The first deuterium drug was approved or led to a wave, and domestic and foreign deuterium drug research and development enterprises briefly cited one or two

On April 3, 2017, the FDA officially approved Teva's Huntington's chorea drug, austedo, which is a small molecule oral inhibitor targeting VMAT-2 It is also the first deuterium drug approved by the FDA The so-called deuterium substitution refers to the replacement of hydrogen in the active molecular group of drugs with the isotope deuterium Because it is non-toxic and non radioactive, and it is about 6-9 times more stable than the hydrocarbon bond, it can close the metabolic site and prolong the half-life of drugs, thus reducing the therapeutic dose, without affecting the pharmacological activity of drugs It is considered as an excellent modification method, and it is also believed to be a breakthrough of chemical combination Property patents and effective ways to avoid R & D risks The effective component of H atom in D atom substitution group is infliximab Abda, which is the deuterium product of infliximab The drug was initially developed by auspex pharmaceuticals, a pharmaceutical company focusing on the research and development of deuterium instead of deuterium After that, auspex was acquired by Teva, and the drug also entered Teva When it comes to deuterium, Teva's product development pipeline has to mention another company, Co NERT pharmaceuticals, which focuses on deuterium Using its DCE platform and innovative drug development methods, concert has developed a series of products with potential advantages, including new drugs for the treatment of lung diseases, cystic fibrosis, central nervous system disorders, autoimmune diseases and inflammatory diseases In the product pipeline of concert, ctp-656 and ctp-543 are proprietary drugs of the company Ctp-656 has been certified as an orphan drug by FDA for its use in the treatment of cystic fibrosis On March 6, 2017, the company signed an agreement with vertex pharmaceuticals, which will be acquired by vertex; ctp-543 is used to treat alopecia areata, an autoimmune disease, and its active ingredient is the product of deuterium modification of ruxolitinib, which has been listed on the market Avp-786, jzp-386 and ctp-730 are products jointly developed with avanir, jazz pharmaceuticals and celgene, respectively In addition to auspex and concert, which focus on the research and development of deuterium drugs, there are many foreign companies also involved in the field of deuterium drugs, such as Takeda's type 2 diabetes drug alogliptin benzoate, GSK's melanoma drug dabrafenib, etc There are also some domestic enterprises involved in the field of deuterium substitute drugs This paper will give you some chestnuts: 1 Suzhou Zejing biopharmaceutical Co., Ltd Zejing Pharmaceutical Co., Ltd is an enterprise engaged in the R & D and production of chemical small molecule new drugs and recombinant protein large molecule new drugs at the same time, focusing on the domestic market, focusing on the R & D and production of new drugs in the fields of anti-tumor, blood diseases, etc., and is also considered to be the third largest deuterium drug company in the world The five chemical projects of the existing deuterium drug product line of Zejing pharmaceutical and their corresponding deuterium original research drugs are: donafinib: sorafenib (Bayer); jakotinib: JAK inhibitor momelotinib (giled); zg0320: ALK inhibitor ceritinib (Novartis); zg0128: idealisib (Gilead); zg5216: obeticolic (intercept) According to the data retrieved by hsmap system of Huoshi creation, Zejing pharmaceutical has applied for 50 patents Part of patents of Zejing pharmaceutical 2 Haichuang pharmaceutical team of Chengdu Haichuang Pharmaceutical Co., Ltd has a solid chemical synthesis ability, which can provide efficient chemical synthesis services for all stages of drug development, including deuterium compounds and other isotopic labeled compounds services Hc-1119, the product line of Haichuang pharmaceutical, is an androgen receptor antagonist for the treatment of prostate cancer, and its active ingredient is deuterodenza Enzalutamide is approved by the FDA for the treatment of advanced metastatic or recurrent castrated resistant prostate cancer patients The trade name is xtandi, and the original manufacturer is Pfizer In October 2016, hisilica pharmaceutical signed a patent license agreement with Haichuang pharmaceutical and obtained the patent of hc-1119 In addition to some patents of Haichuang pharmaceutical, companies such as taijihongnuo and Zhengda Tianqing also have some deuterium substitutes Conclusion: in fact, although deuterium has become a shortcut for new drug research and development, the approval of austedo may set off a small upsurge of deuterium patent application, but its potential risks are also unavoidable Due to the very similar nature of isotopes, whether deuterium drugs can achieve the expected effect is a risky thing Even if they can obtain patents, once they are listed, they may still face lawsuits from the original researchers Although there is no such case at present, the original researchers are more likely to win the lawsuit from multiple perspectives Therefore, the research and development of deuterium drugs is indeed a choice with both risks and benefits, as some people say, either making money or losing money.