On October 24, 2024 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, reported the unveiling of NKT3964 at the EORTC-NCI-AACR (Free EORTC-NCI-AACR Whitepaper) Symposium on Molecular Targets and Cancer Therapeutics ("Triple Meeting") during a Poster Spotlight Session (Press release, NiKang Therapeutics, OCT 24, 2024, View Source [SID1234647389]). 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.

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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 (Free ESMO Whitepaper) 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).