SHANGHAI, May 24, 2024 /PRNewswire/ -- 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.

上海，2024年5月24日/PRNewswire/--Tyligand Bioscience，一家专注于创新癌症疗法的发现和开发的临床阶段生物技术公司，宣布第一名患者已在TSN1611的1/2期试验中服用，用于治疗美国的KRAS G12D突变实体瘤。

The program has been cleared for IND by U.S. FDA and China NMPA in Feb and April 2024, respectively..

该计划已分别于2024年2月和4月获得美国FDA和中国NMPA的IND批准。。

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是一种高选择性和口服生物利用度的小分子，靶向KRAS癌基因的G12D突变体，具有优异的酶和细胞活性。它有效地参与了KRAS G12D的ON状态（GTP限制）和OFF状态（GDP限制）。TSN1611在多种动物模型中表现出优异的体内抗肿瘤活性和持久的反应。

TSN1611 features favorable physicochemical properties, oral pharmacokinetic profiles, and notable brain penetration potential to address a large unmet medical need..

TSN1611具有良好的理化性质，口服药代动力学特征以及显着的大脑渗透潜力，可满足大量未满足的医疗需求。。

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..

正在进行的首次人体多中心临床试验（NCT06385925）旨在评估携带KRAS G12D突变的晚期实体瘤患者的安全性，耐受性，药代动力学特征和初步抗肿瘤活性。美国目前正在招募患者，计划在未来几个月在中国启动。。

'Preclinical profile indicated the potential of TSN1611 as a best-in-class molecule for treating cancers driven by KRAS G12D,' said Dr. 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.'.

“临床前研究表明TSN1611是治疗KRAS G12D驱动的癌症的最佳分子，”Tony Zhang博士说。，Tyligand Bioscience首席执行官：“我们为我们的团队在发现和早期开发工作中的创造力、质量和速度感到骄傲，并感谢我们的合作伙伴和投资者的支持，使TSN1611更接近需要帮助的患者。”。

About Tyligand Bioscience:

关于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.

Tyligand Bioscience成立于2018年，是一家临床阶段的生物技术公司，专注于癌症转化疗法的发现和开发。除了KRAS G12D计划外，该公司还在开发几种分子，包括II型多激酶抑制剂TSN084；TSN222是第一种双作用肿瘤免疫激动剂（DATIA®），是一种抗体-药物偶联物（ADC）平台，具有专有接头和新型有效载荷。

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..

KRAS突变是最常见的驱动癌基因，约占所有人类癌症的25%，其中KRAS G12D是主要的同工型，在胰腺癌，结直肠癌和非小细胞肺癌中尤为普遍。迫切需要针对KRAS G12D的有效疗法来改善患者预后。。