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Important Notice: The Forum does not endorse any medical
product or therapy. ALL medications and supplements
should be taken ONLY under the supervision of a physician,
due to the possibility of side-effects, drug interactions,
etc.
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Name:
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Alzhemed™
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Other Names:
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3-amino-1-propanesulfonic acid, 3-aminopropylsulfonic acid, 3-APS, homotaurine, NC-531, Tramiprosate
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Therapeutic Applications:
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Mild to moderate Alzheimer disease
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Therapy Types:
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Oral, small molecule
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Mechanisms:
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Designed to cross the blood-brain barrier, tramiprosate is an amyloid-β antagonist.
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FDA Phase:
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Not FDA regulated
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Primary Medical Role:
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Tramiprosate has been proposed to inhibit amyloid
deposition.
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Role in Alzheimer's Disease:
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Tramiprosate was designed to prevent amyloid formation and
deposition in the brain, and thus modify the course of AD.
It has been tested extensively in clinical trials in both
the U.S. and the EU for mild to moderate AD. The recent
U.S. Phase 3 trial is widely considered to have failed
(see ARF related news story and comments). The EU
Phase 3 trial has been discontinued (see ARF
related news story). Recent published evidence
demonstrates that tramiprosate alters tau aggregation (see
Santa-Maria et
al., 2007 and comments and ARF
related news story).
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Pharmacological Role:
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Structurally, tramiprosate is a glycosaminoglycan (GAG)
mimetic designed to interfere with the actions of Aβ
early in the cascade of amyloidogenic events. Tramiprosate
is a modification of the amino acid taurine. It binds
preferentially to soluble Aβ peptide and maintains
Aβ in a non-fibrillar form, thereby inhibiting
amyloid formation and deposition. Tramiprosate interferes
with β-sheet formation of amyloid.
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Side Effects:
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The most frequent side effects were gastrointestinal,
including nausea, vomiting, and diarrhea, which were
intermittent and mild to moderate in severity.
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Evidence con its efficacy:
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Tramiprosate failed to demonstrate efficacy in long-term
clinical testing of cognitive improvement.
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Companies:
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Neurochem, Inc.
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Notes:
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On 2 September 2008, Bellus Health (formerly Neurochem Inc.)
commercialized VIVIMIND(TM) (homotaurine) as a branded
nutraceutical through BELLUS Health's wholly owned
subsidiary, OVOS Natural Health Inc.
Updated: 26 January 2009.
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Santa-Maria I, Hernández F, Del Rio J, Moreno FJ, Avila J.
Tramiprosate, a drug of potential interest for the
treatment of Alzheimer's disease, promotes an abnormal
aggregation of tau. Mol Neurodegener. 2007 Sep 6;2:17. Abstract
Aisen PS, Gauthier S, Vellas B, Briand R, Saumier D,
Laurin J, Garceau D. Alzhemed: a potential treatment for
Alzheimer's disease. Curr Alzheimer Res. 2007 Sep;4(4):473-
8. Abstract
Gervais F, Paquette J, Morissette C, Krzywkowski P, Yu M,
Azzi M, Lacombe D, Kong X, Aman A, Laurin J, Szarek WA,
Tremblay P. Targeting soluble Aβ peptide with
Tramiprosate for the treatment of brain amyloidosis.
Neurobiol Aging. 2007 Apr;28(4):537-47. Abstract
Aisen PS, Saumier D, Briand R, Laurin J, Gervais F,
Tremblay P, Garceau D. A Phase II study targeting amyloid-
β with 3APS in mild-to-moderate Alzheimer
disease. Neurology. 2006 Nov 28;67(10):1757-63. Epub 2006
Nov 2. Abstract
Geerts H. NC-531 (Neurochem). Curr Opin Investig Drugs.
2004 Jan ;5(1):95-100. Abstract
Huang TH, Yang DS, Fraser PE, Chakrabartty A. Alternate
aggregation pathways of the Alzheimer beta-amyloid
peptide. An in vitro model of preamyloid. J Biol Chem.
2000 Nov 17;275(46):36436-40.
Abstract
Huang TH, Yang DS, Plaskos NP, Go S, Yip CM, Fraser PE,
Chakrabartty A. Structural studies of soluble oligomers of
the Alzheimer beta-amyloid peptide. J Mol Biol. 2000 Mar
17;297(1):73-87.
Abstract
McLaurin J, Franklin T, Zhang X, Deng J, Fraser PE.
Interactions of Alzheimer amyloid-beta peptides with
glycosaminoglycans effects on fibril nucleation and growth.
Eur J Biochem. 1999 Dec;266(3):1101-10.
Abstract
Yang DS, Yip CM, Huang TH, Chakrabartty A, Fraser PE.
Manipulating the amyloid-beta aggregation pathway with
chemical chaperones. J Biol Chem. 1999 Nov 12;274
(46):32970-4.
Abstract
Kisilevsky R. Anti-amyloid drugs: potential in the
treatment of diseases associated with aging. Drugs Aging.
1996 Feb;8(2):75-83.
Abstract
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