Abstract
Background: The design and development of prodrugs is the most common and effective strategy to overcome pharmacokinetic and pharmacodynamic drawbacks of active drugs. A respected number of prodrugs have been reached the drugs market throughout history and the recent years have witnessed a significant increase in the use of prodrugs as a replacement of their parent drugs for an efficient treatment of various ailment. Methods: A Scan conducted to find recent approved prodrugs and prodrugs in development. Results: Selected prodrugs were reported and categorized in accordance to their target systems. Conclusions: the prodrug approach has shown many successes and still remains a viable and effective approach to deliver new active agents. This conclusion is supported by the recent approved prodrugs and the scan of clinical trials conducted between 2013–2018.
Highlights
Prodrugs are biologically inactive compounds that are activated post-administration to their pharmacologically active forms
The failure of a respected number of drug candidates during and after the drug development process is mainly attributed to poor pharmacokinetic properties including poor aqueous solubility, low permeation, short duration of action, and metabolism by the first-pass effect
One of the strategies to improve the pharmacokinetics profile for a drug is via utilizing the prodrug approach which is intended to overcome physicochemical, biological and organoleptic barriers of some of the currently marketed drugs suffering low bioavailability and patient incompliance
Summary
Prodrugs are biologically inactive compounds that are activated post-administration to their pharmacologically active forms. Among the successful examples are the prodrugs indented for the management of hypertension such as the angiotensin-converting enzyme inhibitors (ACEIs) and angiotensin receptor blockers (ARBs). Others are those used to inhibit platelet aggregation in the cases of clotting disorders and cardiac incidents such as clopidogrel and prasugrel. During the years 2008–2017, 12.4% of all new molecular entities approved by the FDA were prodrugs (31 out of 249) [2]. One might wonder whether recent clinical trials reflect the future of prodrugs as new treatments, parts of combined treatment regimens, or treatments for new indications other than their already approved ones.
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