The Technical Challenge
The design of drugs that are both effective and can be given by mouth
has been likened to the design requirements of a flying submarine (Testa & Caldwell,
As shown above, each member of the design team has a need that the other cannot fulfill. Further, it is hard to imagine what compromise position will result until many, many working models have been built and tested. Although the problem may ultimately have an elegant solution, it is likely that vast sums of money and time will be spent to find it.
This analogy is not too far off the mark in describing the development of oral drugs. Specifically, the needs of those scientists who are trying to develop the most potent drug possible are often not fulfilled by those attempting to deliver the drug by mouth, and vice versa. The two groups often have divergent requirements for the drug’s structure. Worse still, a bioavailability failure of an initial drug candidate does not lead to much useful information for the trip back to the blackboard …
“Once a New Chemical Entity has been identified, the realistic prospect of improving its pharmacokinetic profile by rational drug design is slim, even if pharmacokinetic criteria have been included in the selection process.” –Testa & Caldwell, 1996.
Boosting provides a new strategy for success.
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Copyright BAS 2007