On September 8, 2025 NiKang Therapeutics Inc. ("NiKang"), a clinical stage biotech company focused on developing innovative small molecule oncology medicines to bring transformative therapies to patients in need, reported the successful completion of dosing in the first cohort of its phase 1 dose-escalation study evaluating NKT5097 as a single agent (Press release, NiKang Therapeutics, SEP 8, 2025, View Source [SID1234655847]). NKT5097 is a first-in-class, orally bioavailable small molecule designed to selectively degrade CDK2 and CDK4 simultaneously, offering potential therapeutic benefits for patients with HR+ breast cancer and cancers with aberrant CDK2/cyclin E pathway activation.

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The Phase 1, open-label, dose escalation study (NCT07029399) is designed to assess the safety, tolerability, PK, PD and preliminary anti-tumor activity of NKT5097 in patients with advanced or metastatic solid tumors, with a focus on breast cancer and tumors with CCNE1 amplification. The study aims to determine the recommended dose(s) for future expansion cohorts.

"We are pleased to achieve this significant milestone expeditiously after IND clearance," said Zhenhai Gao, Ph.D., co-founder, president, and CEO of NiKang. "Initial PK data from the first cohort indicated favorable oral exposure consistent with human PK projections. In addition, initial PD data from the first cohort showed deep reduction of TKa level in HR+HER2- breast cancer patients previously treated with CDK4/6 inhibitors. NKT5097 has been well-tolerated to date. Due to its superior selectivity against CDK1 and CDK6, NKT5097 has the potential to mitigate neutropenia and/or diarrhea associated with existing CDK2 or CDK4/(6) inhibitors. These early findings underscore the potential of our dual degrader approach targeting both CDK2 and CDK4 – two key regulators of the cell cycle frequently dysregulated in various cancers including breast cancer. Our innovative, first-in-class CDK2/4 dual degrader holds the promise to replace currently approved CDK4/6 inhibitors as the new leader in treating HR+ breast cancer."

About NKT5097

NKT5097 is a first-in-class, highly potent and selective, orally bioavailable CDK2/4 dual degrader, designed to achieve simultaneous inhibition of the CDK2 and CDK4 pathway. By maximizing selective suppression of these pathways, NKT5097 has the potential to exploit the full therapeutic benefits of CDK2 and CDK4 inhibition. NKT5097 is currently under evaluation in a Phase 1 clinical study in advanced or metastatic solid tumors as a single agent (NCT07029399).