Omeprazole-based fast follower approaches

The development of proton pump inhibitors (PPIs) for the treatment of gastric acid-related disorders is also one good example of how fast follower approaches can efficiently and effectively discover and develop compounds that allow newcomers to gain the market share in a given therapeutic area quickly. 

1) Stability in stomach and plasma prior to reaching the target proton pump. 

2) Quickly transforming into the active form once PPIs being in the acidic environment in the parietal cells. 

The strategies to address the two potential liabilities may be summarized as follows  

1) For an oral PPI, coating techniques were widely applied to protect the acid-liable PPI from being contacted with strong acid in the stomach, thus avoiding the PPI being transformed into the active compound before it gets into the parietal cells. 

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In summary, the omeprazole-based fast follower approaches identified key liabilities associated with omeprazole and put forward medicinal chemistry and formulation strategies to address these potential liabilities. The tactics used in addressing these points involved the following ... 

The following discussion will be centered on the application of the strategies and approaches for enzymatic stability improvement and p Tg fine-tuning, to improve the druggability for the omeprazole-based fast followers. The strategy of reformulating the omeprazole to overcome the solution instability issue associated with the original launched omeprazole can be found in other published reviews. 

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