β-lactam antibiotics are the most commonly used antibacterial drugs in clinical practice. Soon after Fleming reported the antibacterial effect of penicillin in 1929, antibacterial drugs began the antibiotic era. Although it has been used clinically for more than half a century, it is still the drug of choice for Gram-positive cocci (G+) infection due to its high efficiency and low toxicity.
Over the past 70 years, various antibiotics have been widely used in clinics, occupying a dominant position in the world antibiotic market, and have made great contributions to human health. According to a report by the British consulting firm Michael Barbar and Association, the sales of penicillin and cephalosporins in 1997 were US$11 billion.
In 1929, penicillin was used as the first β-lactam antibiotic in clinical practice. In 1945, cephalosporin C was discovered. In the structure of penicillin and cephalosporins, both contain β-lactam rings, which are representative drugs of β-lactam antibiotics.
In the 1960s and 1970s, semi-synthetic penicillins and cephalosporins with 6-aminopenicillanic acid (6-ApA) and 7-aminocephalosporanic acid (7-ACA) as nuclei were developed respectively. antibiotic. Since then, clavulanic acid (also known as clavulanic acid) and thiomycin have been discovered one after another.
On this basis, a series of atypical β-lactam antibiotics such as monocyclic β-propionamides, oxypenems, carbapenems, and carbacephem have been developed. β-lactam antibiotics selectively act on bacterial cell walls, while animal cells have no cell walls, so they are safe for humans.
This kind of antibiotics has a broad antibacterial spectrum, strong antibacterial activity, low toxicity, high industrial level, clear structure-activity relationship, and great flexibility. Therefore, they have been developed and applied in large numbers and will remain the mainstream of antibiotic development for a considerable period of time in the future.
β-lactam antibiotics include penicillins, cephalosporins, cephalosporins, monocyclic lactams and other atypical β-lactam antibiotics. The included ATC is classified as J1C, J1D.
The mechanism of action of various β-lactam antibiotics is similar, and they can inhibit cell wall mucopeptide synthase, namely penicillin binding proteins (PBPs), thereby hindering the synthesis of cell wall mucopeptides, causing bacterial cell wall defects and bacteria Body expansion and cracking. In addition, the lethal effect on bacteria should also include triggering the autolysin activity of the bacteria, and mutant strains lacking autolysin show resistance.
Animals have no cell wall and are not affected by β-lactam drugs. Therefore, this class of drugs has a selective bactericidal effect on bacteria and has low toxicity to the host. In the past ten years, it has been confirmed that the special protein PBPs on the bacterial cytoplasmic membrane is the target of β-lactam drugs. The number, molecular weight, and sensitivity of PBPs on the cell membrane of various bacteria are different, but bacteria with similar taxonomy have similar types and physiological functions of PBPs.
Global market overview
ATC is classified as J1C, β-lactam antibacterial drugs, and penicillin drugs show a V-shaped growth in the global market. It is expected that sales in 2020 will maintain a slow growth trend.
ATC is classified as J1D, and the global market for other β-lactam antibacterials shows a V-shaped growth. The sales of J1D drugs are expected to show a slow growth trend in 2020.
ATC classified as JIC (β-lactam antibacterial drugs, penicillins) global drug sales are shown in the table below. The top three countries in terms of sales volume are China, the United States and India. According to the 2020 world population ranking data, the top three are China, India, and the United States. The number of antibiotics used is closely related to the proportion of the population and the degree of economic development.
Overview of China's therapeutic drug market
The Chinese market for ATC classified as J1C, β-lactam antibacterial drugs, and penicillin drugs showed a V-shaped growth. It is expected that sales in 2020 will maintain a slow growth trend.
ATC is classified as J1D, and the Chinese market for other β-lactam antibacterials shows a V-shaped growth. The sales of J1D drugs are expected to show a slow growth trend in 2020.
The global sales of ATC classified as J1C drugs are approximately US$8 billion, and the Chinese market is approximately US$2 billion. The global ATC classification is US$12 billion in J1D category, and the Chinese market is about US$5 billion. The entire antibiotic market is huge. As existing antibiotics are becoming less sensitive and lack commercial benefits, new antibiotic treatments are needed to reshape the market.
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