Domestic first CDK4/6 inhibitor palbociclib listed

Breast cancer is a malignant tumor that occurs in the breast epithelial tissue, and it is the largest malignant tumor that seriously threatens the health of women in the world. Although my country is not a country with a high incidence of breast cancer, the incidence of breast cancer is increasing every year in recent years.3%～4%The growth rate has risen sharply, with new growth each year.10One patient has.1The median survival of patients diagnosed with advanced, advanced breast cancer is only.2-3year,5The annual survival rate is only about20%In patients with early breast cancer who have received surgery and standard treatment, there are also30-40%advanced breast cancer, patients with advanced breast cancer urgently need innovative treatment options.

2013The U.S. Food and Drug Administration (FDA) Approved the world's first cyclin-dependent kinase (CDK)4/6Inhibitor Aiboxin® IBRANCE®(Pipericelli, Palbociclib) for a breakthrough new drug for the treatment of advanced breast cancer,2015YearFDAApprove Aibo New with fast-track approval process®Listed for the treatment of advanced breast cancer.2018Year7Month31Day, Ebo New®The State Drug Administration of China (CFDA) approved, can be used for hormone receptor positive (HR) and human epidermal growth factor receptor2Negative (HER2-) for breast cancer treatment.

 

CDK4/6inhibitors

cyclin-dependent kinase4/6(cyclin-dependent kinase4/6,CDK4/6)is a kind of silk/Threonine Kinases, and CyclinsD(cyclinD) binding regulatory cellsG1PeriodSPeriod conversion. In many tumors, there are"cyclinD-CDK4/6-INK4-Rbpathway "abnormal, the change of this pathway acceleratesG1stage process, which accelerates the proliferation of tumor cells and then proliferates out of control, so it is currently believed that,CDK4/6Inhibitors can selectively inhibitCDK4/6Restores cell cycle control, thereby blocking tumor cell proliferation. Right.cyclinD-CDK4/6-INK4-Rbpathway intervention as a therapeutic strategy,CDK4/6Therefore, it has become one of the hot targets of anti-tumor in recent years.

CurrentlyFDAA total of three were approvedCDK4/6inhibitor drugs, respectively: Pfizer'sPalbociclib(palbociclib, trade nameIbrance), Novartis'sRibociclib(Trade nameKisqali) and Lilly'sAbemaciclib(Trade nameVerzenio), of which the latter two drugs are not yet available in China. Research data show that whether it is first-line or second-line, premenopausal or postmenopausal, threeCDK4/6Inhibitors can significantly improve the objective response rate and prolong the progression-free survival of patients (PFS), especially in the first-line treatment, threeCDK4/6inhibitors can be prolongedPFS 10More than a month.

 

Drug Introduction

Chinese name: palbociclib

English name:Palbociclib

Trade name: Ebo new®(IBRANCE®)

Molecular formula:C₂₄H₂₉N₇O₂

Pipocelli is a Pfizer (Pfizer Inc.) R & DCDK4/6Inhibitor drugs, suitable for treatmentHR /HER2-Locally advanced or metastatic breast cancer in combination with an aromatase inhibitor as initial endocrine therapy in postmenopausal women.

 

Patent Information

Pipecil is registered in the American Orange Book.3Related U.S. patents, there are3Chinese family patents, all patents have been granted.

Open No.	Patent Name	Application Date	Legal status
US6936612	2-(Pyridin-2-ylamino)-pyrido[2,3-d]pyrimidin-7-ones	2003-01-16	Authorization
US7208489	2-(pyridin-2-ylamino)-pyrido [2,3-d]pyrimidin-7-ones	2005-01-28	Authorization
US7456168	2-(pyridin-2-ylamino)-pyrido [2,3-d]pyrimidin-7-ones	2007-04-11	Authorization
CN101906104B	2-(Pyridine-2-amino group)-pyridinium and[2,3-d]Pyrimidine-7-Ketone	2003-01-10	Authorization
CN101001857B	2-(Pyridine-2-amino group)-pyridinium and[2,3-d]Pyrimidine-7-Ketone	2003-01-10	Authorization
CN102295643B	2-(Pyridine-2-amino group)-pyridinium and[2,3-d]Pyrimidine-7-Ketone	2003-01-10	Authorization

 

 

 

 

 

 

 

 

 

 

 

 

 

 

Layout of domestic pharmaceutical enterprises

According to the China New Drug Research and Development Monitoring Database (CPM) shows that in addition to Qilu Pharmaceutical's application for generic drugs, there are currently more than a dozen research enterprises in the research field, such as Haosen, Hengrui, Haizheng, Zhengda Tianqing, etc., conducting clinical trials, eyeing more than 30Billion dollar market pie.