Our Innovative Small Molecule R&D
Our mission for innovative small molecule R&D is to create important, novel medicines by pursuing bold ideas, employing rigorous research, and striving for scientific excellence in everything we do. At Huiyu, we are passionate about science and dedicated to discovering and developing highly differentiated therapeutics through innovative chemistry to treat diseases in areas of high unmet need such as cancers. While focusing on discovering novel drugs by employing proven methods grounded in medicinal chemistry, molecular biology and pharmacology, we are driven to develop first-in-class or best-in-class oral and injective therapies that profoundly improve patients’ lives. Through scientific excellence and imagination, we leverage our expertise in small molecule drugs to discover and develop groundbreaking medicines. Our scientists won’t see the “undruggable” as an obstacle; they see it as a good opportunity to start with. The strategies we employ include dual-target inhibition, PROTACs (Proteolysis Targeting Chimeras), and novel linker-payload platforms for Antibody-Drug Conjugates (ADCs) — represent the cutting edge of oncology research and drug development.
Targeted therapy and immuno-oncology
Targeted therapy and immuno-oncology (IO) are two innovative approaches in cancer treatment that have significantly advanced the field of oncology in recent years. Our strategy in targeted therapy involves the use of small molecule drugs or other substances to precisely identify and attack cancer cells while causing minimal harm to normal cells. These therapies target specific molecules involved in cancer cell growth, survival, and spread, such as proteins, enzymes, or genetic mutations.
Immuno-oncology harnesses the body's immune system to recognize and destroy cancer cells. The immune system has the ability to recognize and eliminate cancer cells, but tumors can develop mechanisms to evade immune detection. Our small molecule IO strategies involve the development of small molecules that modulate the immune system to enhance anti-tumor immune responses. While traditional IO approaches often focus on biologics such as monoclonal antibodies, small molecule IO therapies offer several potential advantages, including oral administration, improved tissue penetration, and the ability to target intracellular signaling pathways.
In the meantime, at Huiyu, we are actively exploring combination strategies that leverage both targeted therapy and IO to enhance treatment efficacy and overcome drug resistance. Our combination approaches involve targeting specific molecular pathways in cancer cells while simultaneously modulating the immune system to enhance anti-tumor immune responses. Targeted therapy and immuno-oncology represent our two promising avenues among others for the development of personalized and more effective cancer treatments.
Focusing on drug resistance - Dual targeting platform
Drug resistance is a significant challenge in cancer treatment and can occur with both targeted therapy and immuno-oncology approaches. Understanding and addressing drug resistance mechanisms are crucial for improving treatment outcomes and prolonging patient survival. Drug resistance can arise through various mechanisms, including genetic mutations, alterations in drug targets, activation of alternative signaling pathways, drug efflux pumps, and changes in the tumor microenvironment.
Tumor cells may activate compensatory pathways to bypass the effects of targeted therapies.
Huiyu has been focusing on the study of drug resistance mechanisms for years. Recently, a variety of underlying resistance mechanisms to targeted cancer drugs have been elucidated by our biologists. These research results revealed that the dual-target therapeutic strategy would be an attractive avenue. Compared to drug combination strategies, single molecule dual-target inhibiting drugs can avoid the risk of DDI, have a superior pharmacokinetic and safety profile. As a consequence, we have established a mechanism-based Dual-Target Small Molecular Drug Design Platform (DTDDP®). This platform includes two modules, SynFind and MoleFuse. With SynFind we developed a platform that utilizes bioinformatics and systems biology techniques to discover dual-targets, including modules for analyzing target interactions, drug synergies, pathway interactions, and omics data. In the MoleFuse module, we developed a structure-based dual-target molecule generation algorithm that uses reinforcement learning and active learning to make dual-target molecules by joining pharmacophores and optimizing other properties at the same time. Our DTDDP® represents a paradigm shift in the battle against drug resistance. By addressing the issue at its roots, this innovative approach holds great potential for the development of next-generation therapeutics with enhanced efficacy and extended drug lifespan.
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