New selection about medications for Alzheimer's disease – What’s Homotaurine?

New selection about medications for Alzheimer's disease –What’s Homotaurine?


Article Author: YJ Chen / R&D Mannager of Fine Chemical Division

攝影師:Alina Vilchenko: https://www.pexels.com/zh-tw/photo/10505442/

 

Homotaurine (3-APS, Tramiprosate) is composed of an amino group and propanesulfonic acid, which differs from taurine by only one carbon number, and can be found in natural seaweed.

Because its structure is similar to γ-aminobutyric acid (GABA), it also has a neuro-inhibitory effect in the brain. In recent years, it has been found that this structure can inhibit the formation of amyloid β (Aβ) peptides, so it is listed as one of the candidate drugs for the treatment of mild Alzheimer's disease (AD).

 

CAS Number: 3687-18-1

Molecular Weight: 139.17

 

Homotaurine can delay Alzheimer's disease progression

With the development of modern medical care, the average life expectancy of human beings is gradually increasing, and the health problems associated with the aging of the population will increase year by year. According to estimates made by World Health Organization (WHO) and Alzheimer's Disease International (ADI), the prevalence of cognitive impairment is expected to triple by 2050, or about 132 million people worldwide will be affected then. [1]

 

In addition to the activity of neural inhibition in the brain, many studies have shown that homotaurine can also delay the pathology of Alzheimer's disease through oral administration, which can stabilize the monomers of Aβ40 and Aβ42 peptides in the brain and avoid from further polymerization [2-5]. Other studies have also found that the volume change of the hippocampal atrophy in patients who received homotaurine treatment is reduced, that means homotaurine has the effect of delaying brain atrophy. [6-8]

 

Not only Alzheimer's disease but also used in the treatment of diabetes

A study related to type 1 diabetes indicates that after receiving homotaurine treatment, the immune system of the mice with metabolic symptoms can be controlled and thereby improve insulin secretion. Therefore, homotaurine is also seen as a drug candidate for type 1 diabetes treatment. [9]

 

Homotaurine and ALZ-801

ALZ-801 is a homotaurine prodrug, modified with one equivalent of valine functional group on the amino group of homotaurine. ALZ-801 will be metabolized and transformed to homotaurine in vivo, but its valine-conjugated property improves its activity by making itself more easily absorbed by the body and maintained in the patient's blood for a longer time. At present, there have been many studies of ALZ-801 on Alzheimer's disease and relevant reports on clinical phase III [10-12].

CAS Number: 1034190-08-3

Molecular Weight: 238.30

 

Sulfonation and HOPAX

HOPAX has mature sulfonated modification technology and related purification equipment, which can provide quality aminosulfonic acid compounds with high purity. These products are used in pharmaceuticals, Cosmeceutical, energy and electroplating and other related industries.


 

Further reading:The application of Sulfobutyl ether beta-cyclodextrin (SEβCD)

Learn more about Hopax Homotaurine

References
[1]World Alzheimer Report 2015 - The Global Impact of Dementia : An analysis of prevalence, incidence, cost and trends. / Prince, Martin James; Wimo, Anders; Guerchet, Maelenn Mari; Ali, Gemma Claire; Wu, Yu-Tzu; Prina, Matthew.London : Alzheimer's Disease International, 2015. 84 p.
[2]Gervais F, Paquette J, Morissette C, Krzywkowski P, Yu M, Azzi M, et al.. Targeting soluble Aβ peptide with Tramiprosate for the treatment of brain amyloidosis. Neurobiol Aging. (2007) 28:537–47. 10.1016/j.neurobiolaging.2006.02.015
[3]Abushakra S, Porsteinsson A, Vellas B, Cummings J, Gauthier S, Hey JA, et al.. Clinical benefits of tramiprosate in Alzheimer's disease are associated with higher number of APOE4 alleles: the APOE4 gene-dose effect. J Prev Alzheimers Dis. (2016) 3:219–28. 10.14283/jpad.2016.115
[4]Kocis P, Tolar M, Yu J, Sinko W, Ray S, Blennow K, et al.. Elucidating the Aβ42 anti-aggregation mechanism of action of tramiprosate in Alzheimer's disease: integrating molecular analytical methods, pharmacokinetic and clinical Data. CNS Drugs. (2017) 31:495–509. 10.1007/s40263-017-0434-z
[5]Tolar M, Abushakra S, Sabbagh M. The path forward in Alzheimer's disease therapeutics: reevaluating the amyloid cascade hypothesis. Alzheimers Dement. (2019) 1–8. 10.1016/j.jalz.2019.09.075
[6]Gauthier S, Aisen PS, Ferris SH, Saumier D, Duong A, Haine D, et al.. Effect of tramiprosate in patients with mild-to-moderate Alzheimer's disease: exploratory analyses of the MRI sub-group of the Alphase study. J Nutr Heal Aging. (2009) 13:550–7. 10.1007/s12603-009-0106-x
[7]Saumier D, Aisen PS, Gauthier S, Vellas B, Ferris SH, Duong A, et al.. Lessons learned in the use of volumetric MRI in therapeutic trials in Alzheimer's disease: the ALZHEMEDTM (tramiprosate) experience. J Nutr Heal Aging. (2009) 13:370–2. 10.1007/s12603-009-0047-4
[8]Sabbagh MN. Clinical effects of oral tramiprosate in APOE4/4 homozygous patients with mild Alzheimer's disease suggest disease modification. J Prev Alzheimers Dis. (2017) 4:136–7. 10.14283/jpad.2017.24
[9]Tian J, Dang H, O'Laco KA, Song M, Tiu BC, Gilles S, Zakarian C, Kaufman DL. Homotaurine Treatment Enhances CD4+ and CD8+ Regulatory T Cell Responses and Synergizes with Low-Dose Anti-CD3 to Enhance Diabetes Remission in Type 1 Diabetic Mice. Immunohorizons. 2019 Oct 21;3(10):498-510. doi: 10.4049/immunohorizons.1900019.
[10]Tsolaki M. Future strategies of management of Alzheimer's Disease. The role of homotaurine Hell J Nucl Med. (2019) 22:82–94.
[11]Caltagirone C, Ferrannini L, Marchionni N, Nappi G, Scapagnini G, Trabucchi M. The potential protective effect of trampirosate (homotaurine) against Alzheimer's disease: a review. Aging Clin Exp Res. (2012) 24:580–7. doi: 10.3275/8585
[12]Abushakra S, Porsteinsson A, Scheltens P, Sadowsky C, Vellas B, Gauthier S, et al. Clinical effects of tramiprosate in APOE4/4 homozygous patients with mild Alzheimer's disease suggest disease modification potential. J Prev Alzheimers Dis. (2017) 4:149–56. doi: 10.14283/jpad.2017.26

Release date:2022.07.06