The trial aims to determine the recommended dose(s) for the therapy’s expansion when used as a single agent in adults. Credit: Ground Picture/Shutterstock.
NiKang Therapeutics has concluded the first cohort dosing in the open-label Phase I trial of NKT3964 as a monotherapy for treating adults with advanced or metastatic solid tumours.
The dose-escalation trial is structured to assess the therapy’s tolerability, pharmacokinetics (PK), pharmacodynamics (PD), preliminary anti-tumour activity and safety.
It aims to determine the recommended dose(s) for the therapy’s expansion when used as a single agent in this patient group.
NiKang noted that the orally bioavailable small molecule NKT3964 selectively degrades cyclin-dependent kinase 2 (CDK2).
NiKang Therapeutics president, co-founder and CEO Zhenhai Gao said: “Completing dosing in our first cohort brings us one step closer to understanding the potential of this groundbreaking CDK2 degrader, one of several molecules in our portfolio targeting the cell cycle.
“Initial PK data from the first cohort demonstrated good oral exposure that aligns with human PK projections. Additionally, NKT3964 has achieved CDK2 degradation levels in patients that are consistent with those observed in preclinical in vivo studies.
“These early observations are particularly encouraging as they address the considerable challenges of achieving oral bioavailability with a proteolysis-targeting chimeras (PROTAC) degrader. These findings will help guide dose optimisation as the trial advances.”
It is designed to sustain inhibition of the CDK2 pathway without the accumulation of cyclin E, potentially offering therapeutic benefits for individuals with endometrial, gastric, and ovarian cancers, as well as hormone receptor (HR) + human epidermal growth factor receptor 2 (HER2)—breast cancers.
As a clinical-stage biotech company, NiKang develops small-molecule oncology medicines. Its portfolio includes three programmes, NKT2152, NKT3964, and NKT3447 that have progressed to trials.
The company’s approach to drug discovery is rooted in an understanding of the biology of the disease and molecular pathways, employing structure-based design.
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