NEWS

Ibrutinib

Release time:

2018-11-16 17:58

Ibrutinib is meridianFDAThe second new drug approved by the breakthrough drug pathway (the first wasObinutuzumab), while also enjoyingFDAThe other twobuff, and after listing7years of administrative protection.

Ibrutinib (Ibrutinib) isJohnson JohnsonCompany andPharmacyclicsThe company's cooperation in the development of targeted anti-cancer drugs, in.2013Year11Month13The U.S. Food and Drug Administration (FDA) approved for listing, trade nameImbruvica,The drug is used for mantle cell lymphoma (mantle cell lymphoma, MCL) of treatment. chinese chemical name of ibrutinib:1-[3(R)-[4-Amino-3-(4-phenoxyphenyl)-1H-Pyrazole and[3,4-d]Pyrimidine-1-Base]Piperidine-1-Base]-2-Propylene-1-Ketone; Chemical name in English:1-[3(R)-[4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo [3,4-d] pyrimidine-1-yl] piperidin-1-yl]-2-propen-1-one;Molecular formula:C25H24N6O2;Molecular weight:440.50;CASRegistration Number:936563-96-1.

2013Year11Month13On the same day, the U.S. Food and Drug Administration (FDA) approvedImbruvica (Ibrutinib-Ibrutinib)Can be usedmantle cell lymphoma(MCL)The treatment.MCLis a rarenon-Hodgkin's lymphomaof all non-Hodgkin lymphoma cases in the U. S.6%. Usually diagnosedMCLThe cancer has spreadLymph nodebone marrow and other organs.

Mechanism of action: Ibrutinib is a small moleculeBTKinhibitors, are able to interactBTKThe cysteine residue of the active center is covalently bound, thereby inhibiting its activity.BTKFull NameBruton'styrosinekinase, inBCRsignal pathway,cytokine receptorsignal transmission in the signaling pathway, mediatedBCell migration, chemotaxis, adhesion. Preclinical studies have demonstrated that ibrutinib suppresses malignantBCell proliferation, survival.

Clinical Trials:111patients who had received at least one previous treatment after ibrutinib, the overall response rate was65.8%(Complete response17.1%+Partial response48.6%), the median sustained response time was17.5Months.

Supplementary note: Due to multiple accelerationbuffThe addition, the clinical trial of the drug is very crude, the group of patients only.111The clinical endpoint is response rate rather than survival.mantle cell lymphomais a rarenon-Hodgkin's lymphoma, beforeFDARespectively in2006year,2013Approved borte zomib,LenalidomideTreatment of the disease. Ibrutinib isJohnson&JohnsonFromPharmacyclicsKey varieties bought at high prices, in addition to the treatment of mantle cell lymphoma, are also used.Chronic lymphocytic leukemia, smalllymphocyteLymphoma.

 

Patents in China:

The drug is currently available in China.4See the following table for the patents granted:

Patent Name

Patent Number

Type

Application Date

Expiry date

Legal status

Inhibitors of Bruton's tyrosine kinase

CN200680056438.5

Compound

2006-12-28

2026-12-28

Authorization

Inhibitors of Bruton's tyrosine kinase

 CN201210200042.0

Method

2006-12-28

2026-12-28

Authorization

Inhibitors of Bruton's tyrosine kinase

CN201010162270.4

Compound

2006-12-28

2026-12-28

Authorization

Inhibitors of Bruton's tyrosine kinase

CN200880014760.0

Compound

2008-03-27

2028-03-27

Authorization
 

The independent claims of the four patents are as follows:

CN200680056438.5

CN201210200042.0

CN201010162270.4

CN200880014760.0

The clinical trials of the drug have been completed in the Southern Hospital of Southern Medical University, Peking University People's Hospital, and Peking University Cancer Hospital. And the drug has been in China.2017Year8Monthly approval for listing. At present, the domestic generic drug declaration manufacturers are: Harbin treasure pharmaceutical,Shanghai Huilun Jiangsu Pharmaceutical Co., Ltd.,Zhejiang Haizheng Pharmaceutical Co., Ltd.,Xuzhou Wanbang Jinqiao Pharmaceutical Co., Ltd.,Jiangsu Wanbang Biochemical Pharmaceutical Co., Ltd.,Zhengda Tianqing Pharmaceutical Group Co., Ltd.,Lianyungang Runzhong Pharmaceutical Co., Ltd.,Beijing Deep Blue Ocean Biomedical Technology Co., Ltd,Shandong Xinlu Pharmaceutical Co., Ltd,Hangzhou Sino-US Huadong Pharmaceutical Co., Ltd.Wait.

Lymphoma, limited, cell, therapy, 1-, pharmaceutical, fda, response, approved