The present situation of the synthesis of new drug research and development trend
2013/8/16 view:
When China became a member of the world trade organization (WTO), the protection of intellectual property rights of pressure surge, the competition of world technology protection and technological innovation, foreign drug patent protection period couldn't be generic. This brings to the study on the synthesis of new drugs in the severe challenge, but also brings new opportunities.
In the face of the pressure of the drug patent protection, some people think that China's domestic drug innovation way out lies in the characteristic of traditional Chinese medicine (TCM), development technology for TCM modernization. Seems to synthesis of new drugs is no longer comply with China's national conditions. Admittedly, modern biological technology, gene engineering technology and the rapid development of the technology for TCM modernization will open a new land to the discovery of new drugs. But still as the main body of clinical application of new drug research and development of drugs, chemical synthesis also nots allow to ignore.
In the history of China's drug innovation, our original chemical synthetic drug varieties to near zero. The present situation of the synthesis of innovative drugs in China is serious, it is no wonder that many scholars have prospects to the chemical synthesis of innovative drug research in China hold a negative attitude.
1 chemicals production status in our country
Since reform and opening up, China's pharmaceutical industry development speed, speed increases by about 20% a year development, medicine and industrial output increased from $1978 in 6.4 billion to 1978 in 2 33 billion yuan. Medium scale chemical pharmaceutical factory in China more than 4, 000, 24 categories can produce over 400 kinds of active pharmaceutical ingredients 1 preparation 4 more than 000 kinds. Relatively complete varieties of chemicals in China, it can meet the clinical needs, API exports also account for considerable proportion in the international market. But compared with developed countries, our country's pharmaceutical output is quite low, to be developed.
2 the status quo of chemical synthetic drugs
2.1 a serious shortage of funding pharmaceutical industry is too small, the majority of small and medium-sized enterprises, most enterprises have no advantage varieties, low production profit, typically struggle on the break-even line. Therefore unable to create your own research and development system. Most enterprises due to insufficient funds, even it is difficult to complete basic scientific instruments, equipment backward, backward technology, do not have the ability to copy foreign patent medicine.
2.2 low level of scientific research talents, lack of innovative talents, colleges and universities, research institutes and some of the larger pharmaceutical enterprise although has its own research and development system, is devoted to the synthesis of new drug research. But on the chemical synthesis of drug research, almost all go generic foreign patent medicines and outstanding (maturity). The author as a new drug review committee of shaanxi province has also reviews some domestic colleges and scientific research institutes and enterprise institute, a new drug to declare, they adopt the synthesis route and preparation technology is almost 100% to copy the contents of the foreign patent specification, not a spark of innovation research. And even at the very least, foreign literature retrieval is poor, the only source most of pharmacology, toxicology, clinical research data is also foreign product manuals.
2.3 synthetic drug research topic selection project level is poor, most of repeated reporting frequency high medical research unit subject ability is poor, as long as there is a research unit in the domestic first declare new synthetic drug varieties, as long as the pre-clinical research report, the result of several units, and rush to declare, leading to even generic drugs is also a listed is in fierce competition.
2.4 development level low dosage form a single, backward technology, accessories varieties on the quantity and quality lags far behind the foreign advanced enterprise, poor competitiveness, it is difficult to enter the international market. Pharmaceutical output and advanced countries is the main source of the drug product global sales.
3 the world synthetic study the current situation and trend of development of new drugs
The present situation of current world synthesis innovative drug research is that the synthetic drugs all kinds of other products as listed in succession, the discovery of new drugs in slowing the speed of the monomer compounds, research and development cost is higher and higher, the annual cost of drug research and development has more than $40 billion, more than $1982 in 5.4 billion increased by 8 times. The British international drug research center report in 1988/98 time, 10 a listed on the world market, 460 kinds of new molecular ontology, and the least Numbers came in 1998, only 35 species of new molecular ontology. And in the past two years listed continue to decrease in the number of new molecular ontology. In the listing of new products in recent years, anti-infection drugs, cardiovascular drugs, central nervous system drugs, cancer drugs dominate. Due to the difficulty of the drug discovery of new molecular ontology is more and more big, the world's big drug companies drug research institutions are increasing investment, the development of high-tech, new molecular ontology by using high and new technology to find new drugs
3.1 through the use of molecular biology, structural biology, electronics, spectroscopy, chemical and genetic recombination, molecular cloning, computer, graphics, calculation, retrieval and processing technology, such as technology, the research of therapeutic targets the structure and function of biological molecular targets, and on this basis, through by modifying the structure of existing small molecules certain drugs or designing new drugs of small molecules, and study the target molecule and the interaction between drug molecules and small molecules of these modified or innovative drugs for the purpose of screening to discover new drugs, and carries on the research of the system. 3.2 by using combinatorial chemistry method found new drugs. Compared with the traditional chemical synthesis and combinatorial chemistry synthesis of compound A1 to An with compound B1 to Bn each combination to provide the possibility of combining, using reliable and simple chemical reaction purification technology (such as solid phase reaction technology) systematically repeatedly trace to the preparation of the combination of different compounds, the diversity of compounds is set up
3.3 from existing containing chiral carbon atoms without the resolution of racemic form outside sell drugs as a starting point, racemic resolution, respectively, to study the activity of the two enantiomers, choose one of the most active enantiomers, again carries on the stereoselectivity synthesis or asymmetric synthesis and racemic resolution research.
3.4 continue to separate extracted from plants and animals, or microorganisms have known chemical structure of new compounds to study the chemical synthesis method, is still one of the task of synthesis of new drugs.
3.5 research and development of advanced synthesis technology, such as chemical synthesis, chemical synthesis, electrochemical synthesis, microwave solid-phase reaction, nanotechnology, shock wave advanced synthesis technology such as chemical synthesis, select new catalyst, the environmental friendly synthetic technology and the new type of efficient separation technology, to transform the existing synthetic drug with the new technology of production process and is one of the development trend of synthetic drug research.
4 the current way of synthesis of new drug research in China with the task
The situation of fierce competition in the face of the world's innovation drugs, the state has pioneered in the development of our country with independent intellectual property rights, prevention and clinical treatment of urgent need and curative effect of prominent new chemical synthetic drugs, chiral small molecule drugs, synthetic peptides, nucleic acid drugs and carbohydrate synthesis of drugs and the prevention and control of major diseases included in China's current priority to the development of high and new technology industry focus areas to guide the national ministry of science and technology in December 1998 - formally approved the first batch of 15 national major fundamental research projects include "the discovery of drug leads structure and optimize the important disease innovation" project. So our emphasis on innovative drug research.
But be innovative drug research field in our country made the quick results we have very hard work to do, must continue to increase the intensity of pharmaceutical enterprise optimize combination, develop a number of large-scale pharmaceutical group enterprise, through strengthen the consolidation of medical market and management, to ensure that enterprises should get profit, pharmaceutical production enterprises shall ensure that large pharmaceutical enterprise innovative drug research funding; Strengthen the training of innovative drug research. Universities and colleges, scientific research institutes of new drug research and development and enterprise joint development road to go. The combination of capital, technology is the precondition of innovation research; For foreign patents expired, but there is still a development prospect of drug can still copy, but it must be on the synthesis process and the preparation technology to innovate; Using the known drug's mechanism and structure-activity relationship of research results, based on the analysis of the chemical structure of known drug, the drug design synthesis of derivatives and structural analogues and related compounds, and through the pharmacology of the system
5 to discuss
To sum up, the protection of intellectual property rights rules for drug synthesis innovation in our country has brought serious challenges, but also brings us a new opportunity at the same time, the pressure will force synthesis of new drug research in China on the road of independent innovation, will force us to shorten the gap with developed countries, prompted the synthesis technique of innovative drugs in China walk in the forefront of the world.
In the face of the pressure of the drug patent protection, some people think that China's domestic drug innovation way out lies in the characteristic of traditional Chinese medicine (TCM), development technology for TCM modernization. Seems to synthesis of new drugs is no longer comply with China's national conditions. Admittedly, modern biological technology, gene engineering technology and the rapid development of the technology for TCM modernization will open a new land to the discovery of new drugs. But still as the main body of clinical application of new drug research and development of drugs, chemical synthesis also nots allow to ignore.
In the history of China's drug innovation, our original chemical synthetic drug varieties to near zero. The present situation of the synthesis of innovative drugs in China is serious, it is no wonder that many scholars have prospects to the chemical synthesis of innovative drug research in China hold a negative attitude.
1 chemicals production status in our country
Since reform and opening up, China's pharmaceutical industry development speed, speed increases by about 20% a year development, medicine and industrial output increased from $1978 in 6.4 billion to 1978 in 2 33 billion yuan. Medium scale chemical pharmaceutical factory in China more than 4, 000, 24 categories can produce over 400 kinds of active pharmaceutical ingredients 1 preparation 4 more than 000 kinds. Relatively complete varieties of chemicals in China, it can meet the clinical needs, API exports also account for considerable proportion in the international market. But compared with developed countries, our country's pharmaceutical output is quite low, to be developed.
2 the status quo of chemical synthetic drugs
2.1 a serious shortage of funding pharmaceutical industry is too small, the majority of small and medium-sized enterprises, most enterprises have no advantage varieties, low production profit, typically struggle on the break-even line. Therefore unable to create your own research and development system. Most enterprises due to insufficient funds, even it is difficult to complete basic scientific instruments, equipment backward, backward technology, do not have the ability to copy foreign patent medicine.
2.2 low level of scientific research talents, lack of innovative talents, colleges and universities, research institutes and some of the larger pharmaceutical enterprise although has its own research and development system, is devoted to the synthesis of new drug research. But on the chemical synthesis of drug research, almost all go generic foreign patent medicines and outstanding (maturity). The author as a new drug review committee of shaanxi province has also reviews some domestic colleges and scientific research institutes and enterprise institute, a new drug to declare, they adopt the synthesis route and preparation technology is almost 100% to copy the contents of the foreign patent specification, not a spark of innovation research. And even at the very least, foreign literature retrieval is poor, the only source most of pharmacology, toxicology, clinical research data is also foreign product manuals.
2.3 synthetic drug research topic selection project level is poor, most of repeated reporting frequency high medical research unit subject ability is poor, as long as there is a research unit in the domestic first declare new synthetic drug varieties, as long as the pre-clinical research report, the result of several units, and rush to declare, leading to even generic drugs is also a listed is in fierce competition.
2.4 development level low dosage form a single, backward technology, accessories varieties on the quantity and quality lags far behind the foreign advanced enterprise, poor competitiveness, it is difficult to enter the international market. Pharmaceutical output and advanced countries is the main source of the drug product global sales.
3 the world synthetic study the current situation and trend of development of new drugs
The present situation of current world synthesis innovative drug research is that the synthetic drugs all kinds of other products as listed in succession, the discovery of new drugs in slowing the speed of the monomer compounds, research and development cost is higher and higher, the annual cost of drug research and development has more than $40 billion, more than $1982 in 5.4 billion increased by 8 times. The British international drug research center report in 1988/98 time, 10 a listed on the world market, 460 kinds of new molecular ontology, and the least Numbers came in 1998, only 35 species of new molecular ontology. And in the past two years listed continue to decrease in the number of new molecular ontology. In the listing of new products in recent years, anti-infection drugs, cardiovascular drugs, central nervous system drugs, cancer drugs dominate. Due to the difficulty of the drug discovery of new molecular ontology is more and more big, the world's big drug companies drug research institutions are increasing investment, the development of high-tech, new molecular ontology by using high and new technology to find new drugs
3.1 through the use of molecular biology, structural biology, electronics, spectroscopy, chemical and genetic recombination, molecular cloning, computer, graphics, calculation, retrieval and processing technology, such as technology, the research of therapeutic targets the structure and function of biological molecular targets, and on this basis, through by modifying the structure of existing small molecules certain drugs or designing new drugs of small molecules, and study the target molecule and the interaction between drug molecules and small molecules of these modified or innovative drugs for the purpose of screening to discover new drugs, and carries on the research of the system. 3.2 by using combinatorial chemistry method found new drugs. Compared with the traditional chemical synthesis and combinatorial chemistry synthesis of compound A1 to An with compound B1 to Bn each combination to provide the possibility of combining, using reliable and simple chemical reaction purification technology (such as solid phase reaction technology) systematically repeatedly trace to the preparation of the combination of different compounds, the diversity of compounds is set up
3.3 from existing containing chiral carbon atoms without the resolution of racemic form outside sell drugs as a starting point, racemic resolution, respectively, to study the activity of the two enantiomers, choose one of the most active enantiomers, again carries on the stereoselectivity synthesis or asymmetric synthesis and racemic resolution research.
3.4 continue to separate extracted from plants and animals, or microorganisms have known chemical structure of new compounds to study the chemical synthesis method, is still one of the task of synthesis of new drugs.
3.5 research and development of advanced synthesis technology, such as chemical synthesis, chemical synthesis, electrochemical synthesis, microwave solid-phase reaction, nanotechnology, shock wave advanced synthesis technology such as chemical synthesis, select new catalyst, the environmental friendly synthetic technology and the new type of efficient separation technology, to transform the existing synthetic drug with the new technology of production process and is one of the development trend of synthetic drug research.
4 the current way of synthesis of new drug research in China with the task
The situation of fierce competition in the face of the world's innovation drugs, the state has pioneered in the development of our country with independent intellectual property rights, prevention and clinical treatment of urgent need and curative effect of prominent new chemical synthetic drugs, chiral small molecule drugs, synthetic peptides, nucleic acid drugs and carbohydrate synthesis of drugs and the prevention and control of major diseases included in China's current priority to the development of high and new technology industry focus areas to guide the national ministry of science and technology in December 1998 - formally approved the first batch of 15 national major fundamental research projects include "the discovery of drug leads structure and optimize the important disease innovation" project. So our emphasis on innovative drug research.
But be innovative drug research field in our country made the quick results we have very hard work to do, must continue to increase the intensity of pharmaceutical enterprise optimize combination, develop a number of large-scale pharmaceutical group enterprise, through strengthen the consolidation of medical market and management, to ensure that enterprises should get profit, pharmaceutical production enterprises shall ensure that large pharmaceutical enterprise innovative drug research funding; Strengthen the training of innovative drug research. Universities and colleges, scientific research institutes of new drug research and development and enterprise joint development road to go. The combination of capital, technology is the precondition of innovation research; For foreign patents expired, but there is still a development prospect of drug can still copy, but it must be on the synthesis process and the preparation technology to innovate; Using the known drug's mechanism and structure-activity relationship of research results, based on the analysis of the chemical structure of known drug, the drug design synthesis of derivatives and structural analogues and related compounds, and through the pharmacology of the system
5 to discuss
To sum up, the protection of intellectual property rights rules for drug synthesis innovation in our country has brought serious challenges, but also brings us a new opportunity at the same time, the pressure will force synthesis of new drug research in China on the road of independent innovation, will force us to shorten the gap with developed countries, prompted the synthesis technique of innovative drugs in China walk in the forefront of the world.
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