Detailed data of small molecule targeted drugs

Small molecule drugs mainly refer to chemical synthetic drugs, usually organic compounds with molecular weight less than 1000. Small molecule drugs have the advantages of wide application and mature theory. According to statistics, among the commonly used drugs, the number of small molecule drugs can account for 98% of the total.

Definition, action characteristics: the difference, development status and prospect of small molecular drugs, small molecular drugs and macromolecular drugs commonly used in clinic. The definition of small molecule drugs mainly refers to chemically synthesized drugs, usually organic compounds with molecular weight less than 1000. Characteristics of action: The structure of small molecular drugs has good spatial dispersion, and its chemical properties determine its good pharmaceutical and pharmacokinetic properties. These characteristics make small-molecule drugs show great advantages in the process of drug research and development and other drug fields, and small-molecule drug research and development is increasingly favored by the market. Small molecule drugs commonly used in clinic are usually signal transduction inhibitors, which can specifically block the necessary signal transduction pathways in the process of tumor growth and proliferation, thus achieving the purpose of treatment. For example, Gleevec (commonly known as emitinib) produced by Novartis Pharmaceutical for the treatment of chronic myeloid leukemia and gastrointestinal stromal tumors, Iressa (commonly known as gefitinib) produced by AstraZeneca for the treatment of EGFR-targeted non-small cell lung cancer, and Trocquer (commonly known as Roche, Switzerland) all belong to this category and have entered clinical applications. Velcade (commonly known as bortezomib) produced by American Millennium Pharmaceutical Company is an apoptosis inducer and a small molecule drug. Aspirin: Also known as acetylsalicylic acid, o- acetylsalicylic acid, with the chemical name of 2- (acetoxy)-benzoic acid, is a classic non-steroidal anti-inflammatory drug which was born in 18 in the late 1980s. Because of its good antipyretic and anti-rheumatic effects, it has become one of the most widely used drugs. In 1960s, it was found that it had good antithrombotic effect and was widely used in the prevention and treatment of cardiovascular and cerebrovascular diseases. Vitamin C: Vitamin C (also called L- ascorbic acid) is white crystal or crystalline powder; Tasteless, stomach acid; After a long time, the color gradually turns yellow; Acidic reaction of aqueous solution. There are four optical isomers of vitamin C in chemical structure, among which L- configuration dextrorotation has the strongest biological activity. The difference between small molecule drugs and large molecule drugs is 1. Biological macromolecular drugs (including polypeptides, protein, antibodies, polysaccharides and nucleic acids, etc. ) It is mostly used to treat tumor, AIDS, cardiovascular and cerebrovascular diseases, hepatitis and other major diseases. 2. Small molecule drugs: usually signal transduction inhibitors, can specifically block the signal transduction pathways necessary for tumor growth and proliferation, thus achieving the purpose of treatment. 3. Small molecule drugs are absorbed by the power provided by concentration gradient, while large molecule drugs need protein active transport of digestive tract epithelial cells. Some drugs are decomposed by digestive enzymes secreted by the digestive tract and need to be injected. Small molecule drugs have the advantages of wide application and mature theory. According to statistics, among the commonly used drugs, the number of small molecule drugs can account for 98% of the total. In recent years, it has been found that small molecule drugs bring hope to the treatment of refractory hepatitis C and AIDS. Although small-molecule drugs have achieved encouraging results in the treatment of patients with refractory chronic hepatitis C and AIDS, which brings hope to these patients, they still face many challenges: First, the efficacy of small-molecule drugs is based on the joint standard scheme. If the drug is not used according to the drug standard, the side effects of the drug will increase, and the patient's tolerance will decrease, resulting in poor treatment effect. Secondly, although monotherapy with small molecule drugs, especially protease inhibitors, can achieve ideal HCV inhibition effect, HCV is prone to drug-resistant mutation, which can occur about 2 weeks after treatment. In addition, small molecular drugs are prone to multiple drug resistance sites after taking drugs. In a word, the research of small molecule drugs is in the ascendant, and new drugs appear constantly, which brings hope to some patients with refractory hepatitis C and becomes an important direction of anti-cancer and anti-tumor drug treatment research. With the continuous development of this kind of drugs with low drug resistance, high curative effect and few side effects, and the research of new drug combination schemes, it is believed that it will bring new breakthroughs to the treatment of a large number of refractory diseases in the near future. The development of small molecular drugs has reached a plateau (bottleneck), and the annual development speed is fixed in an interval, which is difficult to break through. This is not only reflected in the number of new drugs listed in a certain range every year, but more importantly, pharmaceutical R&D enterprises invest more and more every year, but there is no breakthrough in results. Because it is in the platform period, it is only a matter of time before small molecule drugs are caught up or surpassed. In the next few decades, the market share of macromolecular drugs will be higher and higher, gradually surpassing that of small molecular drugs. However, this does not mean that small-molecule drugs will disappear, nor can it be said that small-molecule drugs will have no future. It can only show that this kind of drug has begun to make steady progress, not accelerate it.