Medicilon Assists Yuyao Biotech's STAT3 dual phosphorylation inhibitor YY201 has been approved for clinical trials

On July 20, 2023, the clinical trial application of YY201, a dual-function phosphorylation site-targeted inhibitor of STAT3 independently developed by Yuyao Biotech, was officially approved by the National Medical Products Administration (NMPA).  The indications are advanced solid tumors and relapsed and refractory hematologic malignancies.

Shanghai Medicilon Inc. (Medicilon), as a partner of Yuyao Biotech, provided YY201 with pharmaceutical research services (including raw materials and preparations), preclinical research services (including drug efficacy, pharmacokinetics, safety evaluation) and IND declaration services, helping YY201 successfully pass IND approval and enter the clinical trial stage.

Due to its relatively flat target interface, STAT3 cannot provide a "pocket" structure for specific binding of small molecules, and is recognized as an "undruggable target".  The team of Yuyao biological scientists has been focusing on the basic and translational research of STAT3 targets, and with the help of AI technology, it has discovered and developed a nanomolar STAT3 dual phosphorylation site inhibitor for the first time, a world-leading First-in-class small molecule target drug "YY201".  The drug directly binds to STAT3, inhibits the Tyr705 and Ser727 double-site phosphorylation of STAT3, inhibits STAT3 function and blocks downstream signal transmission, thereby exerting a tumor-suppressing effect.  In vitro pharmacology and pharmacodynamics studies have shown that the affinity activity of YY201 and STAT3 is 1-10 nanomolar, and it is effective in pancreatic cancer, triple-negative breast cancer, lung cancer, acute myeloid leukemia, lymphoma and other solid tumors and blood tumors in vitro proliferation inhibitory activity at 1-10 nM.  It exhibits significant anti-tumor effects in various in vivo models, and can cause complete regression of tumors at extremely low doses.  Pharmacokinetic and toxicological studies have also confirmed the good druggability and safety of YY201.

The clinical approval of YY201 not only represents another important breakthrough of Yuyao Biotechnology, but also verifies the innovative capabilities of Yuyao Biotech Supermolecular Glue Technology Platform and AI Drug Assisted Development Platform.  At the same time, this also proved the technical service strength of Medicilon in preclinical research.

About Yuyao Biotech
 Yuyao Biotechnology is a new drug research and development enterprise empowered by AI, led by innovation, and focusing on new technologies and new targets.  The company has three world-class new drug research and development platforms and multiple independent original product pipelines, and the core products are currently undergoing clinical research registration.  The product pipeline, YY001, targets the tumor immune microenvironment to treat PD-1 antibody-sensitive and insensitive advanced solid tumors, is about to start Phase 2 clinical research and has the potential to become the world's best immune microenvironment antagonist.  The product YY201 is the world's first transcription factor inhibitor, which is about to start phase 1 clinical research in China and the United States, and other product pipelines will soon enter clinical trials in the future.  The company has applied for more than 20 invention patents and has entered Europe, the United States, Japan, Canada, and Australia through PCT international applications.

Yuyao Biotechnology currently has more than 50 employees that hold doctor and master degrees, has more than 5,000 square meters of R&D and office space in Minhang District, Shanghai, and has completed hundreds of millions of investment in professional institutions.  Yuyao Biotech has won some awards and honors such as the National Excellence Award of the Disruptive Technology Innovation Competition of the Ministry of Science and Technology, Central Committee of the Communist Youth League "Create Youth" China Youth Innovation and Entrepreneurship Competition National Gold Award, the National Gold Award in the First Postdoctoral Innovation and Entrepreneurship Competition of the Ministry of Human Resources and Social Security and the Silver Award in the "Internet +" College Students Innovation and Entrepreneurship Competition of the Ministry of Education.

About Medicilon
Since the founding of our company in 2004, Medicilon (Stock Code: 688202.SH) has grown into one of the professional drug discovery contract research organizations (CRO) in China.  Over the years, Medicilon keeps improving their services in biotechnology and pharmaceutical research.  Their services now span across medicinal chemistry, process chemistry, in vitro and in vivo DMPK, preclinical development and bioanalytical support.  By the end of 2022, Medicilon has provided new drug R&D services to more than 1,840 clients around the world, and participated in the R&D of 330 new drug projects that have been approved for clinical trials.  Medicilon is proud to contribute to human health in the globe.