Home Healthytide Biosciences Advances China's First Homegrown Targeted Peptide Radiopharmaceuticals with Dual-Platform Innovation

Healthytide Biosciences Advances China's First Homegrown Targeted Peptide Radiopharmaceuticals with Dual-Platform Innovation

Oct 17, 2022 10:00 CST Updated 10:00

Over the past century, peptide drugs have mostly been developed as standalone therapeutics based on their intrinsic molecular properties or integrated into related treatment modalities. According to statistics from VCBeat, approximately 118 peptide drugs have been approved domestically and internationally, with around 300 others in clinical trials. However, with the advancement and application of AI and biotechnologies, the emergence of innovative therapies such as small nucleic acid drugs, cell therapies, and gene therapies has gradually overshadowed peptide drugs.


Simple peptide molecules are no longer a novel concept in the market, and research into their properties and structures is relatively mature.Discovering novel targeted peptide molecular structures and developing new conjugation formats represent the “optimal solution” for innovative peptide therapeutics to seek new opportunities.

 

VCBeat’s New Medicine recently interviewed Hangzhou Hetai Jianyu Biotechnology Co., Ltd. (hereinafter referred to as “Hetai Jianyu”), a company focused on “discovery of innovative peptide molecules” and “development of targeted radiopharmaceutical applications.”


“Hetai Jianyu primarily focuses on innovations in peptide molecules and technologies, including the discovery of novel peptide molecular structures and the exploration of innovative conjugation strategies between peptides and other molecular types.”Dr. Gao Jian, Founder, Chairman and CEO of Hetai Jianyu, said.


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 Dr. Gao Jian, Founder, Chairman, and CEO of Hetai Jianyu


Discovery of New Polypeptides


Gao Jian has nearly 20 years of research and work experience in the field of peptides.He pursued his combined master’s and doctoral studies at the State Key Laboratory of Bio-organic Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences. He later went to the University of Basel in Switzerland, where he conducted postdoctoral research under the supervision of a dual member of the German and U.S. academies who was nominated for the Nobel Prize. Upon returning to China after completing his postdoctoral work, he has continued to focus extensively on the preclinical development and industrialization of novel peptide-based drugs.

 

Co-Founder, Director and CTO Gao HeweiAfter completing his integrated bachelor’s, master’s, and doctoral studies in Nuclear Physics, Science and Technology at the Department of Engineering Physics, Tsinghua University, he pursued postdoctoral research at Stanford University in the United States. He currently serves as a doctoral supervisor in Radiation Imaging at the Department of Engineering Physics, Tsinghua University. Previously, Gao Hewei held positions as a Senior Scientist at GE Global Research Center, GE Healthcare, and Reflexion Medical in the United States, where he led the development of the world’s first 256-slice high-end diagnostic CT scanner and the world’s first Biologically Guided Radiation Therapy (BgRT) system for targeted radiopharmaceuticals.

 

As seasoned researchers in the fields of chemistry and physics, respectively, the two co-founders conceived the idea a decade ago, during the early stages of innovative drug development in China, to develop a novel therapeutic agent with distinct clinical applications that leverages the interdisciplinary synergy of “chemistry & physics.” In 2017, Gao Hewei’s pivotal research on the development of targeted radiopharmaceutical-guided diagnostic and therapeutic equipment achieved a breakthrough, earning Breakthrough Device Designation from the U.S. FDA. This prompted Gao Jian to recognize that the specific expression and conjugation capabilities of peptide proteins could fully meet the technical requirements for advancing “targeted radiopharmaceuticals.”

 

In May 2021, Hetai Jianyu was officially established. Leveraging the significant development potential of peptide molecular specificity and conjugation in the field of “targeted radiopharmaceuticals,” and drawing on the complementary technical advantages and research capabilities of both parties, the two founders determined that the company would pursue two strategic directions:SinceLead the construction of a high-throughput screening (HTS) system for targeted peptide-based innovative molecule discovery;Targeted Peptide Radionuclide PET/CT Platform for Precision Tumor Diagnosis and Development of Innovative Radiopharmaceuticals for Radiotherapy.


"De novo drug molecule discovery, from 0 to 1, is the most challenging."The weak peptide molecule discovery system in China is also one of the important reasons for the slow development of innovative peptide drugs in the country.

 

“Ultimately, a high-throughput screening and targeted molecular discovery platform at the foundational level must achieve: high-throughput compound libraries, high-throughput biological screening, rapid screening speed, and cost control.” Hetai Jianyu’s peptide molecular discovery system has made breakthroughs in these four areas. Gao Jian believes that these are the core criteria for evaluating a foundational molecular discovery platform.

 

Through multiple generations of technological innovation, Hetai Jianyu has established the Novotide™ peptide entity library construction and screening technology system. This system enables the annual construction of peptide entity libraries with molecular diversity on a million-scale. Furthermore, unlike screening systems involving mixtures of billions of molecules, Novotide™ yields high-purity single peptide molecules that are suitable for subsequent binding screening against target proteins.

 

On the other hand, the system is also equipped with Hetai Jianyu’s independently developed enzymatic screening platform and cellular functional screening platform, expanding screening dimensions and enhancing the speed and accuracy of screening and evaluation.

 

Ultimately, Novotide™ has achieved technological breakthroughs in the speed, cost, and data accuracy of high-throughput screening for peptide-based molecular entities, enabling rapid discovery, optimization, and engineering of targeted compounds or lead compounds for novel targets. Novotide™ lays a foundation for the development of innovative peptide molecules, offering strong competitiveness and broad application prospects.

 

Conjugation of Novel Radionuclides

 

With Novotide™ securing the foundation for Hetai Jianyu’s discovery of innovative peptide molecules, Gao Hewei led a team to conduct small-animal PET/CT imaging research and development related to radiopharmaceuticals for precise diagnostic targeted radionuclide imaging and targeted radiotherapy.

 

Globally, only 10 targeted peptide radiopharmaceuticals have been approved for market launch, while there is still a gap in domestically approved drugs in this category. Leveraging the technical expertise of its two founders, Hetai Jianyu has entered this field, aligning with current clinical needs and addressing technological pain points by focusing on indications for lung cancer, which has a high incidence rate, and pancreatic cancer, which is difficult to detect at an early stage.

 

Novotide™ is utilized to screen for targeted peptide molecules that specifically bind to receptor proteins highly expressed in specific tumors. These peptides are conjugated with radionuclides of appropriate half-life. The resulting conjugates accurately accumulate in tumor tissues within the human body, allowing clear visualization of tumor morphology under PET/CT imaging. By combining the targeting capability of peptides with the radioactive imaging properties of radionuclides, information such as tumor location, size, primary site, and metastatic lesions can be precisely displayed in the images.


By adjusting radionuclides with different half-lives and leveraging the same technical principles, targeted and precise internal irradiation of tumor tissues can be achieved, thereby delivering the effects of precision radiotherapy.

 

Hetai Jianyu’s R&D pipeline includes a series of key regulatory targets involved in tumor angiogenesis, which modulate tumor cell migration and invasion, mediate tumor cell proliferation, and influence drug resistance and radiation resistance. Based on existing in vivo and in vitro animal study data, this targeted peptide radiopharmaceutical demonstrates high specificity, significant accumulation in tumor tissues, minimal distribution in other metabolic organs, and high contrast in diagnostic imaging.To date, no radiopharmaceuticals for theranostics targeting this class of targets have been marketed.Promising to achieve a breakthrough in radiopharmaceuticals for theranostics targeting this class of targets.

 

In the future, in addition to research on developing new indications, Hetay Jianyu also plans to apply this technology to richer molecular imaging application scenarios, such as magnetic resonance imaging and surgical navigation, thereby achieving precision in molecular imaging with its own unique characteristics.Diagnostic and Therapeutic Drug Development System.


Controlling the Source of Molecular Innovation and Leading the New Drug Development Process


Currently, Hetai Jianyu has established platforms for lead compound discovery, cell and organoid evaluation, and in vivo pharmacokinetic studies in animals. To support subsequent Investigational New Drug (IND) registration filings, strategic collaborations have been formed with leading domestic clinical hospitals’ nuclear medicine departments, universities, research institutions, and enterprises to build comprehensive evaluation systems covering in vivo pharmaceutical sciences, pharmacodynamics, pharmacokinetics, and GLP-compliant toxicology.

 

Hetai Jianyu adheres to the foundational logic of discovering innovative peptide-based molecules, advancing the application and commercialization of novel drug projects with intellectual property rights and specialized biological value, while leading the new drug development process. Through this approach, the company aims to rapidly accelerate the closed-loop development of innovative peptide therapeutics.

 

By mastering the origins of peptide molecule discovery and developing targeted peptide radiopharmaceuticals, an application sector that is currently untapped in China,For Hetai Jianyu, this represents not only an opportunity but also a challenge.

 

Underlying Peptide Molecule Discovery and Screening System, Featured Applications of Peptide Molecules,They are two technical pathways with different focuses, yet interconnected and mutually reinforcing.Simultaneously advancing both technologies presents a significant challenge.But behind Hetai Jianyu lies over 20 years of accumulated expertise in targeted molecular screening and nuclear science and technology applications. The two founders are confident in meeting this challenge and turning it into their own advantage and opportunity.

 

Over the next two years, Hetai Jianyu willContinue to optimize its peptide molecule discovery and screening system, striving to achieve a leading position globally in the same category. Meanwhile,Accelerate the IND Applications for Self-Developed Project Pipelines, and plans to initiate its Series A financing round within the next year to support the subsequent clinical development and application of multiple distinctive targeted peptide radiopharmaceuticals. Over the next five years, Hetai Jianyu will gradually expand its international commercial operations in line with corporate development needs, aligning with markets in Europe, the United States, and Japan while undergoing market validation.