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    Home > Medical News > Latest Medical News > Statistical analysis of target points of drugs on the market, clinical, preclinical and discontinued research in the world

    Statistical analysis of target points of drugs on the market, clinical, preclinical and discontinued research in the world

    • Last Update: 2017-04-13
    • Source: Internet
    • Author: User
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    The research and development of targeted drugs has been the routine choice of new drug research and development projects of major pharmaceutical enterprises The selection of target needs to consider many factors, one of which is the competition of research and development, and excessive homogeneity should be avoided Nature and other magazines have published many articles on the statistical distribution of drug targets, which will not be described in detail in this paper This paper aims to list the main target information of drugs in the global new drug research and development, including the listing, clinical, preclinical and discontinued research, and make statistics on the ratio of each stage of listing / clinical / preclinical / discontinued research, which is helpful for preliminary positioning and evaluation of related targets Main mechanism of action of drugs on the market (target) the drugs selected in this paper do not include generic drugs, and remove the composition and non confirmed target drugs It should be noted that about 20% of drugs are double target or multi-target effects at present Among the more than 2000 drugs still on the market, the top 100 of its mechanism of action (target) is shown in the table below The first four targets are all biological type (protein recombination) drugs, with a corresponding number of up to 670 The related indications are anemia, neutropenia, hepatitis, etc The fifth most common indication of opioid receptor muagonist is pain, and it is basically the development of small chemical molecules Next is the well-known insulin (receptor) target associated with diabetes, but its "ratio of drugs on the market / in research" does not exceed 0.3 (Note: drugs on the market include drugs on the market), indicating that a large number of drugs are currently in clinical or preclinical research and development, and other mechanisms (targets) with low ratio of drugs on the market / in research (less than 0.2) include TNF binding agent, TNF alpha ligand inhibitor ,B-lymphocyte antigen CD20 inhibitor, VEGF-2 receptor antagonist ,VEGF receptor antagonist,Epidermal growth factor antagonist,Topoisomerase II inhibitor,Erbb2 tyrosine kinase receptor inhibitor,Insulin sensitizer 。 On the other hand, the mechanism of action (target) of the low ratio of drugs on the market / under development (greater than 0.8) includes streptokinase inhibitor, PGE1 agonist, alpha adrenoceptor agonist, vitamin D3 receptor agonist, antithrombin III, repetitive acid receptor agonist , indicating that there are not many drugs in clinical or preclinical research and development, which may be affected by many factors such as target itself, clinical demand or market saturation Table 1 Mechanism of action (target) of drugs on the market Top100 note: the mechanism of action (target) of drugs on the market, including pre clinical, clinical and marketing stages, is in clinical stage and includes some drugs on the market The mechanisms of action (targets) of the drugs in clinical stage and including the drugs on the market are shown in the table below, and the insulin and its receptors mentioned in the listing part are also ranked at the top The overall "clinical / (clinical + preclinical + discontinuation) ratio" in this part is low, because the number of discontinuation drugs is considered, and it also reflects the difficulty of new drug research and development The targets with clinical / (clinical + preclinical + discontinuation) ratio greater than 0.4 include b-lympheyte antigen CD19 initiator, FGF3 receptor antagonist, FGF1 receptor antagonist, FGF2 receptor antagonist and CD40 live receptor Antigonit shows that for these targets, the probability of stopping research is relatively small The targets with clinical / preclinical / discontinuation ratio less than 0.1 include toposomerase II inhibitor, DNA gyrase inhibitor, calcium channel inhibitor and PDE 4 inhibitor Although these four targets are all on the market, they have experienced too many discontinuation decisions, which again shows that new drug development is not easy "0" will also appear in the "number of drugs on the market" column of the table below The details will be described in "top 100, a target in clinical stage but not in the market" Table 2 Mechanism of action (target) of clinical drugs Top100 is in the clinical stage, but there is no mechanism of action (target) of drugs on the market This part of statistics focuses more on the research and development of innovative drugs Eight of the top 11 targets belong to the field of small molecule research and development, as shown in the table below The other three are glucon receptor agonist, TLR-4 agonist and CD40 live receptor agonist Preference for biopharmaceutical research and development The "clinical / (clinical + preclinical + discontinuation) ratio" of this part is also low as a whole, and the targets with the ratio lower than 0.1 include Hsp90 inhibitor, RAS GTPase inhibitor, Stat-3 inhibitor and protein farnesyltransferase inhibitor At present, there are many discontinuation projects for these four targets, which are worthy of attention of the project leader Moreover, the number of preclinical items of Hsp90 inhibitor and Stat-3 inhibitor is 29 and 27 respectively, which are the two most preclinical drugs in the following table In addition, the ratio of Glypican-3 inhibitor is higher than 0.8, indicating that the clinical success rate of the target is higher, of course, the number of drug development of the target itself is less To some extent, most of the targets listed in the table below are the main areas of competition for innovative drug research and development in the world today Table 3 The number of drug research and development in this part of the target Top100, which is in the clinical stage but does not have the action mechanism (target) of clinical and listed drugs, is too small, so there is no statistical ratio, and only the target information of TOP33 is listed here The first three mechanisms of action (targets) are leucine rich serine threonine kinase 2 inhibitor, TrkB receptor agonist and K-ras GTPase inhibitor Among them, 11 drugs of K-ras GTPase of ras family are all in early development K-ras is obviously a worldwide research problem Which research and development achievements enter the clinical stage earlier or push to the late clinical stage will take the lead in the market Note that in the following table, the number of bradykinin receptor antagonists and cystine protection inhibitor drugs that have been discontinued has reached 13 and 17 respectively, and the targets of Mitochondrian frataxin inhibitor, aimp2 gene inhibitor and eosinophil peroxidase inhibitor have not been suspended Table 4 The main mechanism of action (target) of TOP33 stop research drug is shown in the table below In the number of stop research drugs, the stop research ratio of most targets is on the high side, and many top targets are also on the top of the list In contrast, erbB2 tyrosine kinase receptor inhibitor and glucagon like peptide 1 agonist's "stop research / (in research + stop research) ratio" is less than 0.4, indicating that these two targets have a high probability of advancing The targets with the ratio greater than 0.9 included renin hibitor, ACAT inhibitor, leukotriene BLT receptor antagonist, NK2 receptor antagonist, 5-HT 1A receptor antagonist, AMPA receptor antagonist, cholecystokine CCK2 receptor antagonist, endopethidase inhibitor and endotherin antagonist These targets are for the central nervous system and the cardiovascular system, which are all areas with high R & D failure rate Table 5 Mechanism of action (target) of discontinued drugs Top100 note: in the research including pre clinical, clinical and marketing stages, conclusion: the research and development of new drugs solves the unmet clinical needs, and as the drugs with better efficacy are gradually developed, it will be difficult to develop better new drugs at present, which requires us to have a comprehensive understanding of the current situation in the research and development field To determine the target for the project of targeted drug research and development, we need to understand the situation of the target in the research and the suspension of the research as well as the effectiveness and safety of the drug in the research In this paper, the ratio of listing / clinical / preclinical / suspension of the research is a macro reference index, in fact, more statistical analysis can be carried out for different disease fields, target types or small molecule / biological drug fields, Understand the current and future trends of new drug research and development in detail To be engaged in new drug development and know one another and one's friends, although it can't guarantee that there will be no danger in a hundred battles, it will not lead to death All of the above belong to the author's point of view If there is any inappropriateness, please criticize and correct it! Original statement: This article is the original manuscript of yaozhi.com, welcome to reprint, reprint please indicate the source, thank you!
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