 |
SHENZHEN, China, May 4, 2026 /PRNewswire/ — XtalPi (2228.HK), a leading AI- and robotics-powered innovation platform, today announced dual breakthroughs in its strategic partnership with PharmaEngine (4162.TWO) PEP08, a next-generation PRMT5 inhibitor discovered via XtalPi’s platform, has successfully begun enrollments in a Phase I solid tumor trial, achieving a new clinical milestone. Built upon the success of PEP08 at the drug discovery stage, the two companies initiated a second project, targeting a different undisclosed synthetic lethality mechanism.
PEP08 received clinical clearance in June 2025 and is currently in Phase I evaluation for solid tumors in Australia and the Taiwan region. The enrollment milestone underscores XtalPi’s ability to deliver differentiated molecules with strong drug-like properties, while demonstrating the program’s steady clinical advancement.
Leveraging XtalPi’s integrated quantum physics-, AI-, and robotics-powered platform, PEP08 was designed to overcome the dose-limiting hematological toxicities seen with first-generation PRMT5 inhibitors. The molecule exploits an innovative MTA-cooperative binding mode to specifically target MTAP-deleted tumors—a genomic alteration found in 10-15% of all human cancers, with higher frequencies observed in NSCLC, pancreatic cancer, glioblastoma, and more. Preclinical data presented at 2025 AACR show PEP08 achieving superior efficacy compared to other clinical-stage MTA-cooperative PRMT5 inhibitors across multiple MTAP-deleted tumor models, supporting a potential best-in-class profile.
Driven by the success of PEP08 at the drug discovery stage, the partnership expanded into a second project. By combining PharmaEngine’s deep oncology expertise with XtalPi’s AI and robotics molecular design engine, the duo aims to capture additional market share in the synthetic lethality space.
Synthetic lethality is widely recognized as challenging yet highly promising frontier in oncology. According to Globocan and industry data, the global market is expected to grow from $4.2 billion to $17.6 billion by 2033, at a 17.3% CAGR. In recent years, several early-stage licensing deals in this space have exceeded $1 billion USD, further underscoring the immense clinical value and commercial appetite for this category.
The clinical advancement of PEP08 and the ongoing collaboration of the second project serve as a dual validation of XtalPi’s AI+robotics discovery engine. By repeatedly meeting rigorous benchmarks in complex target spaces, XtalPi has built a reproducible innovation model that turns deep know-how into high-value clinical assets. Underpinned by a milestone-sharing structure, this model tightly aligns the platform’s evolution with clinical success, quickly translating biological insights into tangible impact for partners and patients around the world.
Dr. Shuhao Wen, Chairman of XtalPi commented, "The clinical progress of PEP08 and the ongoing collaboration of the second project are testaments to the synergy between our teams, and highlights the reliability of XtalPi’s R&D platform in tackling complex targets. We look forward to further applying this model to deliver high-quality pipeline assets for our partners and generate sustained value for our shareholders."
"PharmaEngine has been advancing its R&D capabilities, and our collaboration with XtalPi exemplifies our ability to harness innovative technologies to propel next-generation discoveries in precision oncology," said Dr. Hong-Ren Wang, CEO and President of PharmaEngine. "XtalPi’s R&D platform played a key role in the early-stage discovery of PEP08, providing a robust foundation for its clinical entry. Our collaboration of PEP08 and the second project demonstrates our ongoing efforts to advance cancer treatment development worldwide.
About PharmaEngine, Inc.
PharmaEngine, Inc. (4162.TWO), headquartered in Taipei, began operations in February 2003. PharmaEngine focuses on new drug development by adopting "Virtual Pharmaceutical Company Business Model". PharmaEngine has one commercial product, ONIVYDE®, which is currently approved for the treatment of adult patients with metastatic pancreatic adenocarcinoma. In addition, PharmaEngine is advancing PEP07 (CHK1 inhibitor) and PEP08 (MTA-collaborative PRMT5 inhibitor) through Phase I clinical trials. Leveraging its extensive experience in drug development and project management, the Company aims to continue expanding its pipeline. PharmaEngine also pursues international collaborations and out-licensing agreements to accelerate the discovery, development, and commercialization of novel cancer therapies.
About XtalPi
XtalPi Holdings Limited (XtalPi, 2228.HK) was founded in 2015 by three physicists from the Massachusetts Institute of Technology (MIT). It is an innovative R&D platform powered by quantum physics, artificial intelligence, and robotics. By integrating first-principles calculations, AI algorithms, high-performance cloud computing, and standardized automation systems, XtalPi provides digital and intelligent R&D solutions for companies in the pharmaceutical, materials science, agricultural technology, energy, new chemicals, and cosmetics industries.
