JAK kinase inhibitor development hot global listing 7 varieties of domestic track Hengrui leading!

Theautoimmune diseases, which are widely and mostly difficult to treat, are one of the important directions of drug developmentThe JAK-STAT pathway is a proven and small number of immunomodulatory pathways, especially JAK inhibitors, and several drugs are listed worldwide, such as tofatinibDomestically, the development of JAK inhibitors also has more than 10 varieties into the clinical stage, and by Jiangsu Hengrui led the track, the overall development of hot and clinical indications (such as bone marrow fibrosis, rheumatoid arthritis, baldness, etc.) is very much to look forward tocurrently, a total of 4 JAK family members (JAK1, JAK2, JAK3 and TYK2) and 7 STAT family members (STAT1, STAT2, STAT3, STAT4, STAT5a, STAT5b and STAT6) have been found in mammals;Figure 1.1: Different signal transduction pathways mediated by intracellular-JAKJAK target development time is less than 20 years, but there are nearly 7 varieties have been approved for the market, the indications are mainly tumor and autoimmune diseases, further refining the indications mainly for bone marrow fibrosis and rheumatoid arthritisBelow is the first FDA-approved JAK inhibitor for the treatment of patients with bone marrow fibrosis (Reedinib) and the first JAK inhibitor (Tofatinib) for the treatment of rheumatoid arthritis, developed jointly by Incyte and Novartis, was approved by the U.SFDA in 2011 and is the first FDA-approved JAK1/2 inhibitor to be used to treat patients with critical or high-risk bone marrow fibrosisIn addition, the species has been clinically developed in the field of true erythrocyte growth and acute graft anti-host diseaseglobal sales, the annual sales of Reedinib in 2015 was US$1 billion and increased year by year, reaching US$2.799 billion in 2019But it's amazing! Domestic registration declaration of this variety, in addition to the original Novartis has been approved for import, there is no domestic pharmaceutical companies to register the species declarationTofatinib is an oral small molecule JAK inhibitor developed by Pfizer in the United States with better JAK selectivity, in November 2012, the U.SFDA approved the acetic acid tomeet the treatment of methotrexate in adult patients with moderate to severe active rheumatoid arthritis; At present, in addition to approved indications, Tofatinib is also in the strong direct spina itis, atopic dermatitis, dry corneal conjunctivitis and Crohn's disease and other diseases in the efficacy of verificationglobal sales, Tofatini's annual sales in 2017 were $1 billion, reaching $2.242 billion in 2019Domestic registration declaration for this variety, in addition to the original research Pfizer has been approved for import, the domestic pharmaceutical companies are daqing, Qilu pharmaceutical imitation varieties are registered with the chemical 4 categories of declaration, and has been approved for productiontable 2.1 of the: Jak inhibitors are listed/NDA/III clinical speciesAt present, the development of JAK kinase inhibitors in China, nearly 10 varieties have entered the clinical development stage, the track is the most advanced variety of Hengrui development SHR-0302, has now entered the clinical phase III; Here is mainly introduced under Hengrui Company's SHR-0302, as well as the two Zze-Yu biological ii varietiesthe JAK1 inhibitor SHR-0302, developed by Hengrui, Jiangsu Province,, is currently in clinical phase III for the treatment of rheumatoid arthritis, while for the adaptation of "ulcerative colitis, tertorphilis, Crohn's disease, spot baldness" is also in clinical processIn January 2018, Jiangsu Hengrui entered into a cooperation agreement with Arcutis of the United States, which will receive SHR-0302 as a local external formulation for the treatment of skin diseases and will be exclusively clinically developed, registered and marketed in the United States, the European Union and Japan, while Hengrui will receive a down payment and milestone of US$200 million, plus a post-ipo sales bonusdeveloped two JAK inhibitors, which are now in the clinical stage in ChinaJaktinib, clinically developed for the treatment of bone marrow fibrosis and plaque, including bone marrow fibrosis, isoderitis, psoriasis, isopulmonal fibrosis, aggressive spinabitis and moderate and severe active rheumatoid arthritis;Alkotinib, clinically developed in the direction of non-small cell lung cancer, further identified as advanced NSCLC for the treatment of ALK-positive or ROS1-positive and failed by first-line (chemotherapy or gramibin)table 3.1 of: The development of JAK inhibitors in China isTo sum up, it is an overview of the overall development of JAK kinase inhibitors worldwideMost of the world's listed drugs have been developed by large pharmaceutical companies, and market performance is increasing and receiving higher attentionDomestically, for the direction of the development of related targets, are also very well-known innovative pharmaceutical companies in doing, and will soon enter the harvest period! In the future, it is not just the direction of JAK kinase inhibitors, I believe that the whole field of autoimmune diseases will be a global drug industry.