NiKang Unveils NKT3964, a Potent Oral CDK2 PROTAC Degrader for Cancer, at EORTC-NCI-AACR 2024

NiKang Therapeutics Inc., a clinical-stage biotechnology company, has introduced NKT3964, an innovative small molecule aimed at treating cancers driven by cyclin E. This breakthrough was presented at the EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics in Barcelona, Spain, from October 23-25, 2024. NKT3964 stands out as an orally bioavailable CDK2 degrader, exhibiting a high degree of specificity for CDK2 while showing minimal effects on CDK1 and other related kinases.

NKT3964's unique mechanism allows for prolonged inhibition of the CDK2 pathway without the adverse effect of cyclin E accumulation, which is a significant advancement in cancer therapy. This molecule is particularly targeted at cancers with abnormal CDK2/cyclin E pathway activation, including ovarian, endometrial, gastric, and HR+HER2- breast cancers.

The company has commenced a phase 1, open-label, dose escalation study of NKT3964 to assess its safety, tolerability, pharmacokinetics, and preliminary anti-tumor efficacy. This first-in-human study aims to establish the recommended dose for further expansion in adults with advanced or metastatic solid tumors. The clinical trial (NCT06586957) will provide critical insights into the potential of NKT3964 as a therapeutic agent.

Dr. Zhenhai Gao, co-founder, president, and CEO of NiKang, expressed excitement about presenting NKT3964 at the Triple Meeting. He highlighted that this degrader is part of NiKang's broader strategy, which includes other advanced programs like the CDK2 inhibitor NKT3447 and a CDK2/4 selective dual degrader. Dr. Gao emphasized the significant role of CDK2 in tumor growth and referenced recent clinical data that reinforce CDK2 as a crucial target in oncology. The company's portfolio aims to achieve sustained inhibition of the CDK pathway while avoiding an increase in cyclin E, adopting a comprehensive approach to cancer treatment. Dr. Gao looks forward to exploring the potential of NKT3964 in patients with advanced or metastatic solid tumors.

The details of the poster presentation at the symposium were as follows:
- Title: Discovery of NKT3964: a first-in-class, highly potent and selective, orally bioavailable CDK2 PROTAC degrader for cancer therapy
- Presenter: Dr. Jianlin Geng
- Abstract Number: PB002
- Session: Posters in the Spotlight
- Date/Time: 2:00 p.m.-2:40 p.m. CEST on October 24, 2024

NKT3964 is a first-in-class, highly potent and selective, orally bioavailable CDK2 PROTAC degrader. It effectively inhibits the CDK2 pathway for an extended period without causing cyclin E accumulation. This characteristic is vital for maximizing the therapeutic benefits of CDK2 inhibition. Currently, NKT3964 is being evaluated in a Phase 1 clinical study involving patients with advanced or metastatic solid tumors.

NiKang Therapeutics is dedicated to the discovery and development of innovative small molecule oncology treatments. Their approach integrates deep insights into disease biology and molecular pathways with structure-based drug design, enabling the rapid and efficient advancement of proprietary drug candidates with desirable pharmacological profiles into clinical trials. NiKang has successfully moved three programs into clinical trials, including NKT2152 targeting HIF2α, NKT3447 targeting CDK2, and the newly introduced NKT3964 targeting CDK2.

NiKang's commitment to transforming cancer therapy through innovative solutions continues to push the boundaries of what's possible in oncology, bringing hope to patients with severe unmet medical needs. The introduction of NKT3964 marks a significant milestone in their ongoing efforts to develop cutting-edge treatments for challenging cancers.