Anavex Life Sciences Corp. has announced the issuance of U.S. Patent No. 12,180,174, which covers novel crystalline forms of its drug candidate ANAVEX®2-73 (blarcamesine). This exciting development, reported on January 27, 2025, positions the company to expand its patent portfolio and its therapeutic options for neuroprotection.
The United States Patent and Trademark Office (USPTO) granted this patent, which pertains to the dihydrogen phosphate salt forms of ANAVEX®2-73, alongside methods of use, transdermal patches, and enteric coated oral dosage forms. With the patent expected to remain valid until at least July 2039—barring any extensions—this is seen as transformative for the company's future innovations.
Christopher U. Missling, Ph.D., the President and CEO of Anavex, expressed enthusiasm about the patent issuance. "The issuance of this U.S. Patent again showcases our expertise in identifying and pursuing novel therapeutic forms and formulations rooted in science,” he stated. Missling elaborates on the potential of these unique dihydrogen phosphate crystalline forms, which promise not only to facilitate once-daily oral dosing, but also offer the possibility to deliver the active compound through transdermal patches. This alternative method of administration could greatly simplify patient compliance.
The therapeutic focus of ANAVEX®2-73 extends to several central nervous system (CNS) disorders, including Alzheimer’s disease and Parkinson’s disease. Anavex Life Sciences is dedicated to the development of innovative treatments for these debilitating conditions, showcasing its commitment to addressing significant unmet medical needs.
The concept of crystal polymorphism plays a pivotal role here. Crystal polymorphism refers to the ability of compounds to crystallize in different structures, which can dramatically influence their properties. For pharmaceuticals, the existence of varied crystalline forms can lead to differences in solubility, stability, and overall efficacy. Anavex’s expertise lies in identifying and optimizing these forms for their drug candidates, which has proven to be invaluable.
Polymorphic forms can often lead to significant differences: for example, only one out of several forms of the popular analgesic acetaminophen is made for commercial use, the others being unstable. Finding the best crystal form requires extensive research and expertise, outcomes which Anavex has achieved with its candidates, ANAVEX®2-73 and ANAVEX®19-144.
The announcement of this new patent adds to Anavex’s existing patent portfolio, which already includes several significant patents for ANAVEX®2-73. The company had previously completed Phase 2 and Phase 2b/3 clinical trials for Alzheimer's disease, as well as studies targeting additional CNS disorders, establishing ANAVEX®2-73 as one of their lead candidates.
"We believe the unique properties of the dihydrogen phosphate crystals make it possible to deliver the active (ANAVEX®2-73 freebase) in transdermal patches, which could simplify administration and boost patients' compliance," Missling explained, indicating the transformative potential of this technology for patient care.
Besides Alzheimer’s and Parkinson’s disease, ANAVEX®2-73 has also shown promise for treating Rett syndrome and other neurological conditions. The drug aims to restore cellular homeostasis by targeting SIGMAR1 and muscarinic receptors, which play significant roles in cellular signaling and function. Preclinical studies suggest it could arrest or even reverse the progression of Alzheimer’s disease—a promising assertion for those affected by this condition.
With the foundation laid through rigorous clinical research—including grants from the Michael J. Fox Foundation for Parkinson's Research—Anavex Life Sciences is actively pushing forward. The unique positioning of ANAVEX®2-73, empowered by this new patent, sets the stage for broader deployment across the therapeutic spectrum. This could eventually lead to effective treatments for chronic conditions affecting millions worldwide.
The scientific exploration of ANAVEX®2-73 demonstrates not only Anavex’s deep commitment to research but also the exciting opportunities arising from its innovative approaches to drug development. Moving forward, the company plans to capitalize on this new patent, leveraging it to advance clinical trials and possibly bring novel treatments to market.
For patients and healthcare providers seeking alternative treatment options, news of such advancements is encouraging. Anavex Life Sciences stands at the forefront of biopharmaceutical innovation, continuously striving to provide relief to those suffering from CNS disorders. Their latest patent issuance is just one step on this important path.