New drug obeticholic acid becomes first new treatment for PBC in 20 years

2017Year6Month22Day, the drug obeticholic acid was granted2017 Galeno Italy Award(Galen Prize) Chemosynthetic Drug Award,Galen PrizeThe Chemical Synthetic Drug Award is one of the most recognized honors in the Italian life sciences industry and is awarded to the innovative drug obeticholic acid for its role as aPBCNew treatment options. The scientific committee that awarded the award said that obeticholic acidOcaliva"very innovative" from both a patient perspective and a treatment perspective, noting that its mechanism of action is associatedUDCAare different and complementary, allowingOcalivaMore direct and effective regulation of the molecular and cellular mechanisms underlying disease-by activating farnesolXReceptors, Indirect Inhibitory Cytochrome7A1(CYP7A1) gene expression. DueCYP7A1It is the rate-limiting enzyme in bile acid biosynthesis, so obeticholic acid can inhibit bile acid synthesis and is used in the treatment of primary biliary cholangitis and possibly in nonalcoholic fatty liver disease.

Obeticholic acidobeticholic acid(Trade name:Ocaliva) in2016Year5Month27Day by the United StatesFDAApproved for the treatment of primary biliary cholangitis in adults(PBC)This is also near.20First approved treatment in yearsPBCof drugs. DuePBCis a rare disease, obeticholic acid in2010The European Medicines Agency's Orphan Drug Committee (COMP) orphan drug qualification, as an incentive, orphan drugs can obtain ten years of market exclusivity. China currently has no original research and generic drug registration information, but it is worth noting that Jiangsu Hengrui and Zhengda Tianqing imitation in clinical state, and reference preparation for the record.

 

What is primary biliary cholangitis?

Primary biliary cholangitis(Primary biliary cirrhosis,PBC)Is a chronic intrahepatic cholestatic disease, more common in middle-aged and elderly women. According2010Guangzhou scholars reported that in the health check-up populationPBCThe prevalence49．2/10million, of which40The prevalence of women over the age155．8/10million, althoughPBCThe incidence is low, but because of its serious harm to the human body, it is also very worthy of attention.PBCIt is roughly divided into four stages, the first two stages have no obvious symptoms, and the third stage has clinical symptoms such as fatigue and skin itching; from the onset of symptoms, the average survival time is5～8Year. Portal hypertension-related complications in symptomatic patients10The annual incidence rate is10％～20%, which was higher than that of asymptomatic patients. When patients had esophageal and gastric varices,3The annual survival rate is only59% after the first bleeding3The annual survival rate is about46％。

Previously20year,FDAApprovedPBCThe only drug is ursodeoxycholic acid (UDCA), however a considerable proportion of patients (approx.40%) YesUDCAInadequate response, orUDCAIntolerance. The approval of obeticholic acid undoubtedly brings more hope to these patients.

Brief analysis of patent of obeticholic acid

Compound: U.S. Patent (US7138390B2)2022Year11Month16Expiration date, U. S.NCEExpiration Time2021Year05Month27day,ODEExpiration Time2023Year05Month27day; the patent of the obecholic acid compound has not entered China.

Crystal Form: U.S. Patent (US9238673B2) throughPCTEntering China (CN104781272A), not yet authorized, valid2033The rights to its preparation, crystal form and use were protected.

Nanjing Jiqun, Tianjin hankang, Suzhou Jingyun, Nanjing changao, Xiamen Weiyang, Chengdu Xingong, Chengdu Baiyu, Sichuan ruixikang, Guangdong Lizhu and Jiangsu Hengrui, which have applied for crystal type patents in China, have no authorized patents.

Preparation: The patent is valid2024-2032Year.

The original research company is rightObeticholic acidInternational peripheral patent layout.

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

References

https://mp.weixin.qq.com/s/QszsywsSB0Nb3bWGDtvQrA