On December 21, 2021 Aptamer Science, a company specializing in aptamer platforms, reported that it has completed the development of its own linker technology to be applied to an aptamer-based drug delivery platform (Aptamer Drug conjugate (ApDC)) and has applied for domestic and PCT patents (Press release, Aptamer Sciences, DEC 21, 2021, View Source;idx=271 [SID1234641628]).

Schedule your 30 min Free 1stOncology Demo!
Discover why more than 1,500 members use 1stOncology™ to excel in:

Early/Late Stage Pipeline Development - Target Scouting - Clinical Biomarkers - Indication Selection & Expansion - BD&L Contacts - Conference Reports - Combinatorial Drug Settings - Companion Diagnostics - Drug Repositioning - First-in-class Analysis - Competitive Analysis - Deals & Licensing

                  Schedule Your 30 min Free Demo!

The linker technology developed this time is a dendrimer-type molecular structure that can load multiple payloads, and the number of loaded payloads can be adjusted depending on the number of branched branches.

The junction site with the aptamer is also designed to enable a click reaction mediated by a simple thiol group, which can further improve ApDC production and pharmacological efficacy.

ApDC technology, due to the nature of the aptamer structure, had to limit the drug loading location to the end, which also limited the number of drugs.

The company explains that through the development of this technology, the drug-aptamer ratio (DApR) can be increased by loading the desired amount of drug into ApDC.

An Aptamer Science official said, "In the case of antibody-drug conjugate (ADC) technology, aggregation occurs due to increased hydrophobicity when introducing multiple payloads, which has a significant impact on manufacturing and stability.

"In order to solve this problem, when introducing a hydrophilic group such as PEG, there was a difficulty in making the manufacturing process complicated," he said. "Because the aptamer material itself shows high hydrophilicity,

"It is possible to manufacture stable ApDC with a high drug loading rate using a simple linker without introducing additional functional groups."

The developed branched linker-payload technology is being applied to various ApDCs being developed by the company, such as CD25 and Trop2.

In addition, we plan to introduce it in the development of follow-up technologies, such as targeting immunostimulants (STING, TLR7/8) and targeting delivery of therapeutic radionuclides.

ADC, in which global big pharma companies are investing recently, is emerging as a technical limitation due to side effects such as interstitial lung disease (ILD) and complex manufacturing processes.

ApDC’s advantages over ADC include high cancer tissue penetration, low side effects, and high stability.

Go to article: Aptamer Science "Development of proprietary ApDC linker technology"