Alzheimer's disease AD is an irreversible, progressive neurodegenerative brain disorder with no current cure. One of the important therapeutic approaches of AD is the inhibition of site APP cleaving enzyme 1 BACE1 , which is involved in the rate limiting step of the cleavage process of the amyloid precursor protein APP leading to the generation of the neurotoxic amyloid A protein after the secretase completes its function. ...Furthermore, the review demonstrates with increasing evidence that despite tremendous efforts and promising results conceived with BACE1 inhibitors, the latest studies suggest that their clinical use for treating Alzheimer's disease should be reconsidered. ...