SHANGHAI,China,[April 16],2026–On April 16, 2026, Leadingtac Biopharmaceutical Co., Ltd. ( “Leadingtac”) announced that its independently developed oral KRAS-G12D degrader has officially received approval from the U.S. Food and Drug Administration (FDA).

 This approval marks the successful completion of the project’s Investigational New Drug (IND) application in the United States and its official entry into the clinical development phase, fully demonstrating Lingtai Biopharm’s comprehensive capabilities in innovative drug R&D and global regulatory submissions.

At the same time, Leadingtacthe company submitted an IND application to the Center for Drug Evaluation (CDE) of the National Medical Products Administration (NMPA) in early April 2026.

Dr. Feng Yan, Founder and CEO of Leadingtac, stated: “The FDA’s formal approval of the KRAS-G12D degrader for clinical trials represents a major breakthrough in our R&D journey and signifies that Leadingtac’s technological platform capabilities in the field of targeted protein degradation drugs have once again been recognized by an internationally authoritative body.

This achievement would not have been possible without the hard work and tireless efforts of every employee; it is a testament to our team’s long-term dedication to the field of targeted protein degradation therapeutics. At the same time, I would like to express my sincere gratitude to our investors for their trust and support, as well as to all our partners for their collaborative efforts. Without everyone’s joint efforts, we would not have been able to take this crucial step. Moving forward, we will accelerate our clinical development efforts with the goal of bringing effective, innovative therapies to patients with the KRAS-G12D mutation as soon as possible.”

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 oncogenic driver proteins at their source and more comprehensively block KRAS G12D-mediated abnormal signaling pathways, demonstrating development potential as a next-generation precision anticancer therapy. As one of the company’s key innovation projects in the oncology field, LT-010391 further enriches Leaingtac’s product pipeline in the field of targeted protein degradation therapy.

KRAS mutations are driver mutations in various types of cancer; specifically, the prevalence of the KRAS G12D mutation is 36% in pancreatic cancer, 12% in colorectal cancer, and 4% in non-small cell lung cancer. Consequently, there is a significant unmet clinical need for targeted therapies targeting KRAS mutations.

Recently published clinical data show that drugs targeting KRAS mutations have achieved significant efficacy. The efficacy data for Astellas’ KRAS G12D degrader ASP3082 (Setidegrasib) at a dose of 600 mg (administered once weekly) in 21 patients with pancreatic cancer (7 in second-line treatment and 14 in third-line treatment) are as follows: The overall response rate (ORR) was 24%, with a median duration of response (mDOR) of 4.2 months, median progression-free survival (mPFS) of 3.0 months, and median overall survival (mOS) of 10.3 months.

Revolution Medicines’ pan-RAS inhibitor RMC-6236 (Daraxonrasib) has yielded positive results in the Phase 3 RASolute 302 clinical trial for pancreatic cancer. Compared to the chemotherapy group, median overall survival (mOS) was 13.2 months versus 6.7 months, representing a 60% reduction in the risk of death. Several KRAS G12D small-molecule inhibitors are also currently in clinical development in China.

As the world’s first oral targeted protein degradation agent for KRAS G12D, 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, 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 Zhangjiang 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.