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    Home > Medical News > Latest Medical News > Development and market analysis of peptide drug technology

    Development and market analysis of peptide drug technology

    • Last Update: 2019-05-31
    • Source: Internet
    • Author: User
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    Polypeptide usually refers to the peptide chain composed of no more than 50 amino acids, which is between small molecular drugs (molecular weight 5000) Because peptides are involved in many physiological functions as signal molecules in the body, peptide drugs often play the role of alternative therapy to make up for the lack of endogenous peptide hormones Peptide drugs have been widely recognized and widely used in clinical treatment (Table 1) Table 1 Source of early peptide drugs: bioorganic & medical chemistry research found that no matter what period, the number of natural peptide R & D projects has been small, and the research and development enthusiasm of peptide analogues has never decreased, while the number of heteropolypeptides has increased since 2000, reflecting the development and change of peptide synthesis technology from the side (Figure 1) Figure 1 Types and distribution of clinical peptide candidates in different periods source: bioorganic & Medical Chemistry peptide synthesis (peptide chain synthesis) essentially arranges amino acid units according to the structural rule of natural amino acids In order to synthesize polypeptides with specific sequence, only the directed peptide synthesis method can be used, that is, protecting the amino or carboxyl groups which do not need to be reacted with appropriate groups first, and then conducting the connection reaction At present, peptide synthesis methods are mainly chemical and biological methods (Fig 2) The biosynthesis of polypeptides mainly includes fermentation, enzymolysis and so on With the development of bioengineering technology, the gene engineering method, which is dominated by DNA recombination technology, has also been applied to the synthesis of polypeptides Figure 2 Peptide synthesis method source: in the 1980s, the peptide length in almost all clinical trials was less than 10 amino acids (Figure 3) In the next decade, the average length of polypeptide increased gradually, which was mainly due to the improvement and maturity of peptide synthesis technology At present, the long peptide chain with 40 amino acids can also be successfully developed, indicating that the peptide chain length is no longer the difficulty of peptide drug development Figure 3 Peptide chain length of peptide drugs in different clinical trial stages source: bioorganic & medical chemistry is extracted from nature to synthesis As a new drug, peptide has unique advantages in clinical application and production preparation Firstly, it is similar to recombinant protein medicine and monoclonal antibody medicine in clinical, with strong specificity and good efficacy; secondly, peptide medicine is similar to small molecular medicine in production and preparation, with high purity, controllable quality and easy to determine structure, so peptide therapy has been considered as a potential therapy with high selectivity, effectiveness and relative safety Although peptide therapy has a bright future, it is not perfect Due to the existence of peptidase, the half-life of polypeptide hormone is usually short, which has a negative impact on drug development and treatment Another technical bottleneck of peptide drugs is the low oral utilization rate In order to overcome these technical problems, a new peptide synthesis strategy has emerged in recent years By adjusting the pharmacokinetic characteristics, modifying the amino acid skeleton, adding unnatural amino acids, conjugating the extended half-life groups and improving the solubility, the researchers can reduce the injection frequency of peptide drugs and improve the stability and other physical properties Among them, conjugated binding groups have become an important means to change the properties of polypeptide drugs Since 2010, about 30% of peptide drugs in clinical trials in the world are conjugates (Figure 4), such as structural coupling with polyethylene glycol, lipid and protein It has been proved that the conjugated Fc fragment can prolong the half-life of the peptide, and the peptide drug conjugates can also be used as the payloads and transporters of cytotoxic agents Some common peptide drug conjugates are shown in Table 2 Figure 4 Proportion of peptide drug coupling substances at different stages of clinical trials Table 2 Analysis of some common peptide drug coupling substances source: bioorganic & Medical Chemistry from the perspective of market, in recent years, the compound growth rate of global peptide drug market is more than 12%, and the market scale is close to 20 billion US dollars According to the report of transparency market research, the global peptide drug market is expected to reach US $23.7 billion in 2020, and the peptide drug market is in the rising stage of development as a whole, which has also become an important direction of new drug research and development for foreign pharmaceutical companies For example, pharmaceutical giants such as Pfizer, Merck, Roche, Lilly, Novartis, Sanofi, Bayer and other large multinational pharmaceutical enterprises have increased investment in polypeptide drug research and development through acquisition or merger, and have harvested many listed drugs The world's representative heavy peptide drugs, such as liraglutide, dulaglutide, glatiramelacetate, leuproreline, octreotide, goserelin and exenatide, etc According to the research analysis and development trend forecast report of peptide drug industry in China 2019-2025 released by China industry research network, the scale of peptide drug industry in China has also shown an upward trend in recent years (Figure 5), which is due to the large population base and the increasing aging of China, the presence of a large number of tumor patients and chronic disease patients, the market demand is expected to continue to expand, and the peptide drug industry is still growing There is room for substantial growth Figure 5 In recent years, China's peptide drug market scale (100 million yuan), but compared with developed countries, there is still a large gap in China's peptide drug industry, and the product structure is also different Generally speaking, the immune enhancement products are mostly, while the major or urgent varieties for tumors, diabetes, rare diseases and other major diseases account for less, and the market is still immature and far from saturated According to the cortellis database, as of May 7, 2019, there are 1153 kinds of peptide synthetic drugs in the world and 198 kinds of peptide drugs on the market in 2018, with a wide range of indications, including tumors, cardiovascular diseases, major diseases of endocrine and metabolic diseases or more common diseases, among which the number of drugs for tumors is the largest, and the distribution of different indications is shown in Figure 6 Figure 6 Indication distribution of polypeptide drugs source: cortellis in general, polypeptide drugs have many advantages over traditional drugs, and the global clinical market demand is growing It can be predicted that with the progress of modern synthesis technology, there will be more and more new peptide drugs on the market in the future, which will bring good news to the majority of patients References: 1 Historical perspectives, current development trends, and future directions bioorganic & Medical Chemistry 26 (2018) 2700 – 2707; 2 In depth report on polypeptide industry in pharmaceutical and biological industry: patent cliff gives birth to industry opportunities research progress on polypeptide drugs Fortune Securities 20160905 3 Development status of polypeptide drugs pharmaceutical progress 2014,38 (3): 196-202 4 Peptide synthesis method: Hefei guopeptide biology https:// 5 Peptide drug market expansion drives the output value of peptide drug industry in China to increase 15 times in 9 years https://
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