THRX » Topics » Multivalency

These excerpts taken from the THRX 10-K filed Feb 27, 2009.

Multivalency

        Our proprietary approach combines chemistry and biology to efficiently discover new product candidates using our expertise in multivalency. Multivalency refers to the simultaneous attachment of a single molecule to multiple binding sites on one or more biological targets. When compared to monovalency, whereby a molecule attaches to only one binding site, multivalency can significantly increase a compound's potency, duration of action and/or selectivity. Multivalent compounds generally consist of several individual small molecules, at least one of which is biologically active when bound to its target, joined by linking components.

        Our approach is based on an integration of the following insights:

    Many targets have multiple binding sites and/or exist in clusters with similar or different targets;

    Biological targets with multiple binding sites and/or those that exist in clusters lend themselves to multivalent drug design;

    Molecules that simultaneously attach to multiple binding sites can exhibit considerably greater potency, duration of action and/or selectivity than molecules that attach to only one binding site; and

    Greater potency, duration of action and/or selectivity provides the basis for superior therapeutic effects, including enhanced convenience, tolerability and/or safety compared to conventional drugs.

8


Table of Contents

Multivalency



        Our proprietary approach combines chemistry and biology to efficiently discover new product candidates using our expertise in
multivalency. Multivalency refers to the simultaneous attachment of a single molecule to multiple binding sites on one or more biological targets. When compared to monovalency, whereby a molecule
attaches to only one binding site, multivalency can significantly increase a compound's potency, duration of action and/or selectivity. Multivalent compounds generally consist of several individual
small molecules, at least one of which is biologically active when bound to its target, joined by linking components.



        Our
approach is based on an integration of the following insights:





    Many targets have multiple binding sites and/or exist in clusters with similar or different targets;


    Biological targets with multiple binding sites and/or those that exist in clusters lend themselves to multivalent drug
    design;



    Molecules that simultaneously attach to multiple binding sites can exhibit considerably greater potency, duration of
    action and/or selectivity than molecules that attach to only one binding site; and



    Greater potency, duration of action and/or selectivity provides the basis for superior therapeutic effects, including
    enhanced convenience, tolerability and/or safety compared to conventional drugs.


8









HREF="#bg70301a_main_toc">Table of Contents








These excerpts taken from the THRX 10-K filed Feb 27, 2008.

Multivalency

        Our proprietary approach combines chemistry and biology to efficiently discover new product candidates using our expertise in multivalency. Multivalency refers to the simultaneous attachment of a single molecule to multiple binding sites on one or more biological targets. When compared to monovalency, whereby a molecule attaches to only one binding site, multivalency can significantly increase a compound's potency, duration of action and/or selectivity. Multivalent compounds generally consist of several individual small molecules, at least one of which is biologically active when bound to its target, joined by linking components.

        Our approach is based on an integration of the following insights:

    Many targets have multiple binding sites and/or exist in clusters with similar or different targets;

    Biological targets with multiple binding sites and/or those that exist in clusters lend themselves to multivalent drug design;

    Molecules that simultaneously attach to multiple binding sites can exhibit considerably greater potency, duration of action and/or selectivity than molecules that attach to only one binding site; and

    Greater potency, duration of action and/or selectivity provides the basis for superior therapeutic effects, including enhanced convenience, tolerability and/or safety compared to conventional drugs.

12


Multivalency



        Our proprietary approach combines chemistry and biology to efficiently discover new product candidates using our expertise in multivalency. Multivalency refers to
the simultaneous attachment of a single molecule to multiple binding sites on one or more biological targets. When compared to monovalency, whereby a molecule attaches to only one binding site,
multivalency can significantly increase a compound's potency, duration of action and/or selectivity. Multivalent compounds generally consist of several individual small molecules, at least one of
which is biologically active when bound to its target, joined by linking components.




        Our
approach is based on an integration of the following insights:





    Many
    targets have multiple binding sites and/or exist in clusters with similar or different targets;


    Biological
    targets with multiple binding sites and/or those that exist in clusters lend themselves to multivalent drug design;


    Molecules
    that simultaneously attach to multiple binding sites can exhibit considerably greater potency, duration of action and/or selectivity than molecules that attach to
    only one binding site; and


    Greater
    potency, duration of action and/or selectivity provides the basis for superior therapeutic effects, including enhanced convenience, tolerability and/or safety
    compared to conventional drugs.


12













This excerpt taken from the THRX 10-K filed Mar 1, 2007.

Multivalency

Our proprietary approach combines chemistry and biology to efficiently discover new product candidates for validated targets using our expertise in multivalency. Multivalency refers to the simultaneous attachment of a single molecule to multiple binding sites on one or more biological targets. When compared to monovalency, whereby a molecule attaches to only one binding site, multivalency can significantly increase a compound’s potency, duration of action and/or selectivity. Multivalent compounds generally consist of several individual small molecules, at least one of which is biologically active when bound to its target, joined by linking components.

Our approach is based on an integration of the following insights:

·       Many targets have multiple binding sites and/or exist in clusters with similar or different targets;

·       Biological targets with multiple binding sites and/or those that exist in clusters lend themselves to multivalent drug design;

·       Molecules that simultaneously attach to multiple binding sites can exhibit considerably greater potency, duration of action and/or selectivity than molecules that attach to only one binding site; and

·       Greater potency, duration of action and/or selectivity provides the basis for superior therapeutic effects, including enhanced convenience, tolerability and/or safety compared to conventional drugs.

11




This excerpt taken from the THRX 10-K filed Mar 10, 2006.
Multivalency

Our proprietary approach combines chemistry and biology to efficiently discover new product candidates for validated targets using our expertise in multivalency. Multivalency refers to the simultaneous attachment of a single molecule to multiple binding sites on one or more biological targets.

10




When compared to monovalency, whereby a molecule attaches to only one binding site, multivalency can significantly increase a compound’s potency, duration of action and/or selectivity. Multivalent compounds generally consist of several individual small molecules, at least one of which is biologically active when bound to its target, joined by linking components.

Our approach is based on an integration of the following insights:

·  Many targets have multiple binding sites and/or exist in clusters with similar or different targets;

·  Biological targets with multiple binding sites and/or those that exist in clusters lend themselves to multivalent drug design;

·  Molecules that simultaneously attach to multiple binding sites can exhibit considerably greater potency, duration of action and/or selectivity than molecules that attach to only one binding site; and

·  Greater potency, duration of action and/or selectivity provides the basis for superior therapeutic effects, including enhanced convenience, tolerability and/or safety compared to conventional drugs.

This excerpt taken from the THRX 10-K filed Mar 8, 2006.
Multivalency

Our proprietary approach combines chemistry and biology to efficiently discover new product candidates for validated targets using our expertise in multivalency. Multivalency refers to the simultaneous attachment of a single molecule to multiple binding sites on one or more biological targets. When compared to monovalency, whereby a molecule attaches to only one binding site, multivalency can significantly increase a compound’s potency, duration of action and/or selectivity. Multivalent compounds generally consist of several individual small molecules, at least one of which is biologically active when bound to its target, joined by linking components.

Our approach is based on an integration of the following insights:

·  Many targets have multiple binding sites and/or exist in clusters with similar or different targets;

·  Biological targets with multiple binding sites and/or those that exist in clusters lend themselves to multivalent drug design;

·  Molecules that simultaneously attach to multiple binding sites can exhibit considerably greater potency, duration of action and/or selectivity than molecules that attach to only one binding site; and

·  Greater potency, duration of action and/or selectivity provides the basis for superior therapeutic effects, including enhanced convenience, tolerability and/or safety compared to conventional drugs.

This excerpt taken from the THRX 10-K filed Mar 29, 2005.
Multivalency

Our proprietary approach combines chemistry and biology to efficiently discover new product candidates for validated targets using our expertise in multivalency. Multivalency refers to the simultaneous attachment of a single molecule to multiple binding sites on one or more biological targets. When compared to monovalency, whereby a molecule attaches to only one binding site, multivalency can significantly increase a compound’s potency, duration of action and/or selectivity. Multivalent compounds generally consist of several individual small molecules, at least one of which is biologically active when bound to its target, joined by linking components.

Our approach is based on an integration of the following insights:

·       Many targets have multiple binding sites and/or exist in clusters with similar or different targets;

·       Biological targets with multiple binding sites and/or those that exist in clusters lend themselves to multivalent drug design;

·       Molecules that simultaneously attach to multiple binding sites can exhibit considerably greater potency, duration of action and/or selectivity than molecules that attach to only one binding site; and

·       Greater potency, duration of action and/or selectivity provides the basis for superior therapeutic effects, including enhanced convenience, tolerability and/or safety compared to conventional drugs.

15




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