June 11, 2026, Leadingtac Biopharmaceutical Co., Ltd. ( “Leadingtac”)announced that LT-010391, the company’s independently developed, globally first-in-class oral KRAS G12D-targeted protein degrader, has officially received clinical trial (IND) approval from the Center for Drug Evaluation (CDE) of the National Medical Products Administration (NMPA) of China. It is the only oral KRAS G12D degrader in China to have entered the clinical stage. Previously, LT-010391 had received Investigational New Drug (IND) approval from the U.S. Food and Drug Administration (FDA) on April 16, 2026.

The successful implementation of a global R&D strategy for LT-010391—featuring simultaneous submissions and approvals in both China and the United States, as well as concurrent clinical development—not only serves as strong evidence of Leadingtac’s core R&D capabilities but also marks a major milestone in the development of domestically developed PROTAC innovative drugs and drugs targeting the highly challenging KRAS pathway in China. This signifies that domestically developed innovative drugs are now officially taking on the global challenge of treating high-incidence, treatment-resistant solid tumors with the KRAS G12D mutation, bringing new hope for treatment to cancer patients worldwide.

Dr. Feng Yan, Founder and CEO of Leadingtac, stated: “We are delighted that LT-010391 has successively received clinical trial approvals from the U.S. FDA and China’s CDE. This is not only a significant achievement resulting from the company’s deep commitment to cutting-edge PROTAC technology and focus on major clinical needs, but also marks the official entry of China’s first-in-class, domestically developed oral KRAS G12D PROTAC drug into the global first tier.

Moving forward, the company will continue to strengthen the advantages of our protein degradation drug R&D platform, consistently delivering more globally first-in-class and differentiated innovative drugs. This will contribute to the high-quality innovative development of China’s biopharmaceutical industry and enhance the global competitiveness of domestically developed innovative drugs.”

About the KRAS-G12D degrader

LT-010391 is an innovative oral protein degrader targeting KRAS G12D, independently developed by Leadingtac, intended for the treatment of patients with advanced solid tumors harboring the KRAS G12D mutation. Leveraging its protein degradation mechanism, LT-010391 is expected to eliminate the oncogenic driver protein at its source and more comprehensively block the abnormal signaling pathways mediated by KRAS G12D, demonstrating development potential as a new-generation precision anticancer therapy. As one of the company’s key innovation projects in the oncology field, LT-010391 further enriches Leadingtac’s product pipeline in the field of targeted protein degradation therapy.

As one of the most common driver mutations in human tumors, KRAS gene mutations account for approximately 25% of all cancer cases, with particularly high prevalence in pancreatic ductal adenocarcinoma (37%), colorectal cancer (13%), and non-small cell lung cancer (NSCLC, 4%). Among these, the G12D mutation is the most common KRAS subtype; however, due to the lack of traditional drug-binding sites in its protein structure, it has been considered an “undruggable” target for the past 40 years. Nevertheless, with recent clinical breakthroughs, targeted therapy for KRAS G12D is undergoing a historic turning point, and EvaluatePharma predicts that the clinical demand for such treatments will reach $12 billion by 2035.

Following the release of Phase 2 clinical data for the weekly injection of the KRAS G12D PROTAC drug ASP3082 (Setidegrasib), Astellas initiated a Phase 3 clinical trial in March 2026 to evaluate ASP3082 for the treatment of KRAS G12D-mutated metastatic and locally advanced non-small cell lung cancer (NSCLC) and pancreatic ductal adenocarcinoma (PDAC). and on April 15, 2026, announced the first-in-patient dosing for the global Phase 3 clinical trial in patients with KRAS G12D-mutated metastatic pancreatic cancer.

As the world’s first oral targeted protein degrader for KRAS G12D, LT-010391 is expected to eliminate the cancer-driving protein at its source and more comprehensively block KRAS G12D-mediated abnormal signaling pathways, delivering more durable benefits to patients.

About Leadingtac:

A clinical-stage biopharmaceutical company, Leadingtac has rapidly emerged as a leader in China's Target Protein Degradation (TPD) drug discovery field since its founding in 2019. The company maintains advanced R&D centers in Shanghai and Shaoxing, Zhejiang—China's core hubs for innovative drug development. The company focuses its R&D efforts on the cutting-edge field of Target Protein Degradation (TPD) and has independently developed the highly efficient, versatile SPUD® (Specific Protein Ubiquitination and Degradation) technology platform. This platform enables rapid execution of multiple critical screenings, including:

Nano-SPUD® for Target Proteins: For target protein degradation activity screening.

Nano-SPUD® for E3 Ligases: For screening novel E3 ligase ligands.

Lyso-SPUD® for Lysosome: For activity screening of lysosome-dependent degradation (LYTAC).

Leadingtac has strategically targeted multiple “hard-to-drug” targets using this platform. Its first pipeline candidate, an IRAK4 degradator for autoimmune diseases, holds significant market potential. It has received FDA and CDE approval for clinical trials, completed Phase I healthy subject dose escalation studies, and is currently expanding into indications including atopic dermatitis and hidradenitis suppurativa. Subsequent pipelines target hard-to-drug targets such as KRAS and STAT, aiming to tackle major diseases including lung cancer, pancreatic cancer, and colorectal cancer, with R&D progress leading globally.