Azekuragan is an antagonist of the advanced glycation endproducts, or RAGE, receptor, meaning that it prevents the receptor from acting.
Found in low levels in a healthy brain, RAGE numbers increase during inflammation.
The patent, number 9,717,710 (‘710), covers the use of 5 mg of azeliragon a day to treat people with mild cases of Alzheimer’s. It runs through October 2034.
VTv expects the U.S. Food and Drug Administration to add the patent to its Orange Book some day. That publication, whose official title is “Approved Drug Products with Therapeutic Equivalence Evaluations,” lists all drugs the FDA has approved, including their patent information. To make the book, of course, azeliragon will have to win FDA authorization.
The patent is the latest in a number covering azeliragon, some of which deal with its formulations.
VTv is “the only company developing a treatment for Alzheimer’s disease by targeting the RAGE receptor, which has demonstrated potential in addressing three key pathologies in Alzheimer’s disease: amyloid-β, tau and chronic inflammation,” Steve Holcombe, the company’s president and CEO, said in a press release. “This new patent is an important milestone as vTv prepares for the results of our upcoming Phase 3 [clinical trial] data readout.” Amyloid-β and tau are proteins associated with Alzheimer’s.
The Phase 3 trial (NCT02080364) is evaluating azeliragon’s ability to slow the gradual decline in cognition and function that people with mild Alzheimer’s experience. Data from the first part of the trial is expected by late March 2018. Additional data should be available in December 2018.
The idea for azeliragon grew out of studies showing that RAGE levels that scientists found in the tissue of deceased Alzheimer’s patients appeared to correlate with the severity and progression of the disease. Higher RAGE numbers affect both neurons and glial cells in the brain. They are also associated with blood vessel dysfunction – another factor that influences dementia.
The rationale behind creating a RAGE antagonist was that blocking the receptor could inhibit processes contributing to Alzheimer’s. The thinking was that azeliragon could reduce the accumulation of amyloid-beta protein and prevent the formation of tau protein fibrils, while also reducing brain inflammation.