XtalPi Achieves Clinical Milestone with PEP08, Expands AI Drug Discovery Collaboration with PharmaEngine on Synthetic Lethality Pipeline

Recently, XtalPi (Shenzhen) Technology Co., Ltd.,2228.HK) announced that its strategic cooperation with PharmaEngine Inc. (4162.TWO) has achieved significant dual progress.XtalPi-Empowered Discovery of Next-Generation PRMT5 Inhibitor PEP08 Successfully Initiates Patient Recruitment for Solid Tumors, Achieving Milestone. At the same time, based on the excellent efficiency of the PEP08 AI drug discovery project and the quality of platform delivery,The two parties have also launched a second AI drug discovery project targeting an entirely new "synthetic lethality" site.。

PEP08 Project Approved for Clinical Trials in June 2025, Currently Conducting Phase I Clinical Trials for Solid Tumors in Australia and Taiwan, China. The orderly recruitment and dosing of clinical patients not only preliminarily confirm the good safety and tolerability of PEP08 but also mark that this high-value pipeline is advancing rapidly and steadily towards clinical translation.

This pipeline was precisely designed and screened by XtalPi from a million-level molecular library based on its underlying quantum physics models, AI algorithms, and robotic experimental platforms. It addresses the significant hematological toxicity challenge caused by the poor selectivity of traditional PRMT5 inhibitors.PEP08 innovatively utilizes the MTA synergistic binding mode to specifically target and kill MTAP-deficient tumor cells, which account for 10-15% of human cancers, while maximizing the protection of normal cells. It shows great potential in the treatment of non-small cell lung cancer, pancreatic cancer, and glioblastoma.The preclinical study results published at the 2025 AACR show that,PEP08 has significant advantages over the first-generation PRMT5 inhibitors,Demonstrating "Best-in-Class" Potential。

Building on the success of PEP08 in drug discovery, the two parties have subsequently initiated the development of PEP10, a second synthetic lethality target project.The launch of the new project fully reflects the deep integration of PharmaEngine's strong expertise in tumor biology with XtalPi’s AI molecular design advantages, which will help PharmaEngine accelerate the development of a uniquely competitive synthetic lethality drug pipeline targeting the high-growth global market for precision oncology.

"Synthetic lethality," as a highly challenging target for research and development, has been recognized as a star track for the new generation of anticancer drugs. According to Globocan and industry analysis data, the global synthetic lethality drug market size is expected to increase from USD 4.2 billion to USD 17.6 billion from 2024 to 2033, with an annual compound growth rate of 17.3%. In recent years,Globally, several synthetic lethality pipelines still in the IND and Phase I clinical stages have reached blockbuster licensing deals exceeding one billion dollars, further highlighting the extremely high clinical value and commercial popularity of this field.

The continuous progress of PEP08, along with the simultaneous advancement of the second new drug discovery project, marks that XtalPi's "platform + pipeline" dual-driven model is accelerating the release of scale benefits.In the high-value, fast-growing sectors with active transactions, XtalPi has frequently achieved milestone progress. This not only strongly confirms the depth of its technical barriers but also demonstrates the company's significant commercial upside in generating substantial returns through technology sharing and rights distribution.With high frequency and high-quality R&D delivery, the company is continuously building a long-term profit engine with strong resilience and high certainty.

Dr. Shu-Hao Wen, Chairman of XtalPi, stated:"Congratulations on the breakthrough progress of PEP08 in clinical development. The steady advancement of PEP08 and the smooth launch of the second project signify not only the success of a single drug but also the best endorsement of XtalPi's underlying AI and robotics platform's 'replicable innovation capability.' We are transforming highly challenging biological problems into clinical assets with high certainty. As the platform’s potential continues to be unleashed, we are confident in our ability to continuously empower global partners and, through a diversified pipeline, create long-term compounded commercial value for shareholders."

"PharmaEngine Inc. continues to strengthen its R&D capabilities. Our collaboration with XtalPi fully demonstrates the company's ability to leverage cutting-edge technology to drive the next generation of breakthrough discoveries in the field of precision oncology."Dr. Hong-Ren Wang, General Manager of PharmaEngine Inc., stated"XtalPi's R&D platform played a key role in the early discovery phase of PEP08, laying a solid foundation for its smooth entry into clinical trials. The collaboration between the two parties on PEP08 and the second project is a concrete manifestation of our continuous efforts to advance global cancer treatment."

● CloseYuPharmaEngine Inc. ●

PharmaEngine Inc., headquartered in Taipei City, commenced operations in May 2003. The concept behind PharmaEngine's establishment is to focus on new drug development through international strategic alliances via the "Virtual Pharmaceutical Company Business Model," reducing risks associated with new drug development. PharmaEngine’s commercialized product, ONIVYDE®, is used for treating adult patients with metastatic pancreatic cancer. Additionally, PharmaEngine is actively advancing the Phase I clinical trials of its pipeline products PEP07 (a CHK1 inhibitor) and PEP08 (an MTA-cooperative PRMT5 inhibitor). In the future, leveraging its extensive experience in project management, PharmaEngine plans to continuously expand its R&D pipeline and aims to accelerate the discovery, development, and commercialization of novel cancer drugs through international cooperation or licensing.