Hengrui independently developed innovative drug pyrrotinib maleate tablets approved for listing

Recently, Hengrui Medicine1New Drug "Pyrrotinib Maleate Tablets" WonCFDAApproved for marketing for the treatment of recurrent or metastatic breast cancer.

Pyrrotinib maleate tablets are Hengrui Pharmaceuticals' third innovative chemical drug after irecoxib and apatinib, and are independently developed by Hengrui1.1ClassEGFR/HER2Inhibitors, but also the second domestic.IIPhase clinical trial data are directly declared as innovative drugs on the market, but also domestic.best-in-classHeavy potential varieties, analysts believe that the future of the domestic market incremental space is expected to break through.30 Billions of dollars, becomeHER2The biggest winner of targeted drugs. The main indications for the current application areHER2positive metastatic/advanced breast cancer,HER2Mutant advanced non-small cell lung adenocarcinoma,HER2Expression of positive advanced gastric cancer. Among them, only breast cancer indications have entered phase III clinical, non-small cell lung cancer and gastric cancer, respectively.IIPeriod andIPeriod.

HER2Mechanism of action of targeted drugs

Pyrrotinib maleate is an orally available epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor2(HER2) Dual inhibitors of tyrosine kinases.HER2Is a transmembrane glycoprotein with receptor tyrosine kinase activity, belongs to the epidermal growth factor receptor family, the polymerization of the receptor will lead to the phosphorylation of receptor tyrosine residues, and start a variety of signaling pathways leading to cell proliferation and tumor occurrence;15%~30%of breast cancer and10%~30%of the stomach./Esophageal cancer can occurHER2gene amplification or overexpression,HER2Overexpression of is also seen in other tumors such as the ovary, endometrium, bladder, lung, colon, and head and neck. ForHER2The most representative drug on the market, in addition to the original research drug Herceptin (trastuzumab), as well as the same monoclonal antibody drug.Bolt (Pertuzumab)Outside, andADC(Antibody Drug Conjugates) By Kadsize (T-DM1)As well as small molecule drugs lapatinib, afatinib and so on.

Currently there are17of the home enterpriseHER2Targeted drugs have entered the clinical stage (or declared clinical). in accordance2class (I. e.biosimilar) Declares the rapid progress of research and development of Jiahe Biology, Anke Biology, Fuhong Hanlin, Zhengda Tianqing and other enterprises;HER2-ADCor other according1Class declaration of the rapid progress of Baiotai, Lizhu monoclonal antibody, Qilu Pharmaceutical, Zhejiang Pharmaceutical and other enterprises.

2017Year9Month, Hengrui uses Pyritinib.IIphase clinical data firstCFDASubmit a listing application and include it in the priority review. Piritinib'sIIStunning clinical data, in the treatment of anthracycline and taxane treatment failure, and recurrence./Post-metastatic chemotherapy does not exceed2Line of breast cancer patientsIIIn the clinical trial, the objective response rate of Hengrui's pyrrotinib maleate tablets combined with capecitabine tablets was78.5%The objective remission rate of lapatinib tosylate tablets combined with capecitabine tablets in the control group was57.1%. Median progression-free survival in the pyrrotinib group was18.1months, the median progression-free survival in the lapatinib group was7.0Months. Objective remission rate of pyrrotinib(ORR)progression-free survival(PFS)were significantly better than the control group lapatinib.

Given the stunning therapeutic effect of pyrrolitinib in breast cancer, analysts estimate that the drug is expected to be a peak super.30billions of heavy varieties.

Patents of pyrrotinib maleate

Through data query, its original research patent"6-amino quinazoline or 3-cyano quinoline derivatives, preparation methods and pharmaceutical uses thereof” （WO2011029265A1) in2010Year08Month26This patent gives the preparation method of quinoline derivatives and their application in medicine, and has a patent of the same family in many countries, as follows:

Later successively applied for crystal type patents and peripheral compound patents. In2012Year02Month10day of application"pharmaceutically acceptable salt of (e)-n-[4-[[3-chloro-4-(2-pyridylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolyl]-3-[(2r)-1-methylpyrrolidin-2-yl]prop-2-enamide, preparation method thereof, and medical use thereof” （WO2012122865A3), this patent gives the synthetic route and reaction conditions of pyritinib, in many countries have the same family patent, finishing as follows:

References

https://xueqiu.com/1912517390/112978387