NiKang Therapeutics Presents the Discovery and Unique Mechanism of Action of a Selective CDK2 Inhibitor NKT3447 at AACR Annual Meeting 2024

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NKT3447 is an orally bioavailable small molecule CDK2 inhibitor that exhibits high selectivity against CDK1 and other CDKs, prolonged pharmacodynamic effects, and a distinct mechanism of action.

Metadata
Provider: 
Business Wire, Inc.Business Wire, Inc.
Retrieved on: 
Friday, April 5, 2024
Information
Tags: 
Oncology, Health, Other Science, Clinical Trials, Research, Science, Biotechnology, CDK1, Phosphorylation, CDK2, CDK, Patient, Cell cycle, AACR, Therapy, Cancer, Safety, Pharmacokinetics, Cyclin E, Pharmaceutical industry
Geotags: 
UNITED STATES, NORTH AMERICA, CALIFORNIA, DELAWARE
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Organisation: 
NIKANG THERAPEUTICS, NIKANG THERAPEUTICS INC.
Summary
Key Points: 
  • NKT3447 is an orally bioavailable small molecule CDK2 inhibitor that exhibits high selectivity against CDK1 and other CDKs, prolonged pharmacodynamic effects, and a distinct mechanism of action.
  • It downregulates cyclin E and suppresses activating phosphorylation of CDK2 on Thr160.
  • “We are pleased to share the discovery of NKT3447, a highly selective CDK2 inhibitor with unique properties, at the AACR Annual Meeting”, said Zhenhai Gao, Ph.D., co-founder, president, and CEO of NiKang.
  • Discovery of a selective slow-off CDK2 inhibitor NKT3447 with distinct features of suppressing CDK2, downregulating cyclin E, and achieving prolonged pathway inhibition


NiKang Therapeutics Inc. (“NiKang”), a clinical stage biotech company focused on developing innovative small molecule oncology medicines to help patients with unmet medical needs, announced today the unveiling of NKT3447 at the American Association for Cancer Research (AACR) Annual Meeting 2024. NKT3447 is an orally bioavailable small molecule CDK2 inhibitor that exhibits high selectivity against CDK1 and other CDKs, prolonged pharmacodynamic effects, and a distinct mechanism of action. It downregulates cyclin E and suppresses activating phosphorylation of CDK2 on Thr160.

“We are pleased to share the discovery of NKT3447, a highly selective CDK2 inhibitor with unique properties, at the AACR Annual Meeting”, said Zhenhai Gao, Ph.D., co-founder, president, and CEO of NiKang. “This is the first of three programs targeting the cell cycle that we are expecting to bring to clinic. We have strong conviction in CDK2 as an oncology target and have built an industry-leading potential best in class and/or first in class portfolio that also includes a CDK2-selective degrader and a CDK2/4 dual degrader. Despite clinical success with drugs targeting the cell cycle, it has been challenging to identify inhibitors of CDK2 which have sufficient selectivity against CDK1, and which do not cause a compensatory increase of cyclin E. We have developed a platform to bring unique and selective drugs targeting CDK2 which address these challenges to clinic. We appreciate the opportunity to share the unique properties of NKT3447 and are enthusiastic about exploring the potential of NKT3447 in treating various cancers driven by CDK2 and cyclin E.”

NiKang has initiated a phase 1/1b, open-label, dose escalation and expansion study of NKT3447 as a single agent. This first-in-human study (NCT06264921) is designed to evaluate the safety, tolerability, pharmacokinetics, pharmacodynamics and clinical activity of NKT3447, administered orally, in adult patients with advanced or metastatic solid tumors.

Poster Presentation Details:

Title:

  

Discovery of a selective slow-off CDK2 inhibitor NKT3447 with distinct features of suppressing CDK2, downregulating cyclin E, and achieving prolonged pathway inhibition

Presenter:

  

Ke Liu, Ph.D.

Abstract Number:

  

5705/5 (link to abstract)

Session:

  

Pharmacologic Targeting of Cell Cycle Proteins

Date/Time:

   1:30 - 5:00pm PT on April 9, 2024

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 http://www.nikangtx.com

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