Tyligand Bioscience Announces First Patient Dosed in Phase 1/2 Clinical Trial of TSN1611, a Selective and Orally Bioavailable KRAS G12D Inhibitor

SHANGHAI,May 24,2024 --Tyligand Bioscience,a clinical-stage biotechnology company focused on the discovery and development of innovative cancer therapies,announced that the first patient had been dosed in the Phase 1/2 trial of TSN1611 for the treatment of KRAS G12D mutant solid tumors in the United States. The program has been cleared for IND by U.S. FDA and China NMPA in Feb and April 2024,respectively.

TSN1611 is a highly selective and orally bioavailable small molecule targeting the G12D mutant of KRAS oncogene,with excellent enzymatic and cellular activities. It effectively engages both the ON-state (GTP-bound) and OFF-state (GDP-bound) of KRAS G12D. TSN1611 has demonstrated superior in vivo anti-tumor activity with a durable response across multiple animal models. TSN1611 features favorable physicochemical properties,oral pharmacokinetic profiles,and notable brain penetration potential to address a large unmet medical need.

The ongoing first-in-human,multi-center clinical trial (NCT06385925) is designed to assess the safety,tolerability,pharmacokinetic profile,and preliminary anti-tumor activity in patients with advanced solid tumors harboring the KRAS G12D mutation. Patient recruitment is currently underway in the United States,with plans to initiate in China in the coming months.

"Preclinical profile indicated the potential of TSN1611 as a best-in-class molecule for treating cancers driven by KRAS G12D," saidDr. Tony Zhang,PhD.,CEO of Tyligand Bioscience,"We are proud of our teams for the creativity,quality and speed in the discovery and early development efforts,and grateful for the support from our partners and investors in advancing TSN1611 one step closer toward the patients in need."

About Tyligand Bioscience:

Founded in 2018,Tyligand Bioscience is a clinical stage biotech focusing on the discovery and development of transformative therapies for cancer. In addition to the KRAS G12D program,the company has several molecules in development,including TSN084,a Type II multi-kinase inhibitor; TSN222,a first in kind dual acting tumor immune agonist (DATIA®),and a platform for antibody drug conjugates (ADCs) featuring proprietary linkers and novel payloads.For more information about Tyligand Bioscience,please visit www.tyligand.com.

KRAS mutations are the most common driver oncogenes,implicated in approximately 25% of all human cancers,with KRAS G12D emerging as a predominant isoform,which is particularly prevalent in pancreatic,colorectal,and non-small cell lung cancers. There exists an urgent need for effective therapies targeting KRAS G12D to improve patient outcomes.

CONTACT: Tyligand Bioscience,[email protected],https://www.tyligand.com