On July 7, 2026, Leadingtac Pharmaceutical Co., Ltd. ( “Leadingtac”) announced that LT-010391, a small-molecule drug targeting KRAS G12D protein degradation independently developed by the company for the treatment of advanced solid tumors, had successfully completed the enrollment of the first patient and the first administration of the drug in its Phase I clinical trial, with good safety profiles.

This LT-010391 human trial is a multicenter, open-label Phase I/II study conducted in patients with advanced solid tumors harboring the KRAS G12D mutation. The study consists of two parts: a Phase I dose-escalation and pharmacokinetic (PK) expansion phase, and a Phase II cohort expansion phase. The Phase I portion includes Part A (dose escalation) and Part B (PK expansion). The core objectives of the study are to determine the maximum tolerated dose (MTD) and the recommended Phase II dose (RP2D) of LT-010391 as a monotherapy, while simultaneously conducting a preliminary assessment of the drug’s safety, tolerability, antitumor efficacy, and pharmacokinetic characteristics; The Phase II study will conduct a cohort expansion study of the drug as a monotherapy in patients with KRAS G12D-mutation-positive advanced solid tumors.

About the KRAS-G12D Degradant

LT-010391 is an innovative, orally administered protein degradant targeting KRAS G12D, independently developed by Lingtai Biotech, 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.

KRAS gene mutations are among the most common driver mutations in human tumors, accounting for approximately 25% of all cancer cases, and are particularly prevalent 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 absence 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.

As the world’s first-in-class oral targeted protein degrader for KRAS G12D, LT-010391 is expected to eliminate the oncogenic driver protein at its source, more comprehensively block KRAS G12D-mediated abnormal signaling pathways, and deliver more durable therapeutic 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.