Neprilysin-targeted Therapy for Alzheimer’s Disease

Small molecule therapy through enhancement of neprilysin activity.

Core Benefits

  • Enhancement of neprilysin activity is a new action site of disease-modifying therapy for Alzheimer’s disease (AD).
  • NUP-MBA1(lead compound) enhanced neprilysin activity in specific regions of the brain. These regions(cerebral cortex or hippocampus) are amyloid-vulnerable regions.

Background

Inventor identified neprilysin as a major amyloid-β peptide (Aβ)-degrading enzyme in the brain [Nature Med. 6, 143-151 (2000), Science 292, 1550-1552 (2001)]. The expression of neprilysin declines in the brain not only during aging but also from the early stage of AD development. Decline in neprilysin activity appears to be responsible for sporadic AD, and up-regulation of neprilysin is considered to be a promising strategy for therapy of AD.

In a previous experimental gene therapy for AD-model mice, the inventor demonstrated that the viral vector-mediated neprilysin gene transfer enhanced neprilysin activity in the brains up to 1.5-fold, and that impaired cognitive function of the mice was recovered to normal wild-type mouse level. These results support efficacy of this therapeutic strategy and give us a target value of neprilysin upregulation in vivo.

Data

  • Inventor discovered small molecules for enhancement of neprilysin activity.
  • NUP-MBA1 enhanced neprilysin activity up to 4-fold in vitro study.
  • Subcutaneous administration of NUP-MBA1 enhanced neprilysin level up to 2-fold in the hippocampus of AD model mice.
  • Subcutaneous administration of NUP-MBA1 reduced Aβ42 level in the brain of AD model mice.
  • Oral administration of NUP-MBA1 upregulated neprilysin through gene expression in the brain of AD model mice.

Inventor

Prof. Nobuhisa Iwata, Ph.D.

Department of Genome-based Drug Discovery, Graduate School of Biomedical Sciences, Nagasaki University, Japan

http://www.ph.nagasaki-u.ac.jp/lab/biotech/index-e.html

Patent

PCT/JP2015/081417 (Issued: US, Pending: JP)

Expectations

We are looking for a biotech company who will develop/use this technology further under the patent licensing. These molecules are available under MTA.

Product No. : CD-00853

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