NKT-3447

- NKT3964 is a first-in-class, highly potent and selective CDK2 degrader, and causes prolonged CDK2 pathway inhibition without cyclin E accumulation - NKT3964 is designed to treat patients with cyclin E driven cancers WILMINGTON, Del.--(BUSINESS WIRE)--NiKang Therapeutics ® Inc. (“NiKang”) is a clinical stage biotech company focused on developing innovative small molecule oncology medicines to bring transformative therapies to patients in need. The company announced today the unveiling of NKT3964 at the EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics (“Triple Meeting”) during a Poster Spotlight Session. The conference is being held October 23-25, 2024, in Barcelona, Spain. NKT3964 is a first-in-class, orally bioavailable small molecule CDK2 degrader that selectively degrades CDK2, demonstrating high specificity over CDK1 and other CDK family members. Its high potency and unique mechanism of action result in sustained inhibition of CDK2 pathway without causing cyclin E accumulation. NKT3964 is designed to treat patients with aberrant CDK2/cyclin E pathway activation, including those with ovarian, endometrial, gastric and HR+HER2- breast cancers. NiKang has initiated a phase 1, open-label, dose escalation study of NKT3964 as a single agent. This first-in-human study (NCT06586957) is designed to evaluate the safety, tolerability, pharmacokinetics and preliminary anti-tumor activity to determine the preliminary recommended dose for expansion of NKT3964 in adults with advanced or metastatic solid tumors. “We are excited to share the discovery of NKT3964, a first-in-class oral CDK2 degrader at this year’s Triple Meeting,” said Zhenhai Gao, Ph.D., co-founder, president, and CEO of NiKang. “This is the second of three programs targeting the cell cycle (CDK2 inhibitor NKT3447, CDK2 degrader NKT3964, and a CDK2/4 selective dual degrader) that we have advanced to the clinic. We believe CDK2 plays a critical role in driving tumor growth. Recent clinical data presented at ESMO further validates CDK2 as a key oncology target. We are developing a cutting-edge portfolio of CDK2 and CDK2/4 degraders that can achieve sustained CDK pathway inhibition while avoiding paradoxical cyclin E increase. Our multi-pronged approach allows us to thoroughly and deeply interrogate this pathway. We look forward to exploring NKT3964’s potential in treating patients with advanced or metastatic solid tumors.” Poster Presentation Details: Title: Discovery of NKT3964: a first-in-class, highly potent and selective, orally bioavailable CDK2 PROTAC degrader for cancer therapy Presenter: Jianlin Geng, Ph.D. Abstract Number: PB002 Session: Posters in the Spotlight Date/Time: 2:00 p.m.-2:40 p.m. CEST on October 24, 2024 About NKT3964 NKT3964 is a first-in-class, highly potent and selective, orally bioavailable CDK2 PROTAC degrader, causing prolonged CDK2 pathway inhibition without cyclin E accumulation. It has the potential to maximally inhibit the CDK2 pathway, fully harnessing the therapeutic benefits of CDK2 inhibition. NKT3964 is currently under evaluation in a Phase 1 clinical study in advanced or metastatic solid tumors as a single agent (NCT06586957). About NiKang Therapeutics NiKang Therapeutics is a clinical-stage biotech company focused on discovering and developing innovative small molecule oncology medicines to bring transformative therapies to patients in need. 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. 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 have successfully advanced three programs into clinical trials, including NKT2152 (HIF2α), NKT3447 (CDK2), and NKT3964 (CDK2). For more information, please visit Contacts Kelsey Chen Chief Financial and Operating Officer IR@nikangtx.com

- Highly selective and unique cyclin E-reducing CDK2 inhibitor designed to treat patients with cyclin E amplified cancers being evaluated in patients with selected solid tumors driven by cyclin E or CDK2 - 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). NKT3447 is designed to treat patients with cancers driven by cyclin E amplification or overexpression, which is present in many different tumor types. 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. “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. 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. 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.” “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.” About 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. 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. For more information, please visit