Targeted Delivery System (TDS)
Epeius’ proprietary TDS technology represents an enabling platform for the development of targeted molecular and genetic medicines. This technology can be adapted for the strategic delivery of a broad range of therapeutic genes, recombinant proteins, small peptides and other types of pharmaceutical agents.
The targeted delivery of therapeutic genes and biomolecules is the ideal platform for safe and efficacious disease treatment. Unfortunately, targeted gene delivery has remained elusive and hindered the development of effective genetic medicine. Epeius’ proprietary TDS technology consists of three separate and powerful components: (i) a “pathotropic” or disease seeking guidance system, (ii) a stealth nanoparticle vector or vehicle, and (iii) a designer “killer” gene that compels cancer cells and tumor-associated vasculature to self-destruct without causing collateral damage to non-target tissues. Combined together in a single medicinal unit (a nanoparticle), these three components effectively solve one of the long-standing hurdles in genetic medicine.
When injected intravenously, Epeius’ TDS technology has been demonstrated to efficiently direct gene delivery to metastatic sites, penetrate deep into the tumor, and induce an acute arrest of tumor growth and/or tumor regression without appreciable toxicity in both experimental animal models and human studies.
The Guidance System: Precision-targeted gene delivery is accomplished by incorporating a physiological surveillance function inherent in von Willebrand clotting factor, which is responsible for guiding platelets to exposed collagen in wounds, cancers, and areas of tissue disruption. When injected intravenously, this surveillance function guides the targeted gene delivery vehicle deep into the tumorous tissues, wherein collagenous matrix proteins are exposed and/or newly deposited as a result of tumor invasion, tumor-associated angiogenesis and stroma formation. This powerful and elegantly simple guidance system – designed to deliver the genetic medicine quickly (within minutes) and efficiently to the tumor site – is uniquely suited to function within the context of the human circulatory system.
The Stealth Nanoparticles: Incorporating years of basic research in molecular biology and virology that has demonstrated the broad safety profile of retroviral vectors in a multitude of studies, Epeius employs highly-engineered retroviral vectors into the company’s TDS technology. Even though engineered retroviral vectors have been shown to be safe in humans, they have remained ineffective in genetic medicine due to the inherent non-targeted nature of these vectors. By incorporating Epeius’ unique physiological surveillance functions into viral-based nanoparticles, Epeius has developed a powerful and precision-targeted gene delivery vector that can penetrate deep into the fabric of cancerous tissues, and further, by delivering a therapeutic tumoricidal payload, can impact the course of the disease process.
The Designer Gene: An extensive working knowledge of cellular growth control mechanisms, executive cell cycle enzymes, proto-oncogenes, and their exquisite functions in the body has enabled Epeius to identify the most strategic and efficacious genetic payloads to destroy tumor cells and their associated blood supply, and to enhance the body’s own natural defenses against tumor tissues. In Rexin-G™, Epeuis incorporates a dominant negative mutant of the human cyclin-G1 gene, a powerful, essential, and early part of the cell cycle control pathway. Targeting and aborting the early regulatory components of the cancer cell’s universal replication machinery empowers Rexin-G with striking tumoricidal activity. By targeting proliferative tumor-associated neovasculature, while sparing normal non-dividing blood vessels, Rexin-G exhibits potent anti-angiogenic properties, as well. Combining these powerful tumoricidal and anti-angiogenic activities in a single medicinal unit, Rexin-G exhibits unprecedented single agent efficacy in a broad spectrum of different tumor types.
