Valuable Targets

What are CDK2 inhibitors and how do you quickly get the latest development progress?

16 November 2023
4 min read

CDK2, or cyclin-dependent kinase 2, is a crucial protein involved in cell cycle regulation in the human body. It plays a pivotal role in controlling the progression of cells from the G1 phase to the S phase, allowing DNA replication and cell division to occur. CDK2 forms complexes with cyclins, which activate its kinase activity, leading to the phosphorylation of various target proteins involved in cell cycle progression. 

The CDK2/cyclin E complex plays a crucial role in the phosphorylation of retinoblastoma (Rb) protein and the transition from G1/S phase. The CDK2/cyclin A complex is significantly involved in DNA synthesis during the S phase and the activation of CDK1/cyclin B during the transition from G2/M phase. PF-07104091(19) is an orally available CDK2 inhibitor with a potential antitumor activity. In human ovarian cancer cell models(OVCAR3, OV5392), compound 19(25, 75 and 175mg/kg, twice daily, po) can induce tumor reduction in a dose-dependent manner. Furthermore, the combined administration of 19 and the frontline drug Palbociclib demonstrated a synergistic effect in the model of breast cancer cells. In 2020, Pfizer initiated a Phase I/II clinical trial of compound 19 to assess its safety and tolerance and to test the maximum tolerated dose of compound 19 as a single therapy in patients with small cell lung cancer, non-small cell lung cancer, ovarian cancer or breast cancer(NCT04553133).

Dysregulation of CDK2 activity has been implicated in numerous diseases, including cancer, making it an attractive target for therapeutic interventions aimed at controlling cell proliferation and promoting healthy cell cycle prThe target CDK2 in the pharmaceutical industry has attracted the attention of several companies, including Pfizer Inc., Cyclacel Pharmaceuticals, Inc., Otsuka Holdings Co., Ltd., and Tiziana Life Sciences Ltd. These companies are actively involved in the research and development of drugs targeting CDK2. Indications such as non-small cell lung cancer, ovarian cancer, and triple negative breast cancer have seen the approval of drugs targeting CDK2. The most rapidly progressing drug types under the target CDK2 are small molecule drugs, indicating intense competition in this area. The European Union and the United States are leading in terms of development, with China also making progress. Overall, the competitive landscape for target CDK2 is dynamic, and future development in this area holds significant potential.ogression.

How do they work?

CDK2 inhibitors are a type of drugs that specifically target and inhibit the activity of cyclin-dependent kinase 2 (CDK2). CDK2 is a protein kinase that plays a crucial role in regulating the cell cycle, specifically the transition from the G1 phase to the S phase. By inhibiting CDK2, these inhibitors can disrupt the cell cycle progression and prevent the proliferation of cancer cells.

From a biomedical perspective, CDK2 inhibitors are of great interest in the field of cancer research and treatment. Cancer cells often exhibit uncontrolled cell division and proliferation, and CDK2 is frequently overactive in these cells. By blocking CDK2 activity, CDK2 inhibitors can potentially halt the growth of cancer cells and serve as a targeted therapy for various types of cancer.

It's important to note that CDK2 inhibitors are still under investigation and development, and their clinical use is currently limited to clinical trials. These inhibitors hold promise as potential anticancer agents, but further research is needed to determine their efficacy, safety, and optimal usage in cancer treatment.

List of CDK2 Inhibitors

The currently marketed CDK2 inhibitors include:

For more information, please click on the image below.

What are CDK2 inhibitors used for?

CDK2 inhibitors are under investigation forIndications such as non-small cell lung cancer, ovarian cancer, and triple negative breast cancer.For more information, please click on the image below to log in and search.

表格

描述已自动生成

How to obtain the latest development progress of CDK2 inhibitors?

In the Synapse database, you can keep abreast of the latest research and development advances of CDK2 inhibitors anywhere and anytime, daily or weekly, through the "Set Alert" function. Click on the image below to embark on a brand new journey of drug discovery!

图形用户界面, 文本, 应用程序, 电子邮件

描述已自动生成

图形用户界面, 应用程序

描述已自动生成

GB-1211: brief review of its R&D progress and the clinical result in 2023 ESMO
ESMO 2023
4 min read
GB-1211: brief review of its R&D progress and the clinical result in 2023 ESMO
16 November 2023
On 23 Oct 2023, GALLANT-1: GB1211 galectin-3 (Gal-3) inhibitor plus atezolizumab (atz) for first line treatment in patients (pts) with advanced/metastatic non-small cell lung cancer (NSCLC) was reported at the ESMO Congress.
Read →
Efficient Strategies for Acquiring Sequence Information for an Antibody by Its Name
Bio Sequence
2 min read
Efficient Strategies for Acquiring Sequence Information for an Antibody by Its Name
16 November 2023
This article will teach you three methods to find the corresponding sequence information by the name of an antibody.
Read →
What are CD38 inhibitors and how do you quickly get the latest development progress?
What are CD38 inhibitors and how do you quickly get the latest development progress?
16 November 2023
Inhibitors of CD38 are a kind of treatment aimed at the white blood cells within bone marrow, which are responsible for inducing multiple myeloma.
Read →
Cadonilimab: brief review of its R&D progress and the clinical result in 2023 ESMO
ESMO 2023
4 min read
Cadonilimab: brief review of its R&D progress and the clinical result in 2023 ESMO
16 November 2023
On 23 Oct 2023, the phase Ib/II clinical trial result of Cadonilimab combined with lenvatinib for first-line treatment of advanced hepatocellular carcinoma was reported at the ESMO Congress.
Read →
Get started for free today!
Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.
Start your data trial now!
Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.