WILMINGTON, Del.--(BUSINESS WIRE)--NiKang Therapeutics Inc. (“NiKang”) is a clinical stage biotech company focused on developing innovative small molecule oncology medicines to help patients with unmet medical needs. The Company announced today that the first patient has been dosed in a phase 1/1b, open-label, first-in-human dose escalation and expansion study of single agent NKT3447, a small molecule that inhibits cyclin-dependent kinase 2 (CDK2).

威尔明顿，Del。--（商业新闻短讯）--尼康治疗公司（“尼康”）是一家临床阶段的生物技术公司，专注于开发创新的小分子肿瘤药物，以帮助未满足医疗需求的患者。该公司今天宣布，第一名患者已在1/1b期开放标签中服用单药NKT3447（一种抑制细胞周期蛋白依赖性激酶2（CDK2）的小分子）的首次人体剂量递增和扩展研究。

NKT3447 is designed to treat patients with cancers driven by cyclin E amplification or overexpression, which is present in many different tumor types..

NKT3447旨在治疗由细胞周期蛋白E扩增或过表达驱动的癌症患者，这种肿瘤存在于许多不同的肿瘤类型中。。

The Phase 1/1b trial (NCT06264921) is designed to evaluate the safety, tolerability, pharmacokinetics, pharmacodynamics and clinical activity of NKT3447 in adult patients with advanced or metastatic solid tumors driven by cyclin E or CDK2.

1/1b期试验（NCT06264921）旨在评估NKT3447在由细胞周期蛋白E或CDK2驱动的晚期或转移性实体瘤成年患者中的安全性，耐受性，药代动力学，药效学和临床活性。

“The initiation of dosing in this study marks a major milestone for NiKang, as NKT3447 is the first of our pipeline programs targeting the cell cycle to begin clinical evaluation,” said Zhenhai Gao, Ph.D., co-founder, president, and CEO of NiKang. “We have strong conviction that CDK2 is a key oncology target and have taken a holistic approach to build an industry-leading portfolio that also includes a CDK2-selective degrader and a CDK2/4 dual degrader.

尼康联合创始人、总裁兼首席执行官高振海博士表示：“这项研究的开始标志着尼康的一个重要里程碑，因为NKT3447是我们针对细胞周期开始临床评估的第一个管道项目。”。“我们坚信CDK2是一个关键的肿瘤学目标，并采取了整体的方法来建立一个行业领先的组合，其中还包括CDK2选择性降解剂和CDK2/4双重降解剂。

While there has been clinical success with drugs targeting the cell cycle, it has been challenging to identify inhibitors of CDK2 that spare CDK1 and do not cause a compensatory increase of cyclin E which is a driver of tumor cell proliferation. NKT3447 binds inactive monomeric CDK2, disrupting the CDK2/cyclin E complex without impacting CDK1.

虽然靶向细胞周期的药物在临床上取得了成功，但鉴定CDK2抑制剂具有挑战性，这些抑制剂可以替代CDK1，并且不会引起细胞周期蛋白E的补偿性增加，而细胞周期蛋白E是肿瘤细胞增殖的驱动因素。NKT3447结合无活性的单体CDK2，破坏CDK2/细胞周期蛋白E复合物而不影响CDK1。

Furthermore, its interaction with CDK2 results in suppression of activating phosphorylation of CDK2 on Thr160 and a substantial downregulation of cyclin E, potentially preventing a mechanism of resistance.”.

此外，它与CDK2的相互作用导致抑制Thr160上CDK2的活化磷酸化和细胞周期蛋白E的显着下调，可能阻止耐药机制。”。

“We are excited to initiate clinical trials of NKT3447, which has unique features that have led to sustained pharmacodynamic effects and significant anti-tumor activity in various cyclin E amplified tumor models,” said Joanne Jenkins Lager, M.D., Chief Medical Officer of NiKang. “CDK2 and cyclin E are deregulated in many human cancers, and we believe NKT3447 has the potential to change the standard of care for people with cyclin E amplified or overexpressing cancers including ovarian cancer, endometrial cancer and gastric cancer.”.

尼康首席医学官乔安妮·詹金斯·拉格（JoanneJenkinsLager）医学博士说：“我们很高兴启动NKT3447的临床试验，NKT3447具有独特的功能，可以在各种细胞周期蛋白E扩增的肿瘤模型中产生持续的药效学作用和显着的抗肿瘤活性。”。“CDK2和细胞周期蛋白E在许多人类癌症中失调，我们认为NKT3447有可能改变细胞周期蛋白E扩增或过度表达癌症（包括卵巢癌，子宫内膜癌和胃癌）患者的护理标准。”。

About NiKang Therapeutics

关于NiKang Therapeutics

NiKang Therapeutics is a clinical stage biotech company focused on discovering and developing innovative small molecule oncology medicines to help patients with unmet medical needs. Our target selection is driven by deep insight into disease biology and molecular pathways. Our discovery approach is informed by target structure biology and capitalizes on structure-based drug design.

NiKang Therapeutics是一家临床阶段的生物技术公司，专注于发现和开发创新的小分子肿瘤药物，以帮助未满足医疗需求的患者。我们的目标选择是由对疾病生物学和分子途径的深入了解驱动的。我们的发现方法由目标结构生物学提供信息，并利用基于结构的药物设计。

The successful implementation of our strategy enables us to rapidly and efficiently discover and advance proprietary drug candidates with the most desirable pharmacological features into clinical studies. We strive to bring transformative medicines to patients in need..

我们策略的成功实施使我们能够快速有效地发现并将具有最理想药理学特征的专有候选药物推进临床研究。我们努力为有需要的患者带来变革性药物。