History

APERUS was founded and is majority owned by AVIDIN Ltd., a pharmaceutical research company, and owns all the rights and patents of of Q134R and its related compound family. Its objective is to manage the R&D process and marketing of drug candidates to provide a solution for neurodegenerative diseases The most advanced clinical candidate is Q134R which is a molecule with multiple effects against Alzheimer’s disease.. AVIDIN itself is a drug researcher and developer for diseases of the central nervous system, and for cancer. AVIDIN’s Medicinal Chemistry Department has made major discoveries of potential drug candidates, including Q134R.

Due to the innate complexity of the pathological conditions of the brain of patients with Alzheimer’s disease (AD), the research process has been based on a multiple target approach that could yield the most efficient drugs. Q134R exerts its positive effects on Alzheimer’s disease in three mechanisms of action which makes it a novel and potential disease modifying drug:

Q134R is a strong cytoprotective agent. At nanomolar concentration, it protects neuronal cells against neuronal death induced by reactive oxygen species (ROS) and Abeta (amyloid beta) oligomers, as well as restores mitochondrial functioning. In cellular assays Q134R induces the expression of genes whose protein products combat oxidative-stress, such as hemoxygenase-1 (HMOX-1), gluthatione peroxidase-1 (GPX-1), superoxide dismutase-1 (SOD-1) and erythropoietin (EPO) in a concentration dependent manner.

Q134R has inhibitory effects on NFATs, a family of calcineurin- (CN) dependent transcription factors linked to multiple pathologic hallmarks that emerge during Alzheimer’s disease. Q134R inhibits both the induction of the NFAT transcriptional activity and caspase-3 enzyme activity, therefore prevents neuronal death by dual effects. Numerous studies show that inhibition of CN/NFAT signalling leads to beneficial effects on amyloid pathology, neuroinflammation, neuronal viability, synaptic physiology, and cognitive function in mouse models of Alzheimer’s disease. Q134R exhibits NFAT inhibitory properties without suppressing direct calcineurin activation, hence no immunosuppressive side-effects are anticipated.

Q134R restores memory impairment caused by scopolamine or Abeta oligomers, by modulation of the GABAA-gated Cl- channels, specific for neuronal cells including those playing a role in extrasynaptic signalling that modulates memory functions.