As part of MSQ Ventures’ CEO Founder Webinar Series, we were pleased to host Dr. Jin Li, Founder, Chairman, and CEO of HitGen, for a wide-ranging conversation on the company’s innovations in DNA-encoded library (DEL) technology, drug discovery platforms, and its progress in HDAC inhibitor therapies.

Moderated by Marc Estigarribia, Managing Director at MSQ, the session explored HitGen’s scientific milestones, internal pipeline, and global outlook.

Building a Drug Discovery Platform from the Ground Up

Founded in 2012 and headquartered in Chengdu, China, HitGen has become a pioneer in early-stage small molecule discovery. The company’s foundation was inspired by Dr. Li’s decades of experience in UK-based biotech and big pharma, and his vision to bring cutting-edge discovery technologies like DEL to China at a time when few in Asia were exploring the platform. Today, HitGen operates one of the world’s largest DEL platforms—screening over 1.2 trillion molecules.

Dr. Li highlighted the scientific and technical challenges of building such a vast library, from expanding the range of DNA-compatible chemical reactions to ensuring high-fidelity molecule tracking through barcode ligation. This work has allowed HitGen to consistently deliver hits for difficult target classes, including protein-protein interactions, long considered "undruggable."

Focused Innovation Across Therapeutic Areas

While DEL remains its core, HitGen has expanded into complementary platforms, including fragment-based drug discovery (FBDD), targeted protein degradation, and oligonucleotide therapeutics. These technologies are supported by high-throughput synthesis and a newly developed AI-driven optimization engine called the HALO platform.

Dr. Li noted that HitGen is applying its platform selectively to internal programs, primarily in oncology and immunology. The company’s most advanced asset is an HDAC inhibitor (HG146) targeting c-MYC-driven tumors, currently in Phase 2 clinical trials for adenoid cystic carcinoma. Other assets include innate immune modulators and NTRK/ROS1 inhibitors, the latter already licensed in China with FDA IND clearance for international trials.

Principles for Global Partnerships

With over 500 partnerships globally, including collaborations with six major pharmaceutical companies under the “DEL Consortium,” HitGen emphasizes three pillars in successful alliances: early alignment with partner goals, transparent scientific communication, and strict adherence to commercial principles such as target exclusivity and IP protection.

HitGen also participates in strategic consortia like the Structural Genomics Consortium (SGC), contributing DEL resources to support ligand discovery for 2,000 novel proteins by 2035. This work, which includes open data sharing to train AI drug discovery models, reflects HitGen’s broader commitment to scientific collaboration.

Looking Ahead: Technology, Data, and Global Growth

In the next three to five years, HitGen aims to deepen its capabilities in DEL, expand its applications into nucleic acid delivery and novel E3 ligase targeting, and scale its international reach. Dr. Li shared that the company is actively exploring AI integration, mergers and acquisitions, and external partnerships to meet growing demand for innovation in drug discovery.

With subsidiaries in the U.K. and U.S., HitGen continues to position itself as a globally connected company with a strong presence across Asia, Europe, and North America. Its integrated approach—from early discovery through preclinical development—positions it as a versatile partner in both research services and co-development programs.