Tyligand Bioscience Presents Latest Clinical Data of KRAS G12D Inhibitor TSN1611 at the 2026 ASCO GI

January 9, 2026 – Tyligand Bioscience presented the latest Phase I/II clinical research data of its independently developed KRAS G12D inhibitor TSN1611 in patients with advanced solid tumors as a poster presentation (Abstract 710) at the 2026 American Society of Clinical Oncology Gastrointestinal Cancers Symposium (ASCO GI). The data demonstrated that TSN1611 exhibited positive antitumor activity and a manageable safety profile in previously treated patients with advanced solid tumors, particularly in those with pancreatic ductal adenocarcinoma (PDAC).

Key Efficacy Data: Positive Clinical Activity Demonstrated in Second/Third-Line PDAC

KRAS G12D mutations are highly prevalent in gastrointestinal tumors such as pancreatic and colorectal cancers, for which effective precision targeted therapies remain lacking. As of December 11, 2025, a total of 23 patients with second/third-line PDAC who had completed at least one post-baseline tumor assessment at the recommended Phase II dose (RP2D, 1200 mg BID) were included in the efficacy analysis, and TSN1611 demonstrated clinically meaningful antitumor activity:

•   Objective Response Rate (ORR): Reached 30.4% (95% CI: 13.2, 52.9), with 7 patients achieving partial response (PR).
•   Disease Control Rate (DCR): Reached 82.6% (95% CI: 61.2, 95.0), with 12 patients achieving stable disease (SD).
•   Median Time to Response (TTR): 6.6 weeks (range: 5.6–18 weeks).

These preliminary results indicate that TSN1611 possesses encouraging therapeutic potential in patients with KRAS G12D-mutant PDAC who have failed prior treatments.

Safety and Pharmacokinetics: Adequate Target Inhibition with Manageable Safety

This analysis included a total of 111 patients across various dose cohorts (of which 57 received treatment at the 1200 mg BID dose).

TSN1611 demonstrated favorable overall safety and tolerability. No Grade 4 or 5 treatment-related adverse events (TRAEs) were observed in the study. In the 1200 mg BID dose cohort:

•   The incidence of Grade 3 TRAEs was 8.8%.
•   The rate of treatment discontinuation due to TRAEs was 0.

The most common TRAEs were primarily gastrointestinal-related adverse reactions, including diarrhea, nausea, and vomiting, the majority of which could be effectively managed through routine supportive care, prophylactic management, and dose modification. Pharmacokinetic (PK) and pharmacodynamic (PD) results further supported the rationale for the RP2D. TSN1611 reached steady-state plasma concentrations after 8 days of continuous dosing, with no significant drug accumulation observed. Under the 1200 mg BID regimen, drug exposure reached high levels with low inter-patient variability. Notably, the steady-state trough concentration at this dose was approximately 7-fold the IC90 of p-ERK, indicating a sustained and profound capacity for target pathway inhibition.

About TSN1611

TSN1611 is a highly selective oral KRAS G12D inhibitor independently developed by Tyligand Bioscience. KRAS G12D mutations are highly enriched in gastrointestinal tumors such as pancreatic and colorectal cancers, representing a clear unmet clinical need.

TSN1611 utilizes a differentiated molecular design that can simultaneously bind and inhibit both the active (GTP-bound) and inactive (GDP-bound) states of the KRAS G12D protein, aiming to achieve more sustained and comprehensive inhibition of the KRAS signaling pathway. Currently, TSN1611 is undergoing multi-center Phase I/II clinical trials in China and the United States, with continuous enrollment in the Phase II expansion cohorts. Based on the observed single-agent activity and favorable safety window, Tyligand Bioscience is steadily advancing the monotherapy development of TSN1611 and actively exploring its potential in combination treatment strategies. The goal is to establish a platform-based therapeutic layout around the KRAS G12D target, providing more innovative treatment options for patients.