Targeted Protein Degradation
FIMECS is focusing on a new class of drugs based on targeted protein degradation for the currently ‘undruggable’ targets. Targeted protein degradation has emerged as one of the most promising approaches to eliminate specific disease-causing proteins by utilizing the natural mechanism of protein degradation in our body.
RaPPIDS™, a Drug Discovery Platform for Targeted Protein Degradation
Our hybrid business model is to acquire collaborations with pharmaceutical companies in addition to our pipeline by building our proprietary platform technology, RaPPIDS™ (Rapid Protein Proteolysis Inducer Discovery System), which is focused on targeted protein degradation.
RaPPIDS™, the source of our business, is constantly being improved and expanded through constant investment in R&D.
(1) Basic function
RaPPIDS™, our proprietary technology, is a drug discovery platform for targeted protein degradation based on diversity-oriented synthesis (DOS). RaPPIDS™ consists of two phases: lead generation and lead optimization.
In the lead generation phase, we use “Ready to Conjugate Probes” that consist of multiple E3 ligase binders and linker combinations to quickly generate many kinds of degraders. At this point, the appropriate E3 ligase and linker lengths can be identified in inducing degradation of the target protein to generate lead compounds quickly.
In the lead optimization phase, based on the lead compounds thus obtained, a semi-automated high-throughput DOS approach is used to synthesize divergent compounds with greater diversity in a shorter period of time. Combination of fragmentated E3 ligase binders and linkers makes it possible to discover the best drug candidates in a short time.
We believe that it is currently difficult to accurately predict the ternary complex of target protein, degrader compound, and E3 ligase, which is important for degradation activity. Therefore, efficiently synthesizing and evaluating a large number of degraders is very important in drug discovery for targeted protein degradation.
(2) Identification of novel E3 ligase binders
In the drug discovery for targeted protein degradation, the right “E3 ligase binder”, which plays a major role in protein degradation, is extremely important. Therefore, a strategy of each company is expansion of proprietary lineup of E3 ligase binders. We have also expanded our lineup of E3 ligase binders. With expansion and improvement our platform technology in terms of the efficiency of synthesis and evaluation, we have developed an identification methodology of novel E3 ligase binders toward protein of interest.