1. Peptide analogues are hot spots in research and development

2. Polypeptide drugs have been widely recognized and used in clinical practice.

3. Advantages and disadvantages of peptide drugs

4. Rapid development of peptide drug market

In recent years, the global peptide drug market as a whole is in the rising stage of development. The compound growth rate of market scale is more than 12%, and the market scale is close to 20 billion US dollars. According to a report released by transparency market research, the global peptide drug market is expected to reach US $23.7 billion by 2020. Peptide drugs have also become one of the important directions of new drug research and development.

Peptide analogues are hot spots in research and development

Polypeptide usually refers to the peptide chain composed of no more than 50 amino acids, which is between small molecular medicine (molecular weight < 500) and protein medicine (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.

Polypeptide drugs have been widely recognized and used in clinical practice.

For a long time, the number of natural peptide research and development projects is small, but the enthusiasm of the pharmaceutical industry for peptide analogues research and development has never decreased, especially for heteropolypeptides. Since 2000, the number of research and development has been increasing, which also reflects the development and change of peptide synthesis technology.

The essence of peptide synthesis is to arrange the amino acid units according to the structure 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, the main methods of peptide synthesis are chemical synthesis and biosynthesis. Chemical synthesis mainly includes solid-phase synthesis and liquid-phase synthesis, and biosynthesis mainly includes fermentation, enzymolysis, etc.

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.

In the 1980s, almost all peptides in clinical trials were less than 10 amino acids in length. In the next 10 years, the average length of polypeptide gradually increased, which is mainly due to the continuous maturity and improvement of peptide synthesis technology. At present, the long peptide chain with the length of 40 amino acids can also be successfully developed, indicating that the peptide chain length is no longer the difficulty of peptide drug development.

Advantages and disadvantages of peptide drugs

From natural extraction to artificial synthesis, polypeptide, as a new drug, has shown unique advantages in clinical application and production. In clinic, peptide drugs are similar to recombinant protein drugs and monoclonal antibody drugs, which have the advantages of strong specificity and good curative effect. In the way of production and preparation, peptide drugs are close to small molecular drugs, with the characteristics of high purity, controllable quality and easy to determine the structure, so at present, multi 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 clinical 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 reduce the injection frequency of peptide drugs and improve their 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, 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 payload and transporter of cytotoxic agents (see table for some common peptide drug conjugates).

Rapid development of peptide drug market

In recent years, with the rapid development of the global peptide drug market, peptide drugs have become an important direction of new drug research and development at home and abroad. For example, Pfizer, Merck, Roche, Lilly, Novartis, Sanofi, Bayer and other large multinational pharmaceutical enterprises have increased their investment in peptide drug research and development through acquisition or merger, and have harvested many listed drugs. The world's representative peptide drugs are beneficial to larutin, dulaglutide, galatirine, leuprorelin, octreotide, goserellin and exenatide.

According to the research analysis and development trend forecast report of peptide drug industry in China from 2019 to 2025 released by China industry research network, the market scale of peptide drugs in China has also been on the rise in recent years, reaching RMB 63.5 billion in 2017 (see Figure), which is due to the large population base, aging and a large number of patients with cancer and chronic diseases. It is expected that the market demand will continue to expand in the future, and there is still a large growth space for peptide drugs.

Compared with developed countries and regions, there is still a big gap in the field of polypeptide drugs in China, and there are also differences in product structure, among which immunoenhancement products are the majority, while products for tumors, diabetes, rare diseases, etc. account for a relatively small proportion, 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, 198 kinds of peptide drugs on the market in 2018, with a wide range of indications, including major or more common diseases such as tumors, cardiovascular diseases, endocrine and metabolic diseases, among which the number of drugs for tumors is the largest.

In general, peptide 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, more and more new peptide drugs will be on the market in the future, bringing good news to the majority of patients.

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Chengdu Shengnuo Biotechnology Co., Ltd. has "Chengdu polypeptide drug engineering technology research center" in Chengdu, mainly engaged in polypeptide, polypeptide drug and beauty peptide research. Our zero defect has passed the FDA certification, and now it has become the first-class professional peptide drug and product development, technology transfer, technical service and peptide drug industry in the scale production and export of China's parks.