Tyligand Bioscience Presents the Latest Data for TSN1611 in KRAS G12D-Mutated Non-Small Cell Lung Cancer at the 2026 ASCO Rapid Oral Abstract Session

CHICAGO, May 30, 2026 – Tyligand Bioscience presented the latest Phase I/II clinical data for its oral KRAS G12D inhibitor, TSN1611, at the Rapid Oral Abstract Session of the 2026 American Society of Clinical Oncology (ASCO) Annual Meeting. This presentation focuses on the advanced non-small cell lung cancer (NSCLC) cohort harboring the KRAS G12D mutation, with data showing promising antitumor activity and a manageable safety profile.

Efficacy: Overall DCR Approaching 90%, with Excellent First-Line and Intracranial Activity Signals, 80% ORR in First-Line Evaluable Patients, and Intracranial Antitumor Activity Observed

The study demonstrated the efficacy of TSN1611 across different prior treatment lines in patients with NSCLC. In the 600-1200 mg BID dose cohorts, 27 patients had post-baseline tumor evaluations:

• •   Overall Efficacy (including 1L and previously treated patients): The objective response rate (ORR) of the overall cohort reached 44.4% (12/27), and the disease control rate (DCR) reached 88.9% (24/27). Among 5 patients who had not received prior systemic treatment, TSN1611 showed encouraging activity, achieving an ORR of 80% (4/5) and a DCR of 100% (5/5). These early results warrant further validation in a larger patient population.

Tumor responses were rapid and durable. The median time to response (TTR) was 1.4 months, and the median duration of response (DOR) reached 8.4 months.

Addressing the highly challenging brain metastases in NSCLC, marked shrinkage of intracranial lesions was observed as early as one month after TSN1611 treatment in patients with brain metastases, suggesting intracranial antitumor activity of TSN1611.

Safety Profile: Favorable Overall Tolerability with No Grade 3 or Higher Hepatotoxicity

The safety analysis included 42 NSCLC patients treated across various dose levels:

• •   Overall TRAE Rate: 38 patients (90.5%) experienced treatment-related adverse events (TRAEs). The majority of these events were Grade 1 to 2.
• •   High-Grade Risk Control: The incidence of Grade 3 TRAEs was 21.4% (9/42). No Grade 4 or 5 TRAEs occurred, and there were no treatment discontinuations due to TRAEs.
• •   No ≥ Grade 3 Hepatotoxicity: TSN1611 showed a manageable safety profile regarding hepatotoxicity, a common concern with targeted therapies. Data showed that all liver function-related fluctuations (such as ALT increased or AST increased) remained within the mild Grade 1 to 2 range. No Grade 3 or higher hepatotoxicity events were observed throughout the study. The overall safety profile supports continued dosing and further exploration in combination regimens.

Key Clinical Observations

Based on the oral presentation at the ASCO Annual Meeting, TSN1611 demonstrates the following key clinical characteristics:

1. Consistent Benefit Across Multiple Lines: TSN1611 demonstrated promising antitumor activity in NSCLC, regardless of prior treatment lines.
2. Intracranial Activity: TSN1611 demonstrated rapid shrinkage of brain metastases in NSCLC patients, highlighting its differentiated clinical value compared to other compounds in the class.
3. Favorable Safety and Tolerability: A favorable safety profile of TSN1611 supports tolerability and facilitates future combination regimens.

As a core pipeline asset prioritized for clinical development by Tyligand Bioscience, the oral presentation of TSN1611 at the ASCO Annual Meeting not only serves as a critical validation of the company's R&D capabilities but also marks a solid step forward in the field of KRAS targeted therapies. Based on its observed single-agent activity, intracranial activity signals, and favorable safety profile observed to date, the company is steadily advancing enrollment in its monotherapy expansion cohorts and actively exploring a platform-based combination therapy strategy centered around this molecule, aiming to provide competitive targeted treatment options for patients with KRAS G12D-mutated solid tumors.