Expected to meet unmet demand for ADC
Aptamer Sciences, helmed by CEO Dong-Il Han, unveiled its achievement on December 21st, announcing the successful culmination of proprietary linker technology tailored for 'Aptamer Drug Conjugate (ApDC)' applications in drug delivery platforms. The company has initiated filings for Korean and PCT patents, marking a significant leap in their technological portfolio.
The novel linker technology, fashioned with a 'Dendrimer-type' molecular structure, stands distinguished for its capability to host multiple payloads. The adjustable payload attachment, facilitated by its branched arms, signifies a pivotal feature. Moreover, the adept junction with the aptamer streamlines a simple 'thiol-based' click reaction, thereby elevating both the production efficiency of ApDC and its pharmacological efficacy, elucidated by the company.
Previously constrained by the structural limitations of aptamers, the loading site for drugs within ApDC was confined to the terminus, thereby restricting the payload capacity. However, this recent breakthrough allows for customizable drug loading, thereby augmenting the 'Drug-to-Aptamer Ratio (DApR),' marking a paradigm shift catalyzed by this technological innovation.
An Aptamer Sciences representative highlighted, “In contrast to Antibody Drug Conjugate (ADC) technology, where multiple payloads often lead to heightened hydrophobicity and manufacturing challenges, our technology bypasses these concerns. Aptamers, inherently hydrophilic, facilitate the production of stable ApDC with high drug loading rates, utilizing simple linkers devoid of additional functional groups.”
Furthermore, they emphasized, “The incorporation of branched linker technology in ApDC molecules, forming a micelle structure, holds promise in addressing stability concerns within the body, previously regarded as a limitation in aptamer technology. Ongoing research aims to delve deeper into this potential solution.”
"The application of the developed branched linker-payload technology extends across various ongoing ApDC projects at Aptamer Sciences, targeting diverse areas like CD25, Trop2, and others," the company announced. "Plans are underway to integrate this innovation into forthcoming developments, including immune stimulants (STING, TLR7/8) and therapeutic radioisotope transportation."
While the ADC field garners significant investment from global pharmaceutical companies, boasting 15 newly approved drugs and over 800 substances in varying developmental stages, it grapples with notable technical constraints. Issues such as interstitial lung disease (ILD) and intricate manufacturing processes loom as critical challenges.
Aptamer Sciences asserted, “ApDC presents distinct advantages over ADC, offering superior penetration into cancerous tissues, reduced side effects, and heightened stability.” They further emphasized, “With this breakthrough allowing tailored drug loading, heightened therapeutic efficacy is anticipated.” Additionally, they revealed ongoing partnership engagements for 'AST-201,' a forthcoming solid tumor therapy set to initiate clinical trials next year, and for 'AST-202,' an immunotherapeutic agent currently in preclinical phases.
