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Home: Drug Development: Drugs in Clinical Trials
Drugs In Clinical Trials

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.

Name: Alzhemed™
Other Names: 3-amino-1-propanesulfonic acid, 3-aminopropylsulfonic acid, 3-APS, homotaurine, NC-531, Tramiprosate
Therapeutic Applications: Mild to moderate Alzheimer disease
Therapy Types: Oral, small molecule
Mechanisms: Designed to cross the blood-brain barrier, tramiprosate is an amyloid-β antagonist.
FDA Phase: Not FDA regulated
Primary Medical Role: Tramiprosate has been proposed to inhibit amyloid deposition.
Role in Alzheimer's Disease: 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).
Pharmacological Role: 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.
Side Effects: The most frequent side effects were gastrointestinal, including nausea, vomiting, and diarrhea, which were intermittent and mild to moderate in severity.
Evidence con its efficacy: Tramiprosate failed to demonstrate efficacy in long-term clinical testing of cognitive improvement.
Companies: Neurochem, Inc.
Notes: 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.


References

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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