CDK1: Occupies an important site of signal transduction, clinically refers to pancreatic cancer & glioma!

Cyclin-dependent kinase (CDK) is one of the important members of the protein kinase family; among them, CDK1 plays a key role in cell cycle regulation, checkpoint activation, and DNA damage repair

Important cell signaling site

Tumor cells are characterized by continuous division and uncontrolled proliferation.

There are many studies on whether the functions of CDKs are dependent and replaceable, especially CDK1 vs CDK2

In addition, CDK1 can completely compensate for the loss of CDK2 in terms of cell cycle regulation.

Figure 1.

Disease location: pancreatic cancer & glioma

At present, the development of clinical indications for CDK1 inhibitors is mainly focused on pancreatic cancer and glioma, especially pancreatic cancer

Pancreatic cancer is known as the "king of cancer".

The treatment of pancreatic cancer mainly includes surgical treatment, radiotherapy and chemotherapy

Figure 2.

Clinical drugs: up to stage III

Up to now, through database query, no drugs developed for CDK1 have been marketed, and the highest clinical progress is clinical phase III, such as Rigosertib (Phase III), BEY-1107 (Phase II), Zotiraciclib (Phase II), etc.

➢ Rigosertib (Phase III)

First of all, this is a pan-target inhibitor developed by Onconova Therapeutics for the treatment of first-line high-risk myelodysplastic syndrome (MDS) in combination with azacitidine

➢ BEY-1107 (Phase II)

The development company is Beyondbio, which is a CDK1 inhibitor and is clinically used in the treatment of pancreatic cancer

➢ Zotiraciclib (Phase II)

The development company is Adastra Pharmaceuticals, an oral brain-penetrating multikinase inhibitor, and also a multi-target inhibitor, especially targeting CDK1/2/5/7/9, which is clinically directed towards glioblastoma and interstitial Treatment of degenerative astrocyte tumors

Patent applications in China

Through domestic patent inquiries, the CDK1 inhibitor-related patents applied in China are related to tumors.

Shandong University applied for the invention patent "Cyclin-dependent kinase 1 inhibitor and its use" in 2011.

The Chinese Academy of Medical Sciences Peking Union Medical College Hospital applied for the invention patent "Cyclin-dependent kinase 1 inhibitor and its use" in 2019.

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