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    Dr. Apt. Yudi Wicaksono, S.Si., M.Si

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    Nurul Fathonaa
    The document discusses prodrugs, which are biologically inert derivatives of drug molecules that undergo conversion in the body to release the active pharmaceutical ingredient. Prodrugs can be designed to improve the pharmacokinetic properties and decrease the toxicity of a drug candidate by temporarily attaching a promoiety that is cleaved enzymatically or chemically to release the active drug. The document covers the history, classification, design process, and types of prodrugs, including carrier-linked and bioprecursor prodrugs.

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    Dr. Apt. Yudi Wicaksono, S.Si., M.Si

    Uploaded by

    Nurul Fathonaa
    27 views22 pages
    The document discusses prodrugs, which are biologically inert derivatives of drug molecules that undergo conversion in the body to release the active pharmaceutical ingredient. Prodrugs can be designed to improve the pharmacokinetic properties and decrease the toxicity of a drug candidate by temporarily attaching a promoiety that is cleaved enzymatically or chemically to release the active drug. The document covers the history, classification, design process, and types of prodrugs, including carrier-linked and bioprecursor prodrugs.

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    The document discusses prodrugs, which are biologically inert derivatives of drug molecules that undergo conversion in the body to release the active pharmaceutical ingredient. Prodrugs can be designed to improve the pharmacokinetic properties and decrease the toxicity of a drug candidate by temporarily attaching a promoiety that is cleaved enzymatically or chemically to release the active drug. The document covers the history, classification, design process, and types of prodrugs, including carrier-linked and bioprecursor prodrugs.

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    27 views22 pages

    Dr. Apt. Yudi Wicaksono, S.Si., M.Si

    Uploaded by

    Nurul Fathonaa
    The document discusses prodrugs, which are biologically inert derivatives of drug molecules that undergo conversion in the body to release the active pharmaceutical ingredient. Prodrugs can be designed to improve the pharmacokinetic properties and decrease the toxicity of a drug candidate by temporarily attaching a promoiety that is cleaved enzymatically or chemically to release the active drug. The document covers the history, classification, design process, and types of prodrugs, including carrier-linked and bioprecursor prodrugs.

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    4/1/2023

    Dr. apt. Yudi Wicaksono, S.Si., M.Si.

     Hampir semua obat memiliki sifat-sifat


    fisikokimia dan biologis yang tidak diinginkan.
     Calon obat seringkali tidak dilanjutkan
    pengembangannya karena masalah sifat
    farmakokinetik rendah atau toksisitas tinggi
     Efek teraputik obat-obat tersebut dapat
    ditingkatkan dengan menghilangkan sifat yang
    tidak diinginkan dan mempertahankan sifat
    yang diharapkan

    → dapat dilakukan melalui cara biologis, fisik atau


    kimia.

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    4/1/2023

    Prodrug
    “Biologically inert derivatives of drug molecules that
    undergo an enzymatic and/or chemical conversion in
    vivo to release the pharmacologically active parent
    drug.” (Adrien Albert, 1958)

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    Prodrug Vs. Drug

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    History of Prodrugs

    PRODRUG CONCEPT

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     The drug–promoiety is the prodrug that is typically


    pharmacologically inactive.

     The drug and promoiety are covalently linked via


    bioreversible groups that are chemically or
    enzymatically labile

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    Limitation Of Prodrug:

    Biotransformation (Metabolism)
    of Drugs in the body

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    Steps in Prodrug Design


     Identification of drug delivery problem

     Identification of desired physicochemical properties

     Selection of transport moiety which will give prodrug


    desired transport properties be readily cleaved in the
    desired biological compartment

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    Classification of Prodrugs
     Based on therapeutic categories
     Based on the site of conversion
     Based on the structure

    Classification based on therapeutic categories


     Anticancer prodrugs
     Antiviral prodrugs
     Antibacterial prodrugs
     Nonsteroidal anti-inflammatory
    prodrugs
     Cardiovascular prodrugs

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    Classification based on the site of conversion

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    *ADEP/GDEP/VDEP = antibody-, gene- or virus-directed enzyme prodrugs

    Classification based on the structure

    A.Carrier linked prodrug (Bipartite,


    Tripartite, and Mutual Prodrugs)

    B. Bioprecursors

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    A. Carrier linked prodrug


     Carrier linked prodrug consists of the attachment of a
    carrier group to the active drug to alter its physicochemical
    properties.

    The subsequent enzymatic or non-enzymatic mechanism


    releases the active drug moiety.

    Carrier linked prodrug :

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    A1. Bipartite prodrug

    A.2 Tripartite prodrug


     The carrier group is attached via linker to
    drug.

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    A.3 Mutual prodrugs


     A mutual prodrug consists of two pharmacologically
    active agents coupled together so that each acts as a
    promoiety for the other agent and vice versa.
     A mutual prodrug is a bipartite or tripartite prodrug in
    which the carrier is a synergistic drug with the drug to
    which it is linked.
     Ex. : Benorylate is a mutual prodrug aspirin and
    paracetamol.

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    Mutual prodrug:

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    B. Bioprecursors
     Bioprecursor prodrugs produce their effects after in
    vivo chemical modification of their inactive form.
     Bioprecursor prodrugs rely on oxidative or reductive
    activation reactions unlike the hydrolytic activation of
    carrier-linked prodrugs.
     They metabolized into a new compound that may
    itself be active or further metabolized to an active
    metabolite.

    Bioprecursors

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