Drug Discovery Support Services and Solutions
Early ADME Profiling
Our early ADME profiling service, based on proprietary automated high throughput assay technologies and accumulated data, aids in the section of promising compounds for the next stages. At the late stage of the discovery research, the D/P system,* the in vitro simulator of gastrointestinal absorption, enables predictions of the pharmacokinetics profiles of different formulations and helps clients select candidate compounds for development. * D/P system was originally developed by Prof. Yamashita at Setsunan University and licensed to RDN. RDN is continuously optimizing the system in terms of throughput and predictability.
Physicochemical Property Analysis and Preliminary Formulation
For the effective selection of candidate compounds for development, we offer high throughput physicochemical property analysis services. The risk assessments of compounds executed at the early stage of research guide the strategy of compound optimization and minimize project failures. We provide solutions to solubilize hardly-soluble compounds using various formulations and/or DDS, so that in-vivo pharmacokinetics can be evaluated using prototype compounds. The consulting services on the issues caused by the physicochemical properties will also be available.
Through the expertise of various isolation technologies and mass spectrometry, we offer in vivo quantitative analysis of drug candidate compounds (small molecules /biologics) for pharmacokinetics and their related small molecules as pharmacodynamics biomarkers, where we not only apply the analytical methods given by clients, but also develop novel methods for specific target molecules, if necessary.
Synthetic Chemistry Expertise
We provide a wide variety of bioactive substances and intermediates for exploratory research in small, medium and large quantities in response to client requests. The products are delivered with the standard instrumental analytical data supporting their structures and quality.
Compound Library Construction and HTS Hits Profiling
The construction of DS’s original Pharma Space Library (PSL) is ongoing, utilizing technologies and accumulated know how. The technology of parallel synthesis, which has been developed through compound library design and synthesis, is effectively applied to HTS hit expansion for effective creation of lead compounds.
Design/Synthesis of Tool Compounds for Chemical Biology
Collaborating closely with related functions, the expertise of synthetic chemistry is applied to provide tool compounds that are used to identify target macromolecules for the compounds acquired from phenotype screenings.
Hit to Lead
Compound Library Management
For the execution of the high-throughput screening (HTS) campaign, compound libraries, including DS’s proprietary PSL (Pharma Space Library) are maintained in the automated storage and ready to dispatch on request. The cherry picking process based on the computerized retrieval system allows for the flexible handing of library compounds.
RDN is successful in operating HTS campaigns using high density plates with 1536 and 3456 wells, which reduces both the time and cost for acquiring hits. To improve the success rate of the HTS campaigns further, our efforts are now focusing on the optimization of assay methods in terms of sensitivity, specificity, speed and cost.
Hit compounds acquired in a HTS campaign must be confirmed by another method not used for the HTS campaign, including detection of direct interaction by physical methods. It is very critical, we believe, for hit validation to design hit validation strategy combining assay methods with different readouts and different detection principles.
Structure Based Hits Evaluation and Structure Guided Lead Optimization
To detect the direct interaction of hits or other bioactive molecules with the intended drug targets, X-ray, NMR and SPR are applied depending on the extent to which the details of structural information is required. The modes of interaction between bioactive compounds (drug candidates) and drug targets derived from experimental X-ray analysis or in silico molecular modeling are interpreted by our experts and shared with clients to efficiently create and optimize lead compounds from hit compounds.
In vivo Pharmacological Evaluation
Pharmacological Testing in Various Therapeutic Areas
We provide high-quality in vivo pharmacological screening in cancer, cardiovascular and metabolic disease areas, among others, for optimization of lead compounds.
Construction of a novel in-vivo assay system and custom pharmacological testing
Our value-added solution services include the construction of a new pharmacological assessment system with improved pathological similarity to human disease, and custom pharmacological testing with the composite protocol, in which the in-vivo pharmacological assay is combined with any other test items like in vitro bioassays, pharmacokinetics, pathological assessment, and others.
Recombinant Protein Supply
Production and purification of proteins for HTS, in vitro biological assays and structure biological analysis
Besides offering a protein production service to clients, our protein production platform contributes to improved productivity of other functions by managing the internal supply of proteins required for different purposes.
Natural Product Chemistry
Microbial Resources, Extract Libraries and Bioactive Substance Searches
We supply high-quality, highly diverse extract libraries taken from a range of microbial resources collected using proprietary separation sources, processing methods and separation technologies. Based on various screenings using this highly unique extract library, we carefully scrutinize the potential of active constituents and isolate bioactive compounds with required profiles using our expertise in purification and structural analysis.
Utilizing isolated genes responsible for a biosynthesis or conventional microbial conversion, we provide alternate routes for creating intractable compounds by chemical synthesis, which helps accelerate drug discovery processes.