About: Metabolic Efficacy of Phosphate Prodrugs and the Remdesivir Paradigm

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An Entity of Type : schema:ScholarlyArticle, within Data Space : covidontheweb.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
title	Metabolic Efficacy of Phosphate Prodrugs and the Remdesivir Paradigm
Creator	Wiemer, Andrew
source	Medline; PMC
abstract	[Image: see text] Drugs that contain phosphates (and phosphonates or phosphinates) have intrinsic absorption issues and are therefore often delivered in prodrug forms to promote their uptake. Effective prodrug forms distribute their payload to the site of the intended target and release it efficiently with minimal byproduct toxicity. The ability to balance unwanted payload release during transit with desired release at the site of action is critical to prodrug efficacy. Despite decades of research on prodrug forms, choosing the ideal prodrug form remains a challenge which is often solved empirically. The recent emergency use authorization of the antiviral remdesivir for COVID-19 exemplifies a new approach for delivery of phosphate prodrugs by parenteral dosing, which minimizes payload release during transit and maximizes tissue payload distribution. This review focuses on the role of metabolic activation in efficacy during oral and parenteral dosing of phosphate, phosphonate, and phosphinate prodrugs. Through examining prior structure–activity studies on prodrug forms and the choices that led to development of remdesivir and other clinical drugs and drug candidates, a better understanding of their ability to distribute to the planned site of action, such as the liver, plasma, PBMCs, or peripheral tissues, can be gained. The structure–activity relationships described here will facilitate the rational design of future prodrugs.
has issue date	2020-07-24(xsd:dateTime)
bibo:doi	10.1021/acsptsci.0c00076
bibo:pmid	32821882
has license	no-cc
sha1sum (hex)	6981501d002c5b48ef7bb2dc2de9f7824c1236b8
schema:url	https://doi.org/10.1021/acsptsci.0c00076
resource representing a document's title	Metabolic Efficacy of Phosphate Prodrugs and the Remdesivir Paradigm
has PubMed Central identifier	PMC7409933
has PubMed identifier	32821882
schema:publication	ACS Pharmacol Transl Sci
resource representing a document's body	covid:6981501d002c5b48ef7bb2dc2de9f7824c1236b8#body_text
is schema:about of	named entity 'drugs' named entity 'distribution' named entity 'focuses' named entity 'COVID-19' named entity 'led' »more»

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