XTALPI Inc. (02228) has achieved a significant milestone as its incubated company Signet Therapeutics successfully secured a nomination for the 2025 Prix Galien USA Award, one of the highest honors in the international biopharmaceutical industry. The company's globally first diffuse gastric cancer targeted therapy, SIGX1094R, developed in collaboration with XTALPI, has been nominated for the "Best Biotechnology Product Award," making it the only Chinese biopharmaceutical company to receive this prestigious nomination.

According to public records, the last Chinese biopharmaceutical product to receive a Prix Galien Award nomination was BeiGene's BTK inhibitor Zanubrutinib. This year's Best Biotechnology Product Award features 16 nominated products from global pharmaceutical giants including Amgen, AstraZeneca, Johnson & Johnson, Pfizer, Merck, and Novartis.

**Breakthrough Innovation in Drug Discovery**

SIGX1094R represents a groundbreaking achievement as the world's first first-in-class targeted drug developed using an "organoid + AI" platform, specifically designed for diffuse gastric cancer treatment. The drug has received both Orphan Drug Designation (ODD) and Fast Track Designation (FTD) from the U.S. FDA and is currently undergoing Phase I clinical trials at Peking University Cancer Hospital.

**The "Nobel Prize of Pharmaceuticals"**

Established in 1970, the Prix Galien Award is renowned as the "Nobel Prize of Pharmaceuticals" and represents the highest honor in the pharmaceutical industry. The award emphasizes scientific innovation while focusing on the actual improvement value for human health. The U.S. Prix Galien Award ceremony, established in 2007, features particularly fierce competition with all awards evaluated by an authoritative review committee.

The 2025 review committee comprises 11 distinguished members, including three Nobel Prize laureates: Linda B. Buck, Stanley B. Pursier, and Phillip A. Sharp, along with renowned MIT scientist Robert S. Langer, Stanford University President Emeritus Marc Tessier-Lavigne, and former Gates Foundation CEO Susan Desmond-Hellmann.

Past winners in the Best Medical Product, Best Biotechnology Product, and Best Rare Disease Product categories over the past two years include Pfizer's global first COVID-19 oral medication PAXLOVID, AstraZeneca and Daiichi Sankyo's next-generation ADC HER2+ breast cancer therapy ENHERTU, Novo Nordisk's type 2 diabetes blockbuster semaglutide, and Bristol Myers Squibb's first drug specifically for obstructive hypertrophic cardiomyopathy, Camzyos.

**FDA Recognition and Clinical Progress**

The collaborative first-in-class drug pipeline SIGX1094R features an entirely new molecular scaffold and has received IND approval from both the FDA (June 2024) and China's NMPA (September 2024). The Phase I clinical trial at Peking University Cancer Hospital is progressing smoothly, with all patients in the fourth dose group fully enrolled for safety assessment.

With its significant innovation and excellent activity and safety data, SIGX1094R not only received FDA Orphan Drug Designation for gastric cancer but also won FDA Fast Track Designation in February 2025, potentially significantly shortening its time to market through accelerated approval, priority review, and rolling review policies.

**Addressing a Critical Medical Need**

Gastric cancer ranks as the fifth most common cancer globally and the fourth leading cause of cancer-related deaths (approximately 770,000 deaths). Nearly 50% of new gastric cancer cases worldwide occur in China. According to the latest data from China's National Cancer Center, gastric cancer ranks fifth in malignant tumor incidence and third in mortality in China.

Addressing this challenge, Signet Therapeutics established the first diffuse gastric cancer organoid disease model, first elucidated the mechanism of diffuse gastric cancer, and identified focal adhesion kinase (FAK) as a new target for diffuse gastric cancer, with findings published in Cancer Discovery.

**AI-Powered Drug Design Innovation**

In collaboration with XTALPI, the project achieved unprecedented speed, completing preclinical candidate compound (PCC) delivery in just six months. The entire process from new target discovery to IND approval took only three years, significantly faster than traditional drug development paradigms.

During the initial drug discovery and design phase for SIGX1094R, XTALPI utilized its AI + robotic drug discovery platform to simultaneously conduct target validation and lead compound discovery and optimization, designing a series of inhibitor molecule libraries targeting FAK and screening for molecules with optimal performance in FAK activity inhibition and drug-like properties.

However, evaluation in diffuse gastric cancer organoid models revealed that molecules with the strongest FAK inhibition activity were not necessarily the most efficacious, showing only partial correlation. This observation suggested the involvement of other targets.

**Breakthrough Discovery of Dual-Target Mechanism**

Using its proprietary Xpose algorithm to predict potential binding modes between molecules and targets, and XFEP (Free Energy Perturbation) algorithm to calculate molecular-target binding strength, XTALPI's team successfully identified SRC (FAK's synergistic protein) as a new potential target and experimentally validated the correlation between SRC activity and molecular efficacy.

This discovery first demonstrated that simultaneous inhibition of both FAK and SRC targets provides superior synergistic effects compared to single-target inhibition. FAK and its key binding factor SRC form complexes that activate downstream pathways. In drug development, single inhibition of either FAK or SRC can be compensatorily offset by the other, greatly reducing the drug's anti-tumor effects.

Based on this discovery, XTALPI designed a series of new candidate molecules using its AI + robotic platform that can simultaneously block FAK and SRC key signaling pathways. These molecules demonstrated superior efficacy in organoid models, overcoming the limitations of single-target inhibitors.

**Clinical Promise and Broad Therapeutic Potential**

SIGX1094R not only inhibits phosphorylated FAK but also inhibits phosphorylated SRC, blocking the activity of FAK/SRC complexes and related signaling pathways. Beyond treating diffuse gastric cancer, SIGX1094R has shown promise in preclinical studies for treating various cancers and demonstrated potential in combination therapies with KRAS inhibitors and EGFR inhibitors.

Currently in Phase I clinical trials at Peking University Cancer Hospital, SIGX1094R has demonstrated good safety performance in dose-escalation studies and shown preliminary anti-tumor activity. In the second dose group (12.5 mg, approximately 1/16 of the target dose of 200 mg), a patient with advanced lung metastases from malignant solid tumors achieved stable disease (SD) in two consecutive tumor assessments after SIGX1094R treatment, continuing medication for over nine weeks.

**Strategic Partnerships and Future Outlook**

Signet Therapeutics founder Dr. Zhang Haisheng stated: "We are honored that SIGX1094R, as the world's first drug based on 'organoid + AI' technology to enter clinical stages, has received Prix Galien Award nomination. This represents high recognition from top international experts of our research capabilities and authoritative certification of the organoid + AI development model."

XTALPI Chairman Dr. Wen Shuhao commented: "SIGX1094R represents XTALPI's earliest de novo drug discovery project, and receiving recognition from the top Prix Galien review panel is tremendously exciting. As a source innovation platform, XTALPI not only collaborates deeply with leading global pharmaceutical companies but also actively empowers and accelerates the transformation of cutting-edge scientific progress into pipeline assets and clinical applications."

**Industry Leadership and Record-Breaking Partnerships**

As the first "18C stock" and "AI + robotics first stock" on the Hong Kong Stock Exchange, XTALPI has developed an intelligent autonomous R&D platform integrating quantum physics, AI, and large-scale high-precision robotic experiments, committed to creating vertical super artificial intelligence in life sciences and new materials.

As a pioneer in AI pharmaceuticals, XTALPI's clients include 16 of the world's top 20 pharmaceutical companies. In 2023, XTALPI signed a $250 million AI + robotic drug discovery collaboration with Eli Lilly, setting a record for the highest single-pipeline AI pharmaceutical collaboration in China at that time. In August 2025, XTALPI signed an AI drug development collaboration with DoveTree, an innovative biopharmaceutical company founded by legendary biotech entrepreneur Dr. Gregory Verdine, with a total order value of approximately HK$47 billion ($5.99 billion), again breaking AI drug development order records and receiving an initial payment of approximately HK$400 million ($51 million).

Currently, XTALPI is serving dozens of drug discovery projects, with multiple pipelines applying for or having already received approval to enter clinical trials.