Maelicke_2010_J.Mol.Neurosci_40_135

Reference

Title : Memogain is a galantamine pro-drug having dramatically reduced adverse effects and enhanced efficacy - Maelicke_2010_J.Mol.Neurosci_40_135
Author(s) : Maelicke A , Hoeffle-Maas A , Ludwig J , Maus A , Samochocki M , Jordis U , Koepke AK
Ref : Journal of Molecular Neuroscience , 40 :135 , 2010
Abstract : Memogain (Gln-1062) is an inactive pro-drug of galantamine, the latter being a plant alkaloid approved for the treatment of mild to moderate Alzheimer's disease. Memogain has more than 15-fold higher bioavailability in the brain than the same doses of galantamine. In the brain, Memogain is enzymatically cleaved to galantamine, thereby regaining its pharmacological activity as a cholinergic enhancer. In animal models of drug-induced amnesia, Memogain produced several fold larger cognitive improvement than the same doses of galantamine, without exhibiting any significant levels of gastrointestinal side effects that are typical for the unmodified drug and other inhibitors of cholinesterases, such as donepezil and rivastigmin. In the ferret, dramatically reduced emetic and behavioral responses were observed when Memogain was administered instead of galantamine. Based on these and other preclinical data, Memogain may represent an advantageous drug treatment for Alzheimer's disease, combining much lesser gastrointestinal side effects and considerably higher potency in enhancing cognition, as compared to presently available drugs.
ESTHER : Maelicke_2010_J.Mol.Neurosci_40_135
PubMedSearch : Maelicke_2010_J.Mol.Neurosci_40_135
PubMedID: 19669943

Related information

Inhibitor Memogain
Substrate MemogainMemogain

Citations formats

Maelicke A, Hoeffle-Maas A, Ludwig J, Maus A, Samochocki M, Jordis U, Koepke AK (2010)
Memogain is a galantamine pro-drug having dramatically reduced adverse effects and enhanced efficacy
Journal of Molecular Neuroscience 40 :135

Maelicke A, Hoeffle-Maas A, Ludwig J, Maus A, Samochocki M, Jordis U, Koepke AK (2010)
Journal of Molecular Neuroscience 40 :135

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    [title] => Memogain is a galantamine pro-drug having dramatically reduced adverse effects and enhanced efficacy
    [journal] => Journal of Molecular Neuroscience
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            [content] => Memogain (Gln-1062) is an inactive pro-drug of galantamine, the latter being a plant alkaloid approved for the treatment of mild to moderate Alzheimer's disease. Memogain has more than 15-fold higher bioavailability in the brain than the same doses of galantamine. In the brain, Memogain is enzymatically cleaved to galantamine, thereby regaining its pharmacological activity as a cholinergic enhancer. In animal models of drug-induced amnesia, Memogain produced several fold larger cognitive improvement than the same doses of galantamine, without exhibiting any significant levels of gastrointestinal side effects that are typical for the unmodified drug and other inhibitors of cholinesterases, such as donepezil and rivastigmin. In the ferret, dramatically reduced emetic and behavioral responses were observed when Memogain was administered instead of galantamine. Based on these and other preclinical data, Memogain may represent an advantageous drug treatment for Alzheimer's disease, combining much lesser gastrointestinal side effects and considerably higher potency in enhancing cognition, as compared to presently available drugs.
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