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Prodrug Approach: An Alternative to Improve Pharmacokinetic Properties

Received: 8 February 2019     Accepted: 11 March 2019     Published: 28 March 2019
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Abstract

Prodrugs are the masked forms of active drugs that are designed to be activated once they have been administered into the body by an enzymatic or chemical means. It is a well known molecular modification strategy that aims to optimize the physicochemical and pharmacological properties of drugs to improve their undesirable pharmacokinetic properties and decrease their toxicity. In most of the cases, prodrugs design involves the introduction of carrier/promoiety by a metabolic liable linkage so that after biotransformation by one or two chemical or enzymatic steps it will lead to the active parent drug. However, some prodrugs lack an obvious promoiety but instead result from a molecular modification of the prodrug itself, which generates a new active compound. This review introduces in depth the rationale behind the use of the promoiety, and also considers the possible problems that can arise from inadequate activation of prodrugs.

Published in International Journal of Bioorganic Chemistry (Volume 4, Issue 1)
DOI 10.11648/j.ijbc.20190401.12
Page(s) 7-13
Creative Commons

This is an Open Access article, distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution and reproduction in any medium or format, provided the original work is properly cited.

Copyright

Copyright © The Author(s), 2019. Published by Science Publishing Group

Keywords

Prodrug, Molecular Modification, Promoiety, Carrier-Linked

References
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    Ashwani Kumar Dhingra, Bhawna Chopra, Rameshwar Dass. (2019). Prodrug Approach: An Alternative to Improve Pharmacokinetic Properties. International Journal of Bioorganic Chemistry, 4(1), 7-13. https://doi.org/10.11648/j.ijbc.20190401.12

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    ACS Style

    Ashwani Kumar Dhingra; Bhawna Chopra; Rameshwar Dass. Prodrug Approach: An Alternative to Improve Pharmacokinetic Properties. Int. J. Bioorg. Chem. 2019, 4(1), 7-13. doi: 10.11648/j.ijbc.20190401.12

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    AMA Style

    Ashwani Kumar Dhingra, Bhawna Chopra, Rameshwar Dass. Prodrug Approach: An Alternative to Improve Pharmacokinetic Properties. Int J Bioorg Chem. 2019;4(1):7-13. doi: 10.11648/j.ijbc.20190401.12

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  • @article{10.11648/j.ijbc.20190401.12,
      author = {Ashwani Kumar Dhingra and Bhawna Chopra and Rameshwar Dass},
      title = {Prodrug Approach: An Alternative to Improve Pharmacokinetic Properties},
      journal = {International Journal of Bioorganic Chemistry},
      volume = {4},
      number = {1},
      pages = {7-13},
      doi = {10.11648/j.ijbc.20190401.12},
      url = {https://doi.org/10.11648/j.ijbc.20190401.12},
      eprint = {https://article.sciencepublishinggroup.com/pdf/10.11648.j.ijbc.20190401.12},
      abstract = {Prodrugs are the masked forms of active drugs that are designed to be activated once they have been administered into the body by an enzymatic or chemical means. It is a well known molecular modification strategy that aims to optimize the physicochemical and pharmacological properties of drugs to improve their undesirable pharmacokinetic properties and decrease their toxicity. In most of the cases, prodrugs design involves the introduction of carrier/promoiety by a metabolic liable linkage so that after biotransformation by one or two chemical or enzymatic steps it will lead to the active parent drug. However, some prodrugs lack an obvious promoiety but instead result from a molecular modification of the prodrug itself, which generates a new active compound. This review introduces in depth the rationale behind the use of the promoiety, and also considers the possible problems that can arise from inadequate activation of prodrugs.},
     year = {2019}
    }
    

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    AU  - Ashwani Kumar Dhingra
    AU  - Bhawna Chopra
    AU  - Rameshwar Dass
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    T2  - International Journal of Bioorganic Chemistry
    JF  - International Journal of Bioorganic Chemistry
    JO  - International Journal of Bioorganic Chemistry
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    AB  - Prodrugs are the masked forms of active drugs that are designed to be activated once they have been administered into the body by an enzymatic or chemical means. It is a well known molecular modification strategy that aims to optimize the physicochemical and pharmacological properties of drugs to improve their undesirable pharmacokinetic properties and decrease their toxicity. In most of the cases, prodrugs design involves the introduction of carrier/promoiety by a metabolic liable linkage so that after biotransformation by one or two chemical or enzymatic steps it will lead to the active parent drug. However, some prodrugs lack an obvious promoiety but instead result from a molecular modification of the prodrug itself, which generates a new active compound. This review introduces in depth the rationale behind the use of the promoiety, and also considers the possible problems that can arise from inadequate activation of prodrugs.
    VL  - 4
    IS  - 1
    ER  - 

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Author Information
  • Department of Pharmaceutical Sciences, Guru Gobind Singh College of Pharmacy, Yamuna Nagar, Haryana, India

  • Department of Pharmaceutical Sciences, Guru Gobind Singh College of Pharmacy, Yamuna Nagar, Haryana, India

  • Department of Pharmaceutical Sciences, Guru Gobind Singh College of Pharmacy, Yamuna Nagar, Haryana, India

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