Blockbuster compounds

In the 1970s and the 1980s, the pathways to the penicillins and the cephalosporins including cephamycin C were worked out especially after cell-free systems became available [59]. Late in the 1970s came reports on the production of P-lactam antibiotics which were neither penicillins nor cephalosporins. The most important was clavulanic acid from streptomycetes, which possessed only weak antibiotic activity but was an excellent inhibitor of P-lactamase [60]. It became a blockbuster compound by being coformulated with broad-spectrum semisynthetic penicillins which are susceptible to P-lactamase, for example, with amoxycillin, the combination is known as Augmentin. 

An HPLC assay, content uniformity and related compounds method for a blockbuster new drug product, was developed that utilized concave gradient elution, a flow rate of 1.25 ml/min and no temperature control of the column. Samples were placed in 1000-ml volumetric flasks, sample diluent was added, and the flasks were sonicated for 10 min followed by 30 min of mechanical shaking. This method was to be run in a QC laboratory at the contract manufacturing facility in Puerto Rico. While the developed method worked flawlessly in the development laboratory, the QC laboratory had many problems in performing the procedure. 

With the patent on its blockbuster allergy medicine Claritin set to expire in December 2002, Schering-Plough sued potential generics makers, claiming that they would violate a separate patent on the chemical compound (or metabolite) that is produced in the liver when the pill is swallowed. 

Leo Stembach is also responsible for more than 100 patented compounds without benefit of high- throughput screening to assist him. Perhaps his main legacy is that he created the dream of all dmg companies with his blockbuster. They want a few products that are easy to market, and they should all sell a lot. 

It turned out that the nearly discarded substance had a novel structure, 5, a chlordiazepoxide. It was developed further and became known under the trade name Librium , which was the first antianxiety agent. Librium became the lead compound for the development of many other compounds with related structures. The best known is the diazepam Vh/ium , 6, a tranquilizer used to treat anxiety, muscle spasm, and symptoms of epilepsy. Today, about 40 diazepines are in the market. Nearly forgotten on the laboratory shelf, Librium and Valium became blockbuster drugs that fueled the growth of the Roche company. (Drugs are called blockbusters when sales are much higher than US 1 billion per year.)... 

In 1976 Syntex introduced its follow-up anti-arthritic drug, Naprosyn, which quickly became one of the world s top-selling drugs, and Syntex s major profits source. But, despite sustained emphasis on research and the development of new compounds, Syntex was unable to bring forth another blockbuster on the scale of Naprosyn. As Gambardella points out, the company remained really on the boundary between being a pure research company and true manufacturer with significant development and distri-... 

The large family of medicines known as nonsteroidal anti-inflammatory drags (NS AID, 3.3) today also owes its existence to primitive observations about the effect of the willow Salix in Latin). In this case, it was not the original compound, but a chemical derivative that became a blockbuster drag. The taste of willow bark is bitter, and similar to the taste of the bark of a South American plant Cinchona, which is an effective treatment against malaria. As well as the taste, the effect was also similar willow bark seemed to possess an antifever property. Today, it has been established that salicin is the active ingredient, but a simpler derivative named acetylsalicylic acid proved to be more potent (— 3.25), and is currently sold under the trade name Aspirin. 

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