In the past, prodrug design and development was focused on solving problems with existing drugs approved for marketing. Therefore, bridging data to existing documentation and clinical experience with the active drug was widely accepted by regulatory bodies, thus, resulting in simplified and shortened development for such prodrugs. This has, however, changed and as prodrug design is becoming an integral part of drug discovery it is in principle no different from development of a per se pharmacologically active molecule. Thus, from a development and regulatory perspective, a prodrug is regarded as a novel chemical entity (NCE) having one—and preferably only one— major pharmacological active metabolite i.e., the active drug. Consequently, there are no specific guidelines or regulatory requirements for developing a prodrug. However, the fact that prodrugs are designed to undergo extensive and often fast metabolism in vivo does increase the complexity and the pitfalls during development.
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