Tyligand Bioscience Begins Dosing for Phase 1/2 Trial of KRAS G12D Inhibitor TSN1611

Tyligand Bioscience, a clinical-stage biotechnology firm dedicated to pioneering cancer treatments, has commenced dosing the first patient in its Phase 1/2 trial of TSN1611 for KRAS G12D mutant solid tumors in the United States. This trial follows the clearance for Investigational New Drug (IND) applications by the U.S. FDA and China NMPA in early 2024.

TSN1611 is a selective, orally available small molecule that targets the KRAS G12D mutation, demonstrating potent enzymatic and cellular activities. It interacts with both the active (GTP-bound) and inactive (GDP-bound) states of the KRAS G12D protein. Preclinical studies have shown that TSN1611 offers significant anti-tumor activity with lasting effects in various animal models. The molecule also displays favorable physicochemical characteristics, effective oral pharmacokinetics, and the ability to penetrate the brain, addressing a significant unmet medical need.

The first-in-human, multi-center clinical trial (NCT06385925) aims to evaluate the safety, tolerability, pharmacokinetic profile, and preliminary anti-tumor efficacy of TSN1611 in patients with advanced solid tumors harboring the KRAS G12D mutation. Patient enrollment is currently ongoing in the United States, with plans to expand recruitment to China in the near future.

Dr. Tony Zhang, CEO of Tyligand Bioscience, highlighted the potential of TSN1611 as a leading treatment for KRAS G12D-driven cancers. He acknowledged the dedication and innovation of the company's team in advancing the drug from discovery to early development stages and expressed gratitude to partners and investors for their support in bringing TSN1611 closer to patients.

Established in 2018, Tyligand Bioscience is committed to developing transformative cancer therapies. Beyond the KRAS G12D program, the company is working on several other promising compounds, including TSN084, a Type II multi-kinase inhibitor; TSN222, a dual-acting tumor immune agonist (DATIA®); and a platform for antibody-drug conjugates (ADCs) with unique linkers and novel payloads.

KRAS mutations are among the most prevalent driver oncogenes in human cancers, contributing to about 25% of all cases. The KRAS G12D mutation, in particular, is frequently found in pancreatic, colorectal, and non-small cell lung cancers. There is a pressing need for effective treatments targeting KRAS G12D to improve patient outcomes.

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