Small-molecule market

Tab. 5.1 Worldwide sales of the top ten active pharmaceutical ingredients (APIs) in 2012 (Total small molecules market volume 828 billion Dollars).

Figure 1.2 Worldwide market for small molecule drugs that function as enzyme inhibitors in 2001 and projected for 2006. AAGR = average annual growth rate.

Pharmaceutical drug development of small molecules is initially based on the selection of candidate targets - mainly enzymes, receptors or circulating proteins that are currently targeted by 45, 28 and 11% of marketed compounds, respec-... 

Enzymes involved in TG synthesis continue to represent challenging and intriguing targets for small-molecule intervention against the worldwide epidemic of obesity, metabolic syndrome, and type 2 diabetes, as well as smaller market indications from rare familial diseases to veterinary use. There is also intriguing evidence that inhibition of these enzymes may be beneficial for diseases unrelated to the area of metabolic disorders, such... 

VDC polymer resistance to, 25 711 Small-molecule single-crystal structure determination, 26 423—425 Small molecules, mass spectrometry of, 15 666-667 Smallmouth bass aquaculture, 3 183 common and scientific names, 3 188t Small office home office (SOHO) markets, silica in, 22 376... 

Chemical-based products cover a broad spectrum of materials and forms, ranging from molecules to appliances. Table 16.1-1 shows the various product functional forms, along with examples in major application areas. Examples highlighted in italic are those discussed in this book. Most small molecules such as BTX (benzene-toluene-xyxlene) are sold to chemical and allied products industries while a limited number such as refrigerants and solvents are for sale in the consumer market. In contrast, multicomponent liquid mixtures such as liquid shampoo, semi-solids such as cream and paste, and structured solids such as controlled release herbicide are often sold directly to the consumers. Business-to-consumer sale is even more prevalent for ready-to-use devices and appliances such as diagnostic kits, drinking water filters and air cleaners. 

Strickley, R.J., Parenteral formulation of small molecules therapeutics marketed in the United States-Part III, PDA. Pharm. Sci. Tech., 54, 152, 2000. 

Most of the analyses of R D cosfs for new dug entities and their generic imitators have focused on small molecule NCES. This reflecfs the relative youth of the biotech industry. New biologic entities were first introduced in the 1980s. By 1994, only 29 new biological entities had been introduced into the U.S. market, but this number has increased dramatically since then. In this regard, 41 new biological introductions occurred between 1995 and 2001. 

The majority of active pharmaceutical ingredients on the market are small molecules derived from a synthetic route they are, partially badly, or not soluble in water. 

The first commercially available DPI system appeared on the market in 1949, developed and marketed by Abbott under the name Aerohaler. Like all early pulmonary drug-delivery devices, it delivered small-molecule compoimds (bronchodilators or inhaled corticosteroids) to the airways (not necessarily the deep limg) for the treatment of asthma or chronic obstructive pulmonary disease. Table 6 lists some of the early DPI systems used for asthma and COPD the energy somces in these devices were mechanical and patient inspiration. 

Development of small molecule inhibitors of protein-protein binding interactions has been notoriously difficult. The tremendous investment that the pharmaceutical industry has made in the development and marketing of whole protein... 

Two of the small molecule inhibitors, gefitinib (166, EGF receptor kinase inhibitor) and imat-inib (167, Bcr-Abl receptor kinase inhibitor), have reached the market. Although many of the starting leads for kinase inhibitors were obtained by random screening approaches, further medicinal chemistry was aided by the availability of a number of crystal structures and other modelling approaches The design of irreversible... 

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