Aprogen Develops New Anti-Angiogenic Substance VEEP... "Utilized for Retinal Disease Treatment Development"

APROGEN, a company specializing in antibody drug development, announced on the 17th that it has developed a potent anti-angiogenic factor inhibitor called ‘VEEP’ and is applying it to the development of multiple therapeutics using its multi-receptor, bispecific antibody technology.

APROGEN’s VEEP was developed with the support of its affiliate Iventrus and has secured intellectual property rights by obtaining patents in the United States, Australia, Japan, Canada, and other countries. This substance exhibits a binding affinity to angiogenic factors approximately 20,000 times stronger than the antibody bevacizumab, the key component of Avastin, a well-known broad-spectrum anticancer agent. Additionally, it has a binding affinity hundreds of times higher compared to angiogenic factor receptors.

A company representative explained, “Considering that naturally occurring receptors or antibodies, which are larger in size, generally have significantly higher binding affinities to targets than smaller polypeptides, it is remarkable that the relatively small VEEP protein exhibits such a high binding affinity. A high binding affinity to angiogenic factors means it can more effectively eliminate angiogenic factors present around tumors.”

Before designing VEEP, APROGEN focused on the fact that the angiogenic factor binding receptor VEGFR1 and the neuronal receptor Neuropilin-1 (NRP1) sometimes bind together in vivo and act as a single receptor. Subsequently, they discovered through X-ray protein crystallography that when these two are bound together, the IgG2 domain of VEGFR1 and the b1 domain of NRP1 are positioned closely. By isolating and connecting only the IgG2 and b1 domains, they succeeded in creating a very small hybrid receptor.

VEEP, the world’s first angiogenic factor inhibitor utilizing Neuropilin-1 (NRP1), is relatively small in protein size but binds much more strongly to the angiogenic factor VEGF than the much larger VEGFR1 receptor, NRP1 receptor, or the broadly known anticancer antibody bevacizumab. A company representative stated, “The Kd values (dissociation constants, where a smaller value indicates stronger binding) for VEGF are 33 pM for VEGFR1 receptor, 312 pM for NRP1 receptor, and 1000 pM for bevacizumab antibody, whereas VEEP’s Kd is 0.05 pM. This means VEEP binds to VEGF more than 20,000 times better than bevacizumab, the raw material of Avastin.”

APROGEN is currently expanding the application of VEEP beyond anticancer drugs to treatments for retinal diseases where abnormal angiogenesis is problematic. A company representative said, “When creating bispecific or trispecific receptors or multispecific antibodies, the size of the molecule tends to increase, which is a challenge. However, VEEP is small and has favorable physical properties, making it highly advantageous for development as multi-receptor or multispecific antibody therapeutics. In the trend of developing treatments for diseases such as macular degeneration or diabetic retinopathy, which aim to inhibit multiple targets simultaneously, these characteristics of VEEP represent another competitive edge for our company.”

This content was produced with the assistance of AI translation services.