • Published：2021-11-12
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History
  • Received：2021-06-15
  • Revised：2021-07-12
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Affiliations
    1. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
    2. University of Chinese Academy of Sciences, Beijing 100049, China
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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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